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Said M. Sebti, PhD

Where You Are:
Said M. Sebti, PhD

Senior Member

Office  (813) 745-6734

Education And Training
  • Postdoctoral Fellow, Yale University, New Haven, CT, 1987 - Pharmacology
  • PhD, Purdue University, Lafayette, IN, 1984 - Biochemistry
  • BS, Washington State University, Pullman, WA, 1980 - Biochemistry


Our lab's research interests are focused on understanding the mechanisms by which aberrant signal transduction pathways contribute to oncogenesis and developing novel anticancer drugs based on interfering with these pathways.  Among the pathways studied are those involving the Ras superfamily (Ras,, Rho and Ral), Kinases (Akt, RhoK and Aurora), STAT3, Bcl/Mcl, FTase/GGTase and the proteasome.

  • Cheng C, Liu Y, Balasis ME, Simmons NL, Li J, Song H, Pan L, Qin Y, Nicolaou KC, Sebti SM, Li R. Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-xL Binding to Bim. Mar Drugs. 2014 Mar;12(3):1335-1348. Pubmedid: 24608970.
  • Kazi A, Ozcan S, Tecleab A, Sun Y, Lawrence HR, Sebti SM. Discovery of PI-1840, a novel non-covalent and rapidly reversible proteasome inhibitor with anti-tumor activity. J Biol Chem. 2014 Feb. Pubmedid: 24570003.
  • Patel RA, Liu Y, Wang B, Li R, Sebti SM. Identification of novel ROCK inhibitors with anti-migratory and anti-invasive activities. Oncogene. 2014 Jan;33(5):550-555. Pubmedid: 23396364. Pmcid: PMC3977753.
  • Trevino JG, Verma M, Singh S, Pillai S, Zhang D, Pernazza D, Sebti SM, Lawrence NJ, Centeno BA, Chellappan SP. Selective disruption of rb-raf-1 kinase interaction inhibits pancreatic adenocarcinoma growth irrespective of gemcitabine sensitivity. Mol Cancer Ther. 2013 Dec;12(12):2722-2734. Pubmedid: 24107447.
  • Sampath D, Malik A, Plunkett W, Nowak B, Williams B, Burton M, Verstovsek S, Faderl S, Garcia-Manero G, List AF, Sebti S, Kantarjian HM, Ravandi F, Lancet JE. Phase I clinical, pharmacokinetic, and pharmacodynamic study of the Akt-inhibitor triciribine phosphate monohydrate in patients with advanced hematologic malignancies. Leuk Res. 2013 Nov;37(11):1461-1467. Pubmedid: 23993427.
  • Blaskovich MA, Yendluri V, Lawrence HR, Lawrence NJ, Sebti SM, Springett GM. Lysophosphatidic Acid Acyltransferase Beta Regulates mTOR Signaling. PLoS One. 2013 Oct;8(10):e78632. Pubmedid: 24205284.
  • Almhanna K, Cubitt CL, Zhang S, Kazim S, Husain K, Sullivan D, Sebti S, Malafa M. MK-2206, an Akt inhibitor, enhances carboplatinum/paclitaxel efficacy in gastric cancer cell lines. Cancer Biol Ther. 2013 Oct;14(10):932-936. Pubmedid: 23917345.
  • Hodul PJ, Dong Y, Husain K, Pimiento JM, Chen J, Zhang A, Francois R, Pledger WJ, Coppola D, Sebti SM, Chen DT, Malafa MP. Vitamin E ?-tocotrienol induces p27(Kip1)-dependent cell-cycle arrest in pancreatic cancer cells via an E2F-1-dependent mechanism. PLoS One. 2013 Aug;8(2):e52526. Pubmedid: 23393547. Pmcid: PMC3564846.
  • Schonbrunn E, Betzi S, Alam R, Martin MP, Becker A, Han H, Francis R, Chakrasali R, Jakkaraj S, Kazi A, Sebti SM, Cubitt CL, Gebhard AW, Hazlehurst LA, Tash JS, Georg GI. Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases. J Med Chem. 2013 Jul;56(10):3768-3782. Pubmedid: 23600925. Pmcid: PMC3714109.
  • Berndt N, Patel R, Yang H, Balasis ME, Sebti SM. Akt2 and acid ceramidase cooperate to induce cell invasion and resistance to apoptosis. Cell Cycle. 2013 Jul;12(13):2024-2032. Pubmedid: 23777806. Pmcid: PMC3737305.
  • Gajewski TF, Salama AK, Niedzwiecki D, Johnson J, Linette G, Bucher C, Blaskovich MA, Sebti SM, Haluska F. Phase II study of the farnesyltransferase inhibitor R115777 in advanced melanoma (CALGB 500104). J Transl Med. 2013 Jun;10:246. Pubmedid: 23228035. Pmcid: PMC3543225.
  • Urlam MK, Pireddu R, Ge Y, Zhang X, Sun Y, Lawrence HR, Guida WC, Sebti SM, Lawrence NJ. Development of new N-Arylbenzamides as STAT3 Dimerization Inhibitors. Medchemcomm. 2013 Jun;4(6):932-941. Pubmedid: 24073326.
  • Ozcan S, Kazi A, Marsilio F, Fang B, Guida WC, Koomen J, Lawrence HR, Sebti SM. Oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors. J Med Chem. 2013 May;56(10):3783-3805. Pubmedid: 23547706. Pmcid: PMC3774303.
  • Ucar DA, Magis AT, He DH, Lawrence NJ, Sebti SM, Kurenova E, Zajac-Kaye M, Zhang J, Hochwald SN. Inhibiting the Interaction of cMET and IGF-1R with FAK Effectively Reduces Growth of Pancreatic Cancer Cells in vitro and in vivo. Anticancer Agents Med Chem. 2013 May;13(4):595-602. Pubmedid: 23272972.
  • Zhang X, Sun Y, Pireddu R, Yang H, Urlam MK, Lawrence HR, Guida WC, Lawrence NJ, Sebti SM. A novel inhibitor of STAT3 homodimerization selectively suppresses STAT3 activity and malignant transformation. Cancer Res. 2013 Mar;73(6):1922-1933. Pubmedid: 23322008.
  • Tecleab A, Sebti SM. Depletion of K-Ras promotes proteasome degradation of survivin. Cell Cycle. 2013 Feb;12(3):522-532. Pubmedid: 23324341. Pmcid: PMC3587453.
  • Aitenneite H, El Bouari A, Sebti S, Saadi M, El Ammari L, Adil K. Poly[(?(3)-hydrogenphosphato)(4H-1,2,4-triazole-?N(1))zinc]. Acta Crystallogr Sect E Struct Rep Online. 2012 Nov;68(Pt 11):m1426-m1427. Pubmedid: 23284388. Pmcid: PMC3515161.
  • Patel RA, Forinash KD, Pireddu R, Sun Y, Sun N, Martin MP, Schönbrunn E, Lawrence NJ, Sebti SM. RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer. Cancer Res. 2012 Oct;72(19):5025-5034. Pubmedid: 22846914. Pmcid: PMC3463757.
  • Ucar DA, Kurenova E, Garrett TJ, Cance WG, Nyberg C, Cox A, Massoll N, Ostrov DA, Lawrence N, Sebti SM, Zajac-Kaye M, Hochwald SN. Disruption of the protein interaction between FAK and IGF-1R inhibits melanoma tumor growth. Cell Cycle. 2012 Sep;11(17):3250-3259. Pubmedid: 22894899. Pmcid: PMC3466524.
  • Kim YB, Balasis ME, Doi K, Berndt N, DuBoulay C, Hu CC, Guida W, Wang HG, Sebti SM, Del Valle JR. Synthesis and evaluation of substituted hexahydronaphthalenes as novel inhibitors of the Mcl-1/BimBH3 interaction. Bioorg Med Chem Lett. 2012 Sep;22(18):5961-5965. Pubmedid: 22901384. Pmcid: PMC3432503.
  • Cheng F, Wang H, Horna P, Wang Z, Shah B, Sahakian E, Woan KV, Villagra A, Pinilla-Ibarz J, Sebti S, Smith M, Tao J, Sotomayor EM. Stat3 inhibition augments the immunogenicity of B-cell lymphoma cells, leading to effective antitumor immunity. Cancer Res. 2012 Sep;72(17):4440-4448. Pubmedid: 22728650. Pmcid: PMC3990429.
  • Lawrence HR, Martin MP, Luo Y, Pireddu R, Yang H, Gevariya H, Ozcan S, Zhu JY, Kendig R, Rodriguez M, Elias R, Cheng JQ, Sebti SM, Schonbrunn E, Lawrence NJ. Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors. J Med Chem. 2012 Sep;55(17):7392-7416. Pubmedid: 22803810.
  • Caceres G, Robey RW, Sokol L, McGraw KL, Clark J, Lawrence NJ, Sebti SM, Wiese M, List AF. HG-829 Is a Potent Noncompetitive Inhibitor of the ATP-Binding Cassette Multidrug Resistance Transporter ABCB1. Cancer Res. 2012 Aug;72(16):4204-4213. Pubmedid: 22761337.
  • Ginestier C, Monville F, Wicinski J, Cabaud O, Cervera N, Josselin E, Finetti P, Guille A, Larderet G, Viens P, Sebti S, Bertucci F, Birnbaum D, Charafe-Jauffret E. Mevalonate metabolism regulates Basal breast cancer stem cells and is a potential therapeutic target. Stem Cells. 2012 Jul;30(7):1327-1337. Pubmedid: 22605458.
  • Win-Piazza H, Schneeberger VE, Chen L, Pernazza D, Lawrence HR, Sebti SM, Lawrence NJ, Wu J. Enhanced anti-melanoma efficacy of interferon alfa-2b via inhibition of Shp2. Cancer Lett. 2012 Jul;320(1):81-85. Pubmedid: 22306001. Pmcid: PMC3319810.
  • Pireddu R, Forinash KD, Sun NN, Martin MP, Sung SS, Alexander B, Zhu JY, Guida WC, Schönbrunn E, Sebti SM, Lawrence NJ. Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2). Medchemcomm. 2012 Jun;3(6):699-709. Pubmedid: 23275831.
  • Bai F, Villagra AV, Zou J, Painter JS, Connolly K, Blaskovich MA, Sokol L, Sebti S, Djeu JY, Loughran TP, Wei S, Sotomayor E, Epling-Burnette P. Tipifarnib-mediated suppression of T-bet-dependent signaling pathways. Cancer Immunol Immunother. 2012 Apr;61(4):523-533. Pubmedid: 21983879.
  • Martin MP, Zhu JY, Lawrence HR, Pireddu R, Luo Y, Alam R, Ozcan S, Sebti SM, Lawrence NJ, Schönbrunn E. A novel mechanism by which small molecule inhibitors induce the DFG flip in Aurora A. ACS Chem Biol. 2012 Apr;7(4):698-706. Pubmedid: 22248356.
  • Doi K, Li R, Sung SS, Wu H, Liu Y, Manieri W, Krishnegowda G, Awwad A, Dewey A, Liu X, Amin S, Cheng C, Qin Y, Schonbrunn E, Daughdrill G, Loughran TP, Sebti S, Wang HG. Discovery of marinopyrrole A (maritoclax) as a selective Mcl-1 antagonist that overcomes ABT-737 resistance by binding to and targeting Mcl-1 for proteasomal degradation. J Biol Chem. 2012 Mar;287(13):10224-10235. Pubmedid: 22311987. Pmcid: PMC3323047.
  • Ge Y, Kazi A, Marsilio F, Luo Y, Jain S, Brooks W, Daniel KG, Guida WC, Sebti SM, Lawrence HR. Discovery and synthesis of hydronaphthoquinones as novel proteasome inhibitors. J Med Chem. 2012 Mar;55(5):1978-1998. Pubmedid: 22220566. Pmcid: PMC3530929.
  • Kumar N, Crocker T, Smith T, Pow-Sang J, Spiess PE, Egan K, Quinn G, Schell M, Sebti S, Kazi A, Chuang T, Salup R, Helal M, Zagaja G, Trabulsi E, McLarty J, Fazili T, Williams CR, Schreiber F, Slaton J, Anderson JK. Challenges and potential solutions to meeting accrual goals in a Phase II chemoprevention trial for prostate cancer. Contemp Clin Trials. 2012 Mar;33(2):279-285. Pubmedid: 22101219. Pmcid: PMC3268882.
  • Li R, Martin MP, Liu Y, Wang B, Patel RA, Zhu JY, Sun N, Pireddu R, Lawrence NJ, Li J, Haura EB, Sung SS, Guida WC, Schonbrunn E, Sebti SM. Fragment-based and structure-guided discovery and optimization of rho kinase inhibitors. J Med Chem. 2012 Mar;55(5):2474-2478. Pubmedid: 22272748.
  • Davis R, Pillai S, Lawrence N, Sebti S, Chellappan SP. TNF-?-mediated proliferation of vascular smooth muscle cells involves Raf-1-mediated inactivation of Rb and transcription of E2F1-regulated genes. Cell Cycle. 2012 Jan;11(1):109-118. Pubmedid: 22185776. Pmcid: PMC3272234.
  • Kumar N, Crocker T, Smith T, Connors S, Pow-Sang J, Spiess PE, Egan K, Quinn G, Schell M, Sebti S, Kazi A, Chuang T, Salup R, Helal M, Zagaja G, Trabulsi E, McLarty J, Fazili T, Williams CR, Schreiber F, Anderson K. Prostate Cancer Chemoprevention Targeting Men with High-Grade Prostatic Intraepithelial Neoplasia (HGPIN) and Atypical Small Acinar Proliferation (ASAP): Model for Trial Design and Outcome Measures. J Clin Trials. 2012 Jan;2(1). Pubmedid: 24533253. Pmcid: PMC3924733.
  • Johnson JL, Pillai S, Pernazza D, Sebti SM, Lawrence NJ, Chellappan SP. Regulation of matrix metalloproteinase genes by E2F transcription factors: Rb-Raf-1 interaction as a novel target for metastatic disease. Cancer Res. 2012 Jan;72(2):516-526. Pubmedid: 22086850. Pmcid: PMC3261351.
  • Garrett CR, Coppola D, Wenham RM, Cubitt CL, Neuger AM, Frost TJ, Lush RM, Sullivan DM, Cheng JQ, Sebti SM. Phase I pharmacokinetic and pharmacodynamic study of triciribine phosphate monohydrate, a small-molecule inhibitor of AKT phosphorylation, in adult subjects with solid tumors containing activated AKT. Invest New Drugs. 2011 Dec;29(6):1381-1389. Pubmedid: 20644979.
  • Husain K, Francois RA, Yamauchi T, Perez M, Sebti SM, Malafa MP. Vitamin E ?-tocotrienol augments the antitumor activity of gemcitabine and suppresses constitutive NF-?B activation in pancreatic cancer. Mol Cancer Ther. 2011 Dec;10(12):2363-2372. Pubmedid: 21971120. Pmcid: PMC3237822.
  • Berndt N, Sebti SM. Measurement of protein farnesylation and geranylgeranylation in vitro, in cultured cells and in biopsies, and the effects of prenyl transferase inhibitors. Nat Protoc. 2011 Nov;6(11):1775-1791. Pubmedid: 22036881.
  • Berndt N, Hamilton AD, Sebti SM. Targeting protein prenylation for cancer therapy. Nat Rev Cancer. 2011 Nov;11(11):775-791. Pubmedid: 22020205.
  • Marchion DC, Cottrill HM, Xiong Y, Chen N, Bicaku E, Fulp WJ, Bansal N, Chon HS, Stickles XB, Kamath SG, Hakam A, Li L, Su D, Moreno C, Judson PL, Berchuck A, Wenham RM, Apte SM, Gonzalez-Bosquet J, Bloom GC, Eschrich SA, Sebti S, Chen DT, Lancaster JM. BAD phosphorylation determines ovarian cancer chemosensitivity and patient survival. Clin Cancer Res. 2011 Oct;17(19):6356-6366. Pubmedid: 21849418. Pmcid: PMC3186862.
  • O'Neil BH, Goff LW, Kauh JS, Strosberg JR, Bekaii-Saab TS, Lee RM, Kazi A, Moore DT, Learoyd M, Lush RM, Sebti SM, Sullivan DM. Phase II study of the mitogen-activated protein kinase 1/2 inhibitor selumetinib in patients with advanced hepatocellular carcinoma. J Clin Oncol. 2011 Aug;29(17):2350-2356. Pubmedid: 21519015. Pmcid: PMC3107750.
  • Balasis ME, Forinash KD, Chen YA, Fulp WJ, Coppola D, Hamilton AD, Cheng JQ, Sebti SM. Combination of farnesyltransferase and Akt inhibitors is synergistic in breast cancer cells and causes significant breast tumor regression in ErbB2 transgenic mice. Clin Cancer Res. 2011 May;17(9):2852-2862. Pubmedid: 21536547. Pmcid: PMC3156694.
  • Hu Y, Li X, Sebti SM, Chen J, Cai J. Design and synthesis of AApeptides: A new class of peptide mimics. Bioorg Med Chem Lett. 2011 Mar;21(5):1469-1471. Pubmedid: 21292484.
  • Lancet JE, Duong VH, Winton EF, Stuart RK, Burton M, Zhang S, Cubitt C, Blaskovich MA, Wright JJ, Sebti S, Sullivan DM. A phase I clinical-pharmacodynamic study of the farnesyltransferase inhibitor tipifarnib in combination with the proteasome inhibitor bortezomib in advanced acute leukemias. Clin Cancer Res. 2011 Mar;17(5):1140-1146. Pubmedid: 21233404. Pmcid: PMC3049960.
  • Kazi A, Sun J, Doi K, Sung SS, Takahashi Y, Yin H, Rodriguez JM, Becerril J, Berndt N, Hamilton AD, Wang HG, Sebti SM. The BH3 alpha-helical mimic BH3-M6 disrupts Bcl-X(L), Bcl-2, and MCL-1 protein-protein interactions with Bax, Bak, Bad, or Bim and induces apoptosis in a Bax- and Bim-dependent manner. J Biol Chem. 2011 Mar;286(11):9382-9392. Pubmedid: 21148306. Pmcid: PMC3059047.
  • Mahajan K, Coppola D, Challa S, Fang B, Chen YA, Zhu W, Lopez AS, Koomen J, Engelman RW, Rivera C, Muraoka-Cook RS, Cheng JQ, Schönbrunn E, Sebti SM, Earp HS, Mahajan NP. Ack1 mediated AKT/PKB tyrosine 176 phosphorylation regulates its activation. PLoS One. 2011 Jan;5(3):e9646. Pubmedid: 20333297. Pmcid: PMC2841635.
  • Scott LM, Chen L, Daniel KG, Brooks WH, Guida WC, Lawrence HR, Sebti SM, Lawrence NJ, Wu J. Shp2 protein tyrosine phosphatase inhibitor activity of estramustine phosphate and its triterpenoid analogs. Bioorg Med Chem Lett. 2011 Jan;21(2):730-733. Pubmedid: 21193311. Pmcid: PMC3034307.
  • Singh S, Davis R, Alamanda V, Pireddu R, Pernazza D, Sebti S, Lawrence N, Chellappan S. Rb-Raf-1 interaction disruptor RRD-251 induces apoptosis in metastatic melanoma cells and synergizes with dacarbazine. Mol Cancer Ther. 2010 Dec;9(12):3330-3341. Pubmedid: 21139044. Pmcid: PMC3058238.
  • Berndt N, Yang H, Trinczek B, Betzi S, Zhang Z, Wu B, Lawrence NJ, Pellecchia M, Schönbrunn E, Cheng JQ, Sebti SM. The Akt activation inhibitor TCN-P inhibits Akt phosphorylation by binding to the PH domain of Akt and blocking its recruitment to the plasma membrane. Cell Death Differ. 2010 Nov;17(11):1795-1804. Pubmedid: 20489726. Pmcid: PMC2952662.
  • Fletcher S, Keaney EP, Cummings CG, Blaskovich MA, Hast MA, Glenn MP, Chang SY, Bucher CJ, Floyd RJ, Katt WP, Gelb MH, Van Voorhis WC, Beese LS, Sebti SM, Hamilton AD. Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents. J Med Chem. 2010 Oct;53(19):6867-6888. Pubmedid: 20822181. Pmcid: PMC3045627.
  • Chen L, Pernazza D, Scott LM, Lawrence HR, Ren Y, Luo Y, Wu X, Sung SS, Guida WC, Sebti SM, Lawrence NJ, Wu J. Inhibition of cellular Shp2 activity by a methyl ester analog of SPI-112. Biochem Pharmacol. 2010 Sep;80(6):801-810. Pubmedid: 20510203. Pmcid: PMC2906681.
  • Lawrence HR, Kazi A, Luo Y, Kendig R, Ge Y, Jain S, Daniel K, Santiago D, Guida WC, Sebti SM. Synthesis and biological evaluation of naphthoquinone analogs as a novel class of proteasome inhibitors. Bioorgan Med Chem. 2010 Aug;18(15):5576-5592. Pubmedid: 20621484. Pmcid: PMC3530924.
  • Scott LM, Lawrence HR, Sebti SM, Lawrence NJ, Wu J. Targeting protein tyrosine phosphatases for anticancer drug discovery. Curr Pharm Des. 2010 Jun;16(16):1843-1862. Pubmedid: 20337577. Pmcid: PMC3076191.
  • Hidalgo-Carrillo J, Sebti J, Aramendía MA, Marinas A, Marinas JM, Sebti S, Urbano FJ. A study on the potential application of natural phosphate in photocatalytic processes. J Colloid Interface Sci. 2010 Apr;344(2):475-481. Pubmedid: 20129616.
  • Kim D, Sun M, He L, Zhou QH, Chen J, Sun XM, Bepler G, Sebti SM, Cheng JQ. A small molecule inhibits Akt through direct binding to Akt and preventing Akt membrane translocation. J Biol Chem. 2010 Apr;285(11):8383-8394. Pubmedid: 20068047. Pmcid: PMC2832988.
  • Phan J, Li Z, Kasprzak A, Li B, Sebti S, Guida W, Schönbrunn E, Chen J. Structure-based design of high affinity peptides inhibiting the interaction of p53 with MDM2 and MDMX. J Biol Chem. 2010 Jan;285(3):2174-2183. Pubmedid: 19910468. Pmcid: PMC2804373.
  • Hong DS, Sebti SM, Newman RA, Blaskovich MA, Ye L, Gagel RF, Moulder S, Wheler JJ, Naing A, Tannir NM, Ng CS, Sherman SI, El Naggar AK, Khan R, Trent J, Wright JJ, Kurzrock R. Phase I trial of a combination of the multikinase inhibitor sorafenib and the farnesyltransferase inhibitor tipifarnib in advanced malignancies. Clin Cancer Res. 2009 Nov;15(22):7061-7068. Pubmedid: 19903778. Pmcid: PMC2784003.
  • Lawrence HR, Li Z, Yip ML, Sung SS, Lawrence NJ, McLaughlin ML, McManus GJ, Zaworotko MJ, Sebti SM, Chen J, Guida WC. Identification of a disruptor of the MDM2-p53 protein-protein interaction facilitated by high-throughput in silico docking. Bioorg Med Chem Lett. 2009 Oct;19(14):3756-3759. Pubmedid: 19457663. Pmcid: PMC2754843.
  • Kazi A, Lawrence H, Guida WC, McLaughlin ML, Springett GM, Berndt N, Yip RM, Sebti SM. Discovery of a novel proteasome inhibitor selective for cancer cells over non-transformed cells. Cell Cycle. 2009 Aug;8(12):1940-1951. Pubmedid: 19471122. Pmcid: PMC2892826.
  • Sparano JA, Moulder S, Kazi A, Coppola D, Negassa A, Vahdat L, Li T, Pellegrino C, Fineberg S, Munster P, Malafa M, Lee D, Hoschander S, Hopkins U, Hershman D, Wright JJ, Kleer C, Merajver S, Sebti SM. Phase II trial of tipifarnib plus neoadjuvant doxorubicin-cyclophosphamide in patients with clinical stage IIB-IIIC breast cancer. Clin Cancer Res. 2009 Apr;15(8):2942-2948. Pubmedid: 19351752. Pmcid: PMC2785076.
  • Wei J, Kitada S, Rega MF, Emdadi A, Yuan H, Cellitti J, Stebbins JL, Zhai D, Sun J, Yang L, Dahl R, Zhang Z, Wu B, Wang S, Reed TA, Wang HG, Lawrence N, Sebti S, Reed JC, Pellecchia M. Apogossypol derivatives as antagonists of antiapoptotic Bcl-2 family proteins. Mol Cancer Ther. 2009 Apr;8(4):904-913. Pubmedid: 19372563. Pmcid: PMC2750823.
  • Kazi A, Carie A, Blaskovich MA, Bucher C, Thai V, Moulder S, Peng H, Carrico D, Pusateri E, Pledger WJ, Berndt N, Hamilton A, Sebti SM. Blockade of protein geranylgeranylation inhibits Cdk2-dependent p27Kip1 phosphorylation on Thr187 and accumulates p27Kip1 in the nucleus: implications for breast cancer therapy. Mol Cell Biol. 2009 Apr;29(8):2254-2263. Pubmedid: 19204084. Pmcid: PMC2663293.
  • Hast MA, Fletcher S, Cummings CG, Pusateri EE, Blaskovich MA, Rivas K, Gelb MH, Van Voorhis WC, Sebti SM, Hamilton AD, Beese LS. Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase. Chem Biol. 2009 Feb;16(2):181-192. Pubmedid: 19246009. Pmcid: PMC2671474.
  • Kayser-Bricker KJ, Glenn MP, Lee SH, Sebti SM, Cheng JQ, Hamilton AD. Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents. Bioorg Med Chem. 2009 Feb;17(4):1764-1771. Pubmedid: 19179081.
  • Husain K, Francois RA, Hutchinson SZ, Neuger AM, Lush R, Coppola D, Sebti S, Malafa MP. Vitamin E delta-tocotrienol levels in tumor and pancreatic tissue of mice after oral administration. Pharmacology. 2009;83(3):157-163. Pubmedid: 19142032. Pmcid: PMC2834260.
  • Epling-Burnette PK, Sokol L, Chen X, Bai F, Zhou J, Blaskovich MA, Zou J, Painter JS, Edwards TD, Moscinski L, Yoder JA, Djeu JY, Sebti S, Loughran TP, Wei S. Clinical improvement by farnesyltransferase inhibition in NK large granular lymphocyte leukemia associated with imbalanced NK receptor signaling. Blood. 2008 Dec;112(12):4694-4698. Pubmedid: 18791165. Pmcid: PMC2597136.
  • Gunning PT, Glenn MP, Siddiquee KA, Katt WP, Masson E, Sebti SM, Turkson J, Hamilton AD. Targeting protein-protein interactions: suppression of Stat3 dimerization with rationally designed small-molecule, nonpeptidic SH2 domain binders. Chembiochem. 2008 Nov;9(17):2800-2803. Pubmedid: 19006150. Pmcid: PMC2728599.
  • Fletcher S, Cummings CG, Rivas K, Katt WP, Hornéy C, Buckner FS, Chakrabarti D, Sebti SM, Gelb MH, Van Voorhis WC, Hamilton AD. Potent, Plasmodium-selective farnesyltransferase inhibitors that arrest the growth of malaria parasites: structure-activity relationships of ethylenediamine-analogue scaffolds and homology model validation. J Med Chem. 2008 Oct;51(17):5176-5197. Pubmedid: 18686940. Pmcid: PMC3049929.
  • Lawrence HR, Pireddu R, Chen L, Luo Y, Sung SS, Szymanski AM, Yip ML, Guida WC, Sebti SM, Wu J, Lawrence NJ. Inhibitors of Src homology-2 domain containing protein tyrosine phosphatase-2 (Shp2) based on oxindole scaffolds. J Med Chem. 2008 Aug;51(16):4948-4956. Pubmedid: 18680359. Pmcid: PMC2744494.
  • Gustafsdottir SM, Wennstrom S, Fredriksson S, Schallmeiner E, Hamilton AD, Sebti SM, Landegren U. Use of proximity ligation to screen for inhibitors of interactions between vascular endothelial growth factor A and its receptors. Clin Chem. 2008 Jul;54(7):1218-1225. Pubmedid: 18499900.
  • Kinkade R, Dasgupta P, Carie A, Pernazza D, Carless M, Pillai S, Lawrence N, Sebti SM, Chellappan S. A small molecule disruptor of Rb/Raf-1 interaction inhibits cell proliferation, angiogenesis, and growth of human tumor xenografts in nude mice. Cancer Res. 2008 May;68(10):3810-3818. Pubmedid: 18483265. Pmcid: PMC3233839.
  • Elahi A, Zhang L, Yeatman T, Gery S, Sebti S, Shibata D. HPP1-mediated tumor suppression requires activation of STAT1 pathways. Int J Cancer. 2008 Apr;122(7):1567-1572. Pubmedid: 18059030.
  • Falsetti SC, Wang DA, Peng H, Carrico D, Cox AD, Der CJ, Hamilton AD, Sebti SM. Geranylgeranyltransferase I inhibitors target RalB to inhibit anchorage-dependent growth and induce apoptosis and RalA to inhibit anchorage-independent growth. Mol Cell Biol. 2008 Mar;27(22):8003-8014. Pubmedid: 17875936. Pmcid: PMC2169159.
  • Machida S, Usuba K, Blaskovich MA, Yano A, Harada K, Sebti SM, Kato N, Ohkanda J. Module assembly for protein-surface recognition: geranylgeranyltransferase I bivalent inhibitors for simultaneous targeting of interior and exterior protein surfaces. Chemistry. 2008 Feb;14(5):1392-1401. Pubmedid: 18200641.
  • Kurzrock R, Kantarjian H, Blaskovich M, Bucher C, Verstovsek S, Wright J, Pilat S, Cortes J, Estey E, Giles F, Beran M, Sebti S. Phase I study of alternate-week administration of tipifarnib in patients withmyelodysplastic syndrome. Clin Cancer Res. 2008 Jan;14(2):509-514. Pubmedid: 18223226.
  • Siddiquee K, Gunning P, Glenn M, Katt W, Zhang S, Schroeck C, Sebti S, Jove R, Hamilton A, Turkson J. An oxazole-based small-molecule Stat3 inhibitor modulates Stat3 stability and processing and induces antitumor cell effects. Acs Chem Biol. 2007 Dec;2(12):787-798. Pubmedid: 18154266.
  • Sagatys E, Garrett CR, Boulware D, Kelley S, Malafa M, Cheng JQ, Sebti S, Coppola D. Activation of the serine/threonine protein kinase Akt during the progression of Barrett neoplasia. Hum Pathol. 2007 Oct;38(10):1526-1531. Pubmedid: 17640711.
  • Saglam O, Garrett CR, Boulware D, Sayegh Z, Shibata D, Malafa M, Yeatman T, Cheng JQ, Sebti S, Coppola D. Activation of the serine/threonine protein kinase AKT during the progression of colorectal neoplasia. Clin Colorectal Cancer. 2007 Sep;6(9):652-656. Pubmedid: 17945038.
  • Epifano F, Curini M, Genovese S, Blaskovich M, Hamilton A, Sebti SM. Prenyloxyphenylpropanoids as novel lead compounds for the selective inhibition of geranylgeranyl transferase I. Bioorg Med Chem Lett. 2007 May;17(9):2639-2642. Pubmedid: 17314046.
  • Siddiquee K, Zhang S, Guida WC, Blaskovich MA, Greedy B, Lawrence HR, Yip ML, Jove R, McLaughlin MM, Lawrence NJ, Sebti SM, Turkson J. Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity. Proc Natl Acad Sci U S A. 2007 May;104(18):7391-7396. Pubmedid: 17463090. Pmcid: PMC1863497.
  • Carie AE, Sebti SM. A chemical biology approach identifies a beta-2 adrenergic receptor agonist that causes human tumor regression by blocking the Raf-1/Mek-1/Erk1/2 pathway. Oncogene. 2007 May;26(26):3777-3788. Pubmedid: 17260025.
  • Kayser KJ, Glenn MP, Sebti SM, Cheng JQ, Hamilton AD. Modifications of the GSK3beta substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics. Bioorg Med Chem Lett. 2007 Apr;17(7):2068-2073. Pubmedid: 17276059.
  • Gunning P, Katt W, Glenn M, Siddique K, Kim J, Jove R, Sebti S, Turkson J, Hamilton A. Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: Structural recognition of STAT SH2 domains. Bioorg Med Chem Lett. 2007 Apr;17(7):1875-1878. Pubmedid: 17336521.
  • Delarue F, Adnane J, Joshi B, Blaskovich M, Wang D, Hawker J, BizouarnF, Ohkanda J, Zhu K, Hamilton A, Chellappan S, Sebti S. Farnesyltransferase and geranylgeranyltransferase I inhibitors upregulate RhoB expression by HDAC1 dissociation, HAT association and histone acetylation of the RhoB promoter. Oncogene. 2007 Feb;26(5):633-640. Pubmedid: 16909123.
  • Hu B, Gilkes DM, Farooqi B, Sebti SM, Chen J. MDMX overexpression prevents p53 activation by the MDM2 inhibitor Nutlin. J Biol Chem. 2006 Nov;281(44):33030-33035. Pubmedid: 16905541.
  • Glenn MP, Chang SY, Hornéy C, Rivas K, Yokoyama K, Pusateri EE, Fletcher S, Cummings CG, Buckner FS, Pendyala PR, Chakrabarti D, Sebti SM, Gelb M, Van Voorhis WC, Hamilton AD. Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites. J Med Chem. 2006 Sep;49(19):5710-5727. Pubmedid: 16970397. Pmcid: PMC2728208.
  • Tang D, Park H, Georgescu S, Sebti S, Hamilton A, Galper J. Simvastatin potentiates tumor necrosis factor alpha-mediated apoptosis of human vascular endothelial cells via the inhibition of the geranylgeranylation of RhoA. Life Sci. 2006 Sep;79(15):1484-1492. Pubmedid: 16740276.
  • Chen L, Sung SS, Yip ML, Lawrence HR, Ren Y, Guida WC, Sebti SM, Lawrence NJ, Wu J. Discovery of a novel shp2 protein tyrosine phosphatase inhibitor. Mol Pharmacol. 2006 Aug;70(2):562-570. Pubmedid: 16717135.
  • Sparano J, Moulder S, Kazi A, Vahdat L, Li T, Pellegrino C, Munster P, Malafa M, Lee D, Hoschander S, Hopkins U, Hershman D, Wright J, Sebti S. Targeted inhibition of farnesyltransferase in locally advanced breast cancer: a phase I and II trial of tipifarnib plus dose-dense doxorubicin and cyclophosphamide. J Clin Oncol. 2006 Jul;24(19):3013-3018. Pubmedid: 16769985.
  • Zhou H, Wang DA, Baldini L, Ennis E, Jain R, Carie A, Sebti SM, Hamilton AD. Structure-activity studies on a library of potent calix[4]arene-based PDGF antagonists that inhibit PDGF-stimulated PDGFR tyrosine phosphorylation. Org Biomol Chem. 2006 Jun;4(12):2376-2386. Pubmedid: 16763682.
  • Peng H, Carrico D, Thai V, Blaskovich M, Bucher C, Pusateri E, Sebti S, Hamilton A. Synthesis and evaluation of potent, highly-selective, 3-aryl-piperazinone inhibitors of protein geranylgeranyltransferase-I. Org Biomol Chem. 2006 May;4(9):1768-1784. Pubmedid: 16633570.
  • Ohkanda J, Strickland CL, Blaskovich MA, Carrico D, Lockman JW, Vogt A, Bucher CJ, Sun J, Qian Y, Knowles D, Pusateri EE, Sebti SM, Hamilton AD. Structure-based design of imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase. Org Biomol Chem. 2006 Feb;4(3):482-492. Pubmedid: 16446806.
  • Donapaty S, Louis S, Horvath E, Kun J, Sebti SM, Malafa MP. RRR-alpha-tocopherol succinate down-regulates oncogenic Ras signaling. Mol Cancer Ther. 2006 Feb;5(2):309-316. Pubmedid: 16505104.
  • Guida W, Hamilton A, Crotty J, Sebti S. Protein farnesyltransferase: Flexible docking studies on inhibitors using computational modeling. J Comput Aided Mol Des. 2005 Dec;19(12):871-85. Pubmedid: 16607571.
  • Takahashi Y, Karbowski M, Yamaguchi H, Kazi A, Wu J, Sebti SM, Youle RJ, Wang HG. Loss of Bif-1 suppresses Bax/Bak conformational change and mitochondrial apoptosis. Mol Cell Biol. 2005 Nov;25(21):9369-9382. Pubmedid: 16227588. Pmcid: PMC1265816.
  • Nefedova Y, Cheng P, Gilkes D, Blaskovich M, Beg AA, Sebti SM, Gabrilovich DI. Activation of dendritic cells via inhibition of Jak2/STAT3 signaling. J Immunol. 2005 Oct;175(7):4338-4346. Pubmedid: 16177074. Pmcid: PMC1351251.
  • Nefedova Y, Nagaraj S, Rosenbauer A, Muro-Cacho C, Sebti SM, Gabrilovich DI. Regulation of dendritic cell differentiation and antitumor immune response in cancer by pharmacologic-selective inhibition of the janus-activated kinase 2/signal transducers and activators of transcription 3 pathway. Cancer Res. 2005 Oct;65(20):9525-9535. Pubmedid: 16230418. Pmcid: PMC1351362.
  • Turkson J, Zhang S, Mora LB, Burns A, Sebti S, Jove R. A novel platinum compound inhibits constitutive Stat3 signaling and induces cell cycle arrest and apoptosis of malignant cells. J Biol Chem. 2005 Sep;280(38):32979-32988. Pubmedid: 16046414.
  • Cloughesy T, Kuhn J, Robins H, Abrey L, Wen P, Fink K, Lieberman F, Mehta M, Chang S, Yung A, DeAngelis L, Schiff D, Junck L, Groves M, Paquette S, Wright J, Lamborn K, Sebti S, Prados M. Phase I trial of tipifarnib in patients with recurrent malignant glioma takingenzyme-inducing antiepileptic drugs: a North American Brain Tumor Consortium. J Clin Oncol. 2005 Aug;23(27):6647-6656. Pubmedid: 16170172.
  • Glenn M, Chang S, Hucke O, Verlinde C, Rivas K, Horney C, Yokoyama K, Buckner F, Pendyala P, Chakrabarti D, Gelb M, Van Voorhis W, Sebti S, Hamilton A. Structurally simple farnesyltransferase inhibitors arrest the growth of malaria parasites. Angew Chem Int Ed Engl. 2005 Aug;44(31):4903-4906. Pubmedid: 16007716.
  • Yin H, Lee G, Sedey K, Kutzki O, Park H, Orner B, Ernst J, Wang H, Sebti S, Hamilton A. Terphenyl-Based Bak BH3 alpha-helical proteomimetics as low-molecular-weight antagonists of Bcl-xL. J Am Chem Soc. 2005 Jul;127(29):10191-10196. Pubmedid: 16028929.
  • Sun J, Wang DA, Jain RK, Carie A, Paquette S, Ennis E, Blaskovich MA, Baldini L, Coppola D, Hamilton AD, Sebti SM. Inhibiting angiogenesis and tumorigenesis by a synthetic molecule that blocks binding of both VEGF and PDGF to their receptors. Oncogene. 2005 Jul;24(29):4701-4709. Pubmedid: 15897913.
  • Zhu K, Gerbino E, Beaupre DM, Mackley PA, Muro-Cacho C, Beam C, Hamilton AD, Lichtenheld MG, Kerr WG, Dalton W, Alsina M, Sebti SM. Farnesyltransferase inhibitor R115777 (Zarnestra, Tipifarnib) synergizes with paclitaxel to induce apoptosis and mitotic arrest and to inhibit tumor growth of multiple myeloma cells. Blood. 2005 Jun;105(12):4759-4766. Pubmedid: 15728126. Pmcid: PMC1895008.
  • Chen L, Yin H, Farooqi B, Sebti S, Hamilton AD, Chen J. p53 alpha-Helix mimetics antagonize p53/MDM2 interaction and activate p53. Mol Cancer Ther. 2005 Jun;4(6):1019-1025. Pubmedid: 15956260.
  • Nallan L, Bauer K, Bendale P, Rivas K, Yokoyama K, Horney C, Pendyala P, Floyd D, Lombardo L, Williams D, Hamilton A, Sebti S, Windsor W, Weber P, Buckner F, Chakrabarti D, Gelb M, Van Voorhis W. Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. J Med Chem. 2005 Jun;48(11):3704-3713. Pubmedid: 15916422.
  • Sun J, Blaskovich MA, Jove R, Livingston SK, Coppola D, Sebti SM. Cucurbitacin Q: a selective STAT3 activation inhibitor with potent antitumor activity. Oncogene. 2005 May;24(20):3236-3245. Pubmedid: 15735720.
  • Wang D, Sebti S. Palmitoylated cysteine 192 is required for RhoB tumor-suppressive and apoptotic activities. J Biol Chem. 2005 May;280(19):19243-19249. Pubmedid: 15713677.
  • Sebti S. Protein farnesylation: implications for normal physiology, malignant transformation, and cancer therapy. Cancer Cell. 2005 Apr;7(4):297-300. Pubmedid: 15837619.
  • Yin H, Lee G, Sedey K, Rodriguez J, Wang H, Sebti S, Hamilton A. Terephthalamide derivatives as mimetics of helical peptides: disruption of the Bcl-x(L)/Bak interaction. J Am Chem Soc. 2005 Apr;127(15):5463-5468. Pubmedid: 15826183.
  • Yin H, Lee G, Park H, Payne G, Rodriguez J, Sebti S, Hamilton A. Terphenyl-based helical mimetics that disrupt the p53/HDM2 interaction. Angew Chem Int Ed Engl. 2005 Apr;44(18):2704-2707. Pubmedid: 15765497.
  • Zuckerbraun B, Barbato J, Hamilton A, Sebti S, Tzeng E. Inhibition of geranylgeranyltransferase I decreases generation of vascular reactive oxygen species and increases vascular nitric oxide production. J Surg Res. 2005 Apr;124(2):256-263. Pubmedid: 15820256.
  • Mazieres J, Tillement V, Allal C, Clanet C, Bobin L, Chen Z, Sebti SM, Favre G, Pradines A. Geranylgeranylated, but not farnesylated, RhoB suppresses Ras transformation of NIH-3T3 cells. Exp Cell Res. 2005 Apr;304(2):354-364. Pubmedid: 15748883.
  • Carrico D, Blaskovich M, Bucher C, Sebti S, Hamilton A. Design, synthesis, and evaluation of potent and selective benzoyleneurea-based inhibitors of protein geranylgeranyltransferase-I. Bioorg Med Chem. 2005 Feb;13(3):677-688. Pubmedid: 15653335.
  • Woo JT, Nakagawa H, Krecic AM, Nagai K, Hamilton AD, Sebti SM, Stern PH. Inhibitory effects of mevastatin and a geranylgeranyl transferase I inhibitor (GGTI-2166) on mononuclear osteoclast formation induced by receptor activator of NF kappa B ligand (RANKL) or tumor necrosis factor-alpha (TNF-alpha). Biochem Pharmacol. 2005 Jan;69(1):87-95. Pubmedid: 15588717.
  • Carrico D, Ohkanda J, Kendrick H, Yokoyama K, Blaskovich MA, Bucher CJ, Buckner FS, Van Voorhis WC, Chakrabarti D, Croft SL, Gelb MH, Sebti SM, Hamilton AD. In vitro and in vivo antimalarial activity of peptidomimetic protein farnesyltransferase inhibitors with improved membrane permeability. Bioorg Med Chem. 2004 Dec;12(24):6517-6526. Pubmedid: 15556768.
  • Epling-Burnette PK, Bai F, Wei S, Painter JS, Olashaw N, Hamilton A, Sebti S, Djeu JY, Loughran TP. ERK couples chronic survival of NK cells to constitutively activated Ras in lymphoproliferative disease of granular lymphocytes (LDGL). Oncogene. 2004 Dec;23(57):9220-9229. Pubmedid: 15516985.
  • Dasgupta P, Sun J, Wang S, Fusaro G, Betts V, Padmanabhan J, Sebti SM, Chellappan SP. Disruption of the Rb--Raf-1 interaction inhibits tumor growth and angiogenesis. Mol Cell Biol. 2004 Nov;24(21):9527-9541. Pubmedid: 15485920. Pmcid: PMC522224.
  • Gasparetto M, Gentry T, Sebti S, O'Bryan E, Nimmanapalli R, Blaskovich MA, Bhalla K, Rizzieri D, Haaland P, Dunne J, Smith C. Identification of compounds that enhance the anti-lymphoma activity of rituximab using flow cytometric high-content screening. J Immunol Methods. 2004 Sep;292(1-2):59-71. Pubmedid: 15350512.
  • Yang L, Dan HC, Sun M, Liu Q, Sun XM, Feldman RI, Hamilton AD, Polokoff M, Nicosia SV, Herlyn M, Sebti SM, Cheng JQ. Akt/protein kinase B signaling inhibitor-2, a selective small molecule inhibitor of Akt signaling with antitumor activity in cancer cells overexpressing Akt. Cancer Res. 2004 Jul;64(13):4394-4399. Pubmedid: 15231645.
  • Jiang K, Sun J, Cheng J, Djeu JY, Wei S, Sebti S. Akt mediates Ras downregulation of RhoB, a suppressor of transformation, invasion, and metastasis. Mol Cell Biol. 2004 Jun;24(12):5565-5576. Pubmedid: 15169915. Pmcid: PMC419878.
  • Alsina M, Fonseca R, Wilson EF, Belle AN, Gerbino E, Price-Troska T, Overton RM, Ahmann G, Bruzek LM, Adjei AA, Kaufmann SH, Wright JJ, Sullivan D, Djulbegovic B, Cantor AB, Greipp PR, Dalton WS, Sebti SM. Farnesyltransferase inhibitor tipifarnib is well tolerated, induces stabilization of disease, and inhibits farnesylation and oncogenic/tumor survival pathways in patients with advanced multiple myeloma. Blood. 2004 May;103(9):3271-3277. Pubmedid: 14726402.
  • Sun J, Blaskovich MA, Jain RK, Delarue F, Paris D, Brem S, Wotoczek-Obadia M, Lin Q, Coppola D, Choi K, Mullan M, Hamilton AD, Sebti SM. Blocking angiogenesis and tumorigenesis with GFA-116, a synthetic molecule that inhibits binding of vascular endothelial growth factor to its receptor. Cancer Res. 2004 May;64(10):3586-3592. Pubmedid: 15150116.
  • Turkson J, Kim JS, Zhang S, Yuan J, Huang M, Glenn M, Haura E, Sebti S, Hamilton AD, Jove R. Novel peptidomimetic inhibitors of signal transducer and activator of transcription 3 dimerization and biological activity. Mol Cancer Ther. 2004 Mar;3(3):261-269. Pubmedid: 15026546.
  • Jiang K, Delarue FL, Sebti SM. EGFR, ErbB2 and Ras but not Src suppress RhoB expression while ectopic expression of RhoB antagonizes oncogene-mediated transformation. Oncogene. 2004 Feb;23(5):1136-1145. Pubmedid: 14647415.
  • Ohkanda J, Buckner F, Lockman J, Yokoyama K, Carrico D, Eastman R, deLuca-Fradley K, Davies W, Croft S, Van Voorhis W, Gelb M, Sebti S, HamiltonAD. Design and synthesis of peptidomimetic protein farnesyltransferase inhibitors as anti-Trypanosoma brucei agents. J Med Chem. 2004 Jan;47(2):432-445. Pubmedid: 14711313.
  • Dan HC, Jiang K, Coppola D, Hamilton A, Nicosia SV, Sebti SM, Cheng JQ. Phosphatidylinositol-3-OH kinase/AKT and survivin pathways as critical targets for geranylgeranyltransferase I inhibitor-induced apoptosis. Oncogene. 2004 Jan;23(3):706-715. Pubmedid: 14737105.
  • Paris D, Townsend K, Quadros A, Humphrey J, Sun J, Brem S, Wotoczek-Obadia M, DelleDonne A, Patel N, Obregon DF, Crescentini R, Abdullah L, Coppola D, Rojiani A,, Crawford F, Sebti SM, Mullan M. Inhibition of angiogenesis by Abeta peptides. Angiogenesis. 2004;7(1):75-85. Pubmedid: 15302999.
  • Turkson J, Zhang S, Palmer J, Kay H, Stanko J, Mora L, Sebti S, Yu H, Jove R. Inhibition of constitutive signal transducer and activator of transcription 3 activation by novel platinum complexes with potent antitumor activity. Mol Cancer Ther. 2004;3(12):1533-1542. Pubmedid: 15634646.
  • Sebti S, Adjei A. Farnesyltransferase inhibitors. Semin Oncol. 2004;31(1):28-39. Pubmedid: 14981578.
  • Mazieres J, Antonia T, Daste G, Muro-Cacho C, Berchery D, Tillement V, Pradines A, Sebti S, Favre G. Loss of RhoB expression in human lung cancer progression. Clin Cancer Res. 2004;10(8):2742-2750. Pubmedid: 15102679.
  • Buckner F, Yokoyama K, Lockman J, Aikenhead K, Ohkanda J, Sadilek M, Sebti S, Van Voorhis W, Hamilton A, Gelb MH. A class of sterol 14-demethylase inhibitors as anti-Trypanosoma cruzi agents. Proc Natl Acad Sci U S A. 2003 Dec;100(25):15149-15153. Pubmedid: 14657358. Pmcid: PMC299928.
  • Forsberg M, Blomgran R, Lerm M, Särndahl E, Sebti SM, Hamilton A, Stendahl O, Zheng L. Differential effects of invasion by and phagocytosis of Salmonella typhimurium on apoptosis in human macrophages: potential role of Rho-GTPases and Akt. J Leukoc Biol. 2003 Oct;74(4):620-629. Pubmedid: 12960245.
  • Zhang Z, Wang Y, Lantry L, Kastens E, Liu G, Hamilton A, Sebti S, LubetRA, You M. Farnesyltransferase inhibitors are potent lung cancer chemopreventive agents in A/J mice with a dominant-negative p53 and/or heterozygous deletion of Ink4a/Arf. Oncogene. 2003 Sep;22(40):6257-6265. Pubmedid: 13679864.
  • Bordier BB, Ohkanda J, Liu P, Lee SY, Salazar FH, Marion PL, Ohashi K, Meuse L, Kay MA, Casey JL, Sebti SM, Hamilton AD, Glenn JS. In vivo antiviral efficacy of prenylation inhibitors against hepatitis delta virus. J Clin Invest. 2003 Aug;112(3):407-414. Pubmedid: 12897208. Pmcid: PMC166292.
  • Peng Y, Li C, Chen L, Sebti S, Chen J. Rescue of mutant p53 transcription function by ellipticine. Oncogene. 2003 Jul;22(29):4478-4487. Pubmedid: 12881704.
  • Blaskovich MA, Sun J, Cantor A, Turkson J, Jove R, Sebti SM. Discovery of JSI-124 (cucurbitacin I), a selective Janus kinase/signal transducer and activator of transcription 3 signaling pathway inhibitor with potent antitumor activity against human and murine cancer cells in mice. Cancer Res. 2003 Mar;63(6):1270-1279. Pubmedid: 12649187.
  • Doisneau-Sixou S, Cestac P, Chouini S, Carroll J, Hamilton A, Sebti S, Poirot M, Balaguer P, Faye J, Sutherland R, Favre G. Contrasting effects of prenyltransferase inhibitors on estrogen-dependent cell cycle progression and estrogen receptor-mediated transcriptional activity in MCF-7 cells. Endocrinology. 2003 Mar;144(3):989-998. Pubmedid: 12586776.
  • Bolick SC, Landowski TH, Boulware D, Oshiro MM, Ohkanda J, Hamilton AD, Sebti SM, Dalton WS. The farnesyl transferase inhibitor, FTI-277, inhibits growth and induces apoptosis in drug-resistant myeloma tumor cells. Leukemia. 2003 Feb;17(2):451-457. Pubmedid: 12592346.
  • Mazzocca A, Giusti S, Hamilton AD, Sebti SM, Pantaleo P, Carloni V. Growth inhibition by the farnesyltransferase inhibitor FTI-277 involves Bcl-2 expression and defective association with Raf-1 in liver cancer cell lines. Mol Pharmacol. 2003 Jan;63(1):159-166. Pubmedid: 12488548.
  • Santucci R, Mackley P, Sebti S, Alsina M. Farnesyltransferase inhibitors and their role in the treatment of multiple myeloma. Cancer Control. 2003;10(5):384-387. Pubmedid: 14581893.
  • Ohkanda J, Blaskovich M, Sebti S, Hamilton A. The development of protein farnesyltransferase inhibitors as signaling-based anticancer agents. Prog Cell Cycle Res. 2003;5:211-217. Pubmedid: 14593715.
  • Zhu K, Hamilton A, Sebti S. Farnesyltransferase inhibitors as anticancer agents: current status. Curr Opin Investig Drugs. 2003;4(12):1428-1435. Pubmedid: 14763128.
  • Sebti S. Blocked pathways: FTIs shut down oncogene signals. Oncologist. 2003;8(Suppl):30-38. Pubmedid: 14671226.
  • Sebti S, Der C. Opinion: Searching for the elusive targets of farnesyltransferase inhibitors. Nat Rev Cancer. 2003;3(12):945-951. Pubmedid: 14737124.
  • Sun J, Ohkanda J, Coppola D, Yin H, Kothare M, Busciglio B, Hamilton A, Sebti S. Geranylgeranyltransferase I inhibitor GGTI-2154 induces breast carcinoma apoptosis and tumor regression in H-Ras transgenic mice. Cancer Res. 2003;63(24):8922-8929. Pubmedid: 14695209.
  • Jackson R, Adnane J, Coppola D, Cantor A, Sebti S, Pledger W. Loss of the cell cycle inhibitors p21(Cip1) and p27(Kip1) enhances tumorigenesis in knockout mouse models. Oncogene. 2002 Dec;21(55):8486-8497. Pubmedid: 12466968.
  • Allal C, Pradines A, Hamilton AD, Sebti SM, Favre G. Farnesylated RhoB prevents cell cycle arrest and actin cytoskeleton disruption caused by the geranylgeranyltransferase I inhibitor GGTI-298. Cell Cycle. 2002 Nov-Dec;1(6):430-437. Pubmedid: 12548020.
  • Crespo N, Delarue F, Ohkanda J, Carrico D, Hamilton A, Sebti S. The farnesyltransferase inhibitor, FTI-2153, inhibits bipolar spindle formation during mitosis independently of transformation and Ras and p53 mutation status. Cell Death Differ. 2002 Jul;9(7):702-709. Pubmedid: 12058275.
  • Zahouily M, Rhihil A, Bazoui H, Sebti S, Zakarya D. Structure-toxicity relationships study of a series of organophosphorus insecticides. J Mol Model. 2002 May;8(5):168-172. Pubmedid: 12858851.
  • Li X, Liu L, Tupper J, Bannerman D, Winn R, Sebti S, Hamilton A, Harlan J. Inhibition of protein geranylgeranylation and RhoA/RhoA kinase pathway induces apoptosis in human endothelial cells. J Biol Chem. 2002 May;277(18):15309-15316. Pubmedid: 11839765.
  • Walters CE, Pryce G, Hankey DJ, Sebti SM, Hamilton AD, Baker D, Greenwood J, Adamson P. Inhibition of Rho GTPases with protein prenyltransferase inhibitors prevents leukocyte recruitment to the central nervous system and attenuates clinical signs of disease in an animal model of multiple sclerosis. J Immunol. 2002 Apr;168(8):4087-4094. Pubmedid: 11937568. Pmcid: PMC3836400.
  • Arteaga CL, Khuri F, Krystal G, Sebti S. Overview of rationale and clinical trials with signal transduction inhibitors in lung cancer. Semin Oncol. 2002 Feb;29(1 Suppl 4):15-26. Pubmedid: 11894010.
  • Ohkanda J, Lockman JW, Kothare MA, Qian Y, Blaskovich MA, Sebti SM, Hamilton AD. Design and synthesis of potent nonpeptidic farnesyltransferase inhibitors based on a terphenyl scaffold. J Med Chem. 2002 Jan;45(1):177-188. Pubmedid: 11754590.
  • Bazoui H, Zahouily M, Sebti S, Boulajaaj S, Zakarya D. Structure-cytotoxicity relationships for a series of HEPT derivatives. J Mol Model. 2002 Jan;8(1):1-7. Pubmedid: 12111397.
  • Burdelya L, Catlett-Falcone R, Levitzki A, Cheng F, Mora L, Sotomayor E, Coppola D, Sun J, Sebti S, Dalton W, Jove R, Yu H. Combination therapy with AG-490 and interleukin 12 achieves greater antitumor effects than either agent alone. Mol Cancer Ther. 2002;1(11):893-899. Pubmedid: 12481410.
  • Adnane J, Seijo E, Chen Z, Bizouarn F, Leal M, Sebti S, Munoz-Antonia T. RhoB, not RhoA, represses the transcription of the transforming growth factor beta type II receptor by a mechanism involving activator protein 1. J Biol Chem. 2002;277(10):8500-8507. Pubmedid: 11741970.
  • Ohkanda J, Knowles D, Blaskovich M, Sebti S, Hamilton A. Inhibitors of protein farnesyltransferase as novel anticancer agents. Curr Top Med Chem. 2002;2(3):303-323. Pubmedid: 11944822.
  • Adnane J, Muro-Cacho C, Mathews L, Sebti S, Munoz-Antonia T. Suppression of RhoB expression in invasive carcinoma from head and neck cancer patients. Clin Cancer Res. 2002;8(7):2225-2232. Pubmedid: 12114424.
  • Finder JD, Petrus JL, Hamilton A, Villavicencio RT, Pitt BR, Sebti SM. Signal transduction pathways of IL-1beta-mediated iNOS in pulmonary vascular smooth muscle cells. Am J Physiol Lung Cell Mol Physiol. 2001 Oct;281(4):L816-L823. Pubmedid: 11557585.
  • Crespo N, Ohkanda J, Yen T, Hamilton A, Sebti S. The farnesyltransferase inhibitor, FTI-2153, blocks bipolar spindle formation and chromosome alignment and causes prometaphase accumulation during mitosis of human lung cancer cells. J Biol Chem. 2001 May;276(19):16161-16167. Pubmedid: 11154688.
  • Kucich U, Rosenbloom J, Herrick D, Abrams W, Hamilton A, Sebti S, Rosenbloom J. Signaling events required for transforming growth factor-beta stimulation of connective tissue growth factor expression by cultured human lung fibroblasts. Arch Biochem Biophys. 2001;395(1):103-112. Pubmedid: 11673871.
  • Teng S, Sun J, Irby R, Hamilton A, Sebti S, Yeatman T. V-Src transformation is mediated through farnesylated protein. J Surg Res. 2001;99(2):343-346. Pubmedid: 11469908.
  • Ohkanda J, Lockman J, Yokoyama K, Gelb M, Croft S, Kendrick H, Harrell M, Feagin J, Blaskovich M, Sebti S, Hamilton A. Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity. Bioorg Med Chem Lett. 2001;11(6):761-764. Pubmedid: 11277514.
  • Delarue F, Taylor B, Sebti S. Ras and RhoA suppress whereas RhoB enhances cytokine-induced transcription of nitric oxide synthase-2 in human normal liver AKN-1 cells and lung cancer A-549 cells. Oncogene. 2001;20(45):6531-6537. Pubmedid: 11641777.
  • Turkson J, Ryan D, Kim J, Zhang Y, Chen Z, Haura E, Laudano A, Sebti S, Hamilton A, Jove R. Phosphotyrosyl peptides block Stat3-mediated DNA binding activity, gene regulation, and cell transformation. J Biol Chem. 2001;276(48):45443-45455. Pubmedid: 11579100.
  • Dey A, She H, Kim L, Boruch A, Guris DL, Carlberg K, Sebti SM, Woodley DT, Imamoto A, Li W. Colony-stimulating factor-1 receptor utilizes multiple signaling pathways to induce cyclin D2 expression. Mol Biol Cell. 2000 Nov;11(11):3835-3848. Pubmedid: 11071910. Pmcid: PMC15040.
  • Adnane J, Bizouarn F, Chen Z, Ohkanda J, Hamilton A, Munoz-Antonia T, Sebti S. Inhibition of farnesyltransferase increases TGFbeta type II receptor expression and enhances the responsiveness of human cancer cells to TGFbeta. Oncogene. 2000 Nov;19(48):5525-5533. Pubmedid: 11114730.
  • Wei S, Gilvary D, Corliss B, Sebti S, Sun J, Straus D, Leibson P, Trapain J, Hamilton A, Weber M, Djeu J. Direct tumor lysis by NK cells uses a Ras-independent mitogen-activated protein kinase signal pathway. J Immunol. 2000 Oct;165(7):3811-3819. Pubmedid: 11034387.
  • Kucich U, Rosenberg JC, Shen G, Abrams WR, Hamilton AD, Sebti SM, Rosenbloom J. TGF-beta1 stimulation of fibronectin transcription in cultured human lung fibroblasts requires active geranylgeranyl transferase I, phosphatidylcholine-specific phospholipase C, protein kinase C-delta, and p38, but not erk1/erk2. Arch Biochem Biophys. 2000 Feb;374(2):313-324. Pubmedid: 10666313.
  • Boota A, Johnson B, Lee K, Blaskovich M, Liu S, Kagan V, Hamilton A, Pitt B, Sebti S, Davies P. Prenyltransferase inhibitors block superoxide production by pulmonary vascular smooth muscle. Am J Physiol Lung Cell Mol Physiol. 2000 Feb;278(2):L329-L334. Pubmedid: 10666117.
  • Lantry L, Zhang Z, Yao R, Crist K, Wang Y, Ohkanda J, Hamilton A, Sebti S, Lubet R, You M. Effect of farnesyltransferase inhibitor FTI-276 on established lung adenomas from A/J mice induced by 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone. Carcinogenesis. 2000 Jan;21(1):113-116. Pubmedid: 10607742.
  • Carloni V, Pinzani M, Giusti S, Romanelli RG, Parola M, Bellomo G, Failli P, Hamilton AD, Sebti SM, Laffi G, Gentilini P. Tyrosine phosphorylation of focal adhesion kinase by PDGF is dependent on ras in human hepatic stellate cells. Hepatology. 2000 Jan;31(1):131-140. Pubmedid: 10613738.
  • Jiang K, Coppola D, Crespo NC, Nicosia SV, Hamilton AD, Sebti SM, Cheng JQ. The phosphoinositide 3-OH kinase/AKT2 pathway as a critical target for farnesyltransferase inhibitor-induced apoptosis. Mol Cell Biol. 2000 Jan;20(1):139-148. Pubmedid: 10594016. Pmcid: PMC85069.
  • Blaskovich M, Lin Q, Delarue F, Sun J, Park H, Coppola D, Hamilton A, Sebti S. Design of GFB-111, a platelet-derived growth factor binding molecule with antiangiogenic and anticancer activity against human tumors in mice. Nat Biotechnol. 2000;18(10):1065-1070. Pubmedid: 11017044.
  • Cohen-Jonathan E, Muschel R, Gillies McKenna W, Evans S, Cerniglia G, MickR, Kusewitt D, Sebti S, Hamilton A, Oliff A, Kohl N, Gibbs J, Bernhard E. Farnesyltransferase inhibitors potentiate the antitumor effect of radiation on a human tumor xenograft expressing activated HRAS. Radiat Res. 2000;154(2):125-132. Pubmedid: 10931682.
  • Sun J, Nam S, Lee C, Li B, Coppola D, Hamilton A, Dou Q, Sebti S. CEP1612, a dipeptidyl proteasome inhibitor, induces p21WAF1 and p27KIP1 expression and apoptosis and inhibits the growth of the human lung adenocarcinoma A-549 in nude mice. Cancer Res. 2000;61(4):1280-1284. Pubmedid: 11245420.
  • Chen Z, Sun J, Pradines A, Favre G, Adnane J, Sebti S. Both farnesylated and geranylgeranylated RhoB inhibit malignant transformation and suppress human tumor growth in nude mice. J Biol Chem. 2000;275(4):17974-17978. Pubmedid: 10770919.
  • Cohen E, Muschel R, McKenna W, Evans S, Cerniglia G, Mick R, Kusewitt D, Sebti S, Hamilton A, Oliff A, Kohl N, Gibbs J, Bernhard E. Farnesyltransferase inhibitors potentiate the antitumor effect of radiation on a human tumor xenograft expressing activated HRAS. Radiat Res. 2000;152(2):125-132. Pubmedid: 10931682.
  • Sebti S, Hamilton A. Inhibition of Rho GTPases using protein geranylgeranyltransferase I inhibitors. Methods Enzymol. 2000;325:381-388. Pubmedid: 11036620.
  • Qian Y, Marugan J, Fossum R, Vogt A, Sebti S, Hamilton A. Probing the hydrophobic pocket of farnesyltransferase: aromatic substitution of CAAX peptidomimetics leads to highly potent inhibitors. Biorg Med Chem Lett. 2000;7(12):3011-3024. Pubmedid: 10658608.
  • Zhang H, Wei S, Sun J, Coppola D, Zhong B, Wu G, Goodwin B, Sebti S, Djeu JY, Blanck G. Retinoblastoma protein activation of interleukin 8 expression inhibits tumor cell survival in nude mice. Cell Growth Differ. 2000;11(12):635-639. Pubmedid: 11149598.
  • Allal C, Favre G, Couderc B, Sandrine S, Sizou S, Hamilton A, Sebti S, LajoieMazenc I, Pradines A. RhoA prenylation is required for promotion of cell growth and transformation and cytoskeleton organization but not for induction of serum response element transcription. J Biol Chem. 2000;275(40):31001-31008. Pubmedid: 11027361.
  • Coxon F, Helfrich M, Van't Hof R, Ralston S, Hamilton A, Sebti S, Ralston S, Rogers M. Protein geranylgeranylation is required for osteoclast formation, function, and survival: inhibition by bisphosphonates and GGTI-298. J Bone Miner Res. 2000;15(8):1467-1476. Pubmedid: 10934645.
  • Adnane J, Jackson R, Nicosia S, Cantor A, Pledger W, Sebti S. Loss of p21WAF1/CIP1 accelerates Ras oncogenesis in a transgenic/knockout mammary cancer model. Oncogene. 2000;19(47):5338-5347. Pubmedid: 11103935.
  • Sebti S, Hamilton A. Farnesyltransferase and geranylgeranyltransferase I inhibitors and cancer therapy: lesssons from mechanisms and bench-to-bedside translational studies. Oncogene. 2000;19(56):6584-6593. Pubmedid: 11426643.
  • Rosenbloom J, Saitta B, Gaidarova S, Sandorfi N, Rosenbloom JC, Abrams W, Hamilton A, Sebti S, Kucich U, Jimenez S. Inhibition of type I collagen gene expression in normal and systemic sclerosis fibroblasts by a specific inhibitor of geranylgeranyl transferase I. Arthritis Rheum. 2000;43(7):1624-1632. Pubmedid: 10902768.
  • Sebti S, Hamilton A. Farnesyltransferase and geranylgeranyltransferase I inhibitors in cancer therapy: important mechanistic and bench to bedside issues. Expert Opin Investig Drugs. 2000;9(12):2767-2782. Pubmedid: 11093352.
  • Kothare M, Ohkanda J, Lockman J, Qian Y, Blaskovich M, Sebti S, Hamilton A. Development of a tripeptide mimetic strategy for the inhibition of protein farnesyltransferase. Tetrahedron Lett. 2000;56:9833-9841. Pubmedid: noPMID.
  • Sebti S, Hamilton A. Design of growth factor antagonists with antiangiogenic and antitumor properties. Oncogene. 2000;19(56):6566-6573. Pubmedid: 11426641.
  • Liu L, Moesner P, Kovach NL, Bailey R, Hamilton AD, Sebti SM, Harlan JM. Integrin-dependent leukocyte adhesion involves geranylgeranylated protein(s). J Biol Chem. 1999 Nov;274(47):33334-33340. Pubmedid: 10559211.
  • Turkson J, Bowman T, Adnane J, Zhang Y, Djeu JY, Sekharam M, Frank DA, Holzman LB, Wu J, Sebti S, Jove R. Requirement for Ras/Rac1-mediated p38 and c-Jun N-terminal kinase signaling in Stat3 transcriptional activity induced by the Src oncoprotein. Mol Cell Biol. 1999 Nov;19(11):7519-7528. Pubmedid: 10523640. Pmcid: PMC84756.
  • Cohen E, Toulas C, Ader I, Monteil A, Allal C, Bonnet J, Hamilton A, Sebti S, Daly-Schveitzer N, Favre G. The farnesyltransferase inhibitor FTI-277 suppresses the 24-kDa FGF2-induced radioresistance in HeLa cells expressing wild-type RAS. Radiat Res. 1999 Oct;152(4):404-411. Pubmedid: 10477917.
  • Mazet J, Padieu M, Osman H, Maume G, Mailliet P, Dereu N, Hamilton A, Lavelle F, Sebti S, Maume B. Combination of the novel farnesyltransferase inhibitor RPR130401 and the geranylgeranyltransferase-1 inhibitor GGTI-298 disrupts MAP kinase activation and G(1)-S transition in Ki-Ras-overexpressing transformed adrenocortical cells. FEBS Lett. 1999 Oct;460(2):235-240. Pubmedid: 10544242.
  • Sun J, Blaskovich M, Knowles D, Qian Y, Ohkanda J, Bailey R, Hamilton A, Sebti S. Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine. Cancer Res. 1999 Oct;59(19):4919-4926. Pubmedid: 10519405.
  • Vasudevan A, Qian Y, Vogt A, Blaskovich M, Sebti S, Hamilton A. Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I. J Med Chem. 1999 Apr;42(8):1333-1340. Pubmedid: 10212118.
  • Pollack I, Bredel M, Erff M, Hamilton A, Sebti S. Inhibition of Ras and related guanosine triphosphate-dependent proteins as a therapeutic strategy for blocking malignant glioma growth: II--preclinical studies in a nude mouse model. Neurosurgery. 1999;45(5):1208-1214. Pubmedid: 10549939.
  • O'Conner S, Barr K, Wang L, Sorensen B, Tasker A, Sham H, Ng S, Cohen J, Devine E, Cherian S, Saeed B, Zhang H, Lee J, Warner R, Tahir S, Kovar P, Ewing P, Alder J, Mitten M, Leal J, Marsh K, Bauch J, Hoffman D, Sebti S, Rosenberg S. Second-generation peptidomimetic inhibitors of protein farnesyltransferase demonstrating improved cellular potency and significant in vivo efficacy. J Med Chem. 1999;42(18):3701-3710. Pubmedid: 10479301.
  • Sun Z, Qian Y, Chen Z, Marfurt J, Hamilton A, Sebti S. The geranylgeranyltransferase I inhibitor GGTI-298 induces hypophosphorylation of Rb and partner switching of cyclin-dependent kinase inhibitors: a potential mechanism for GGTI-298 antitumor activity. J Biol Chem. 1999;274:6930-6934. Pubmedid: 10066746.
  • Bowman T, Yu H, Sebti S, Dalton W, Jove R. Signal transducers and activators of transcription: novel targets for anticancer therapeutics. Cancer Control. 1999;6(5):427-435. Pubmedid: 10758575.
  • Adnane J, Bizouarn FA, Qian Y, Hamilton AD, Sebti SM. p21(WAF1/CIP1) is upregulated by the geranylgeranyltransferase I inhibitor GGTI-298 through a transforming growth factor beta- and Sp1-responsive element: involvement of the small GTPase rhoA. Mol Cell Biol. 1998 Dec;18(12):6962-6970. Pubmedid: 9819384. Pmcid: PMC109279.
  • Kucich U, Rosenbloom JC, Shen G, Abrams WR, Blaskovich MA, Hamilton AD, Ohkanda J, Sebti SM, Rosenbloom J. Requirement for geranylgeranyl transferase I and acyl transferase in the TGF-beta-stimulated pathway leading to elastin mRNA stabilization. Biochem Bioph Res Co. 1998 Nov;252(1):111-116. Pubmedid: 9813154.
  • Bredel M, Pollack IF, Freund JM, Hamilton AD, Sebti SM. Inhibition of Ras and related G-proteins as a therapeutic strategy for blocking malignant glioma growth. Neurosurgery. 1998 Jul;43(1):124-131. Pubmedid: 9657198.
  • Stark WW, Blaskovich MA, Johnson BA, Qian Y, Vasudevan A, Pitt B, Hamilton AD, Sebti SM, Davies P. Inhibiting geranylgeranylation blocks growth and promotes apoptosis in pulmonary vascular smooth muscle cells. Am J Physiol. 1998 Jul;275(1 Pt 1):L55-L63. Pubmedid: 9688935.
  • Bernhard EJ, McKenna WG, Hamilton AD, Sebti SM, Qian Y, Wu JM, Muschel RJ. Inhibiting Ras prenylation increases the radiosensitivity of human tumor cell lines with activating mutations of ras oncogenes. Cancer Res. 1998 Apr;58(8):1754-1761. Pubmedid: 9563495.
  • Sun J, Qian Y, Hamilton AD, Sebti SM. Both farnesyltransferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic K-Ras prenylation but each alone is sufficient to suppress human tumor growth in nude mouse xenografts. Oncogene. 1998 Mar;16(11):1467-1473. Pubmedid: 9525745.
  • Qian Y, Vogt A, Vasudevan A, Sebti S, Hamilton A. Selective inhibition of type-I geranylgeranyltransferase in vitro and in whole cells by CAAL peptidomimetics. Biorg Med Chem Lett. 1998;6(3):293-299. Pubmedid: 09568283.
  • Stark W, Blaskovich M, Johnson B, Vasudevan A, Hamilton A, Sebti S, Davies P. Inhibiting geranylgeranylation blocks growth and promotes apoptosis in pulmonary vascular smooth muscle cells. Am J Physiol. 1998;275(1):L55-L63. Pubmedid: 09688935.
  • Kucich U, Rosenberg J, Shen G, Abrams W, Blaskovich M, Ohkanda J, Hamilton A, Sebti S, Rosenberg J. Requirement for geranylgeranyl transferase I and acyl transferase in the TGF-beta-stimulated pathway leading to elastin mRNA stabilization. Biochem Biophys Res Commun. 1998;252(1):111-116. Pubmedid: 09813154.
  • Bredel M, Pollack I, Freund J, Hamilton A, Sebti S. Inhibition of Ras and related G-proteins as a therapeutic strategy for blocking malignant glioma growth. Neurosurgery. 1998;43(1):124-132. Pubmedid: 09657198.
  • Hamilton A, Sebti S. New approaches to anticancer drug design based on the inhibition of farnesyltransferase. Ddt. 1998;3(1):26-33. Pubmedid: noPMID.
  • Adnane J, Bizouarn F, Qian Y, Hamilton A, Sebti S. p21(WAF1/CIP1) is upregulated by the geranylgeranyltransferase I inhibitor GGTI-298 through a transforming growth factor beta- and Sp1-responsive element: involvement of the small GTPase rhoA. Mol Cell Biol. 1998;18(12):6962-6970. Pubmedid: 09819384.
  • Bernhard E, McKenna W, Hamilton A, Sebti S, Qian Y, Muschel R. Inhibiting Ras prenylation increases the radiosensitivity of human tumor cell lines with activating mutations of ras oncogenes. Cancer Res. 1998;58(8):1754-1761. Pubmedid: 09563495.
  • Sebti S, Hamilton A. New approaches to anti-cancer drug design based on the inhibition of farnesyltransferase. Drug Discovery. 1998;3:26-33. Pubmedid: noPMID.
  • Sun J, Qian Y, Hamilton A, Sebti S. Both farnesyltransferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic K-Ras prenylation but each alone is sufficient to suppress human tumor growth in nude mouse xenografts. Oncogene. 1998;16(11):1467-1473. Pubmedid: 09525745.
  • Vogt A, Sun J, Qian Y, Hamilton AD, Sebti SM. The geranylgeranyltransferase-I inhibitor GGTI-298 arrests human tumor cells in G0/G1 and induces p21(WAF1/CIP1/SDI1) in a p53-independent manner. J Biol Chem. 1997 Oct;272(43):27224-27229. Pubmedid: 9341167.
  • Lerner EC, Zhang TT, Knowles DB, Qian Y, Hamilton AD, Sebti SM. Inhibition of the prenylation of K-Ras, but not H- or N-Ras, is highly resistant to CAAX peptidomimetics and requires both a farnesyltransferase and a geranylgeranyltransferase I inhibitor in human tumor cell lines. Oncogene. 1997 Sep;15(11):1283-1288. Pubmedid: 9315095.
  • Finder JD, Litz JL, Blaskovich MA, McGuire TF, Qian Y, Hamilton AD, Davies P, Sebti SM. Inhibition of protein geranylgeranylation causes a superinduction of nitric-oxide synthase-2 by interleukin-1beta in vascular smooth muscle cells. J Biol Chem. 1997 May;272(21):13484-13488. Pubmedid: 9153192.
  • Miquel K, Pradines A, Sun J, Qian Y, Hamilton AD, Sebti SM, Favre G. GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells. Cancer Res. 1997 May;57(10):1846-1850. Pubmedid: 9157972.
  • McGuire TF, Sebti SM. Geranylgeraniol potentiates lovastatin inhibition of oncogenic H-Ras processing and signaling while preventing cytotoxicity. Oncogene. 1997 Jan;14(3):305-312. Pubmedid: 9018116.
  • Sebti S, Hamilton A. Anticancer activity of farnesyltransferase and geranylgeranyltransferase I inhibitors: prospects for drug development. Expert Opinion On Inv Drugs. 1997;6:1711-1714. Pubmedid: 15989575.
  • Lerner E, Hamilton A, Sebti S. Inhibition of Ras prenylation: a signaling target for novel anticancer drug design. Anticancer Drug Design. 1997;12:229-238. Pubmedid: 09199657.
  • Qian Y, Sebti S, Hamilton A. Farnesyltransferase as as target for anti-cancer drug design. Biopolymers. 1997;43:25-41. Pubmedid: 09174410.
  • Clark G, Kinch M, Rogers-Graham K, Sebti S, Hamilton A, Der C. The Ras-related protein Rheb is farnesylated and antagonizes Ras signaling and transformation. J Biol Chem. 1997;272:10609-10615. Pubmedid: 09099708.
  • Sebti S, McGuire T. Geranylgeraniol potentiates lovastatin inhibition of oncogenic H-Ras processing and signaling while preventing cytotoxicity. Oncogene. 1997;14:305-312. Pubmedid: 09018116.
  • Qian Y, Sebti S, Hamilton A. Peptidomimetic inhibitors of farnesyltransferase: an approach to new antitumor agents. Adv Amino Acid Mem And Pep. 1997;1:165-192. Pubmedid: noPMID.
  • Sebti S, Hamilton A. Inhibition of Ras prenylation: a novel approach to cancer chemotherapy. Pharmacol Ther. 1997;74(1):103-114. Pubmedid: 09336018.
  • Sebti S, Hamilton A. Inhibitors of prenyltransferases. Curr Opin Oncol. 1997;9:557-561. Pubmedid: 09370077.
  • Vogt A, Sun J, Qian Y, Hamilton A, Sebti S. The geranylgeranyltransferase-I inhibitor GGTI-298 arrests human tumor cells in G0/G1 and induces p21 (WAF1/CIP1/SDI1) in a p53-independent manner. J Biol Chem. 1997;272(43):27224-27229. Pubmedid: 09341167.
  • Miquel K, Pradines A, Sun J, Hamilton A, Sebti S, Favre G, Qian Y. GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells. Cancer Res. 1997;57(10):1846-1850. Pubmedid: 09157972.
  • Lerner E, Zhang T, Knowles D, Qian Y, Hamilton A, Sebti S. Inhibition of the prenylation of K-Ras, but not H- or N-Ras, is highly resistant to CAAX peptidomimetics and requires both a farnesyltransferase and a geranylgeranyltransferase I inhibitor in human tumor cell lines. Oncogene. 1997;15(11):1283-1288. Pubmedid: 09315095.
  • Finder J, Litz J, Blaskovich M, McGuire T, Qian Y, Hamilton A, Davies P, Sebti S. Inhibition of protein geranylgeranylation causes a superinduction of nitric oxide synthase-2 by interleukin-1(beta) in vascular smooth muscle cells. J Biol Chem. 1997;272:13484-13488. Pubmedid: 09153192.
  • McGuire TF, Qian Y, Vogt A, Hamilton AD, Sebti SM. Platelet-derived growth factor receptor tyrosine phosphorylation requires protein geranylgeranylation but not farnesylation. J Biol Chem. 1996 Nov;271(44):27402-27407. Pubmedid: 8910319.
  • Vogt A, Qian Y, McGuire TF, Hamilton AD, Sebti SM. Protein geranylgeranylation, not farnesylation, is required for the G1 to S phase transition in mouse fibroblasts. Oncogene. 1996 Nov;13(9):1991-1999. Pubmedid: 8934546.
  • Pei Z, Sebti SM. Cys102 and His398 are required for bleomycin-inactivating activity but not for hexamer formation of yeast bleomycin hydrolase. Biochemistry-Us. 1996 Aug;35(33):10751-10756. Pubmedid: 8718865.
  • Bernhard EJ, Kao G, Cox AD, Sebti SM, Hamilton AD, Muschel RJ, McKenna WG. The farnesyltransferase inhibitor FTI-277 radiosensitizes H-ras-transformed rat embryo fibroblasts. Cancer Res. 1996 Apr;56(8):1727-1730. Pubmedid: 8620483.
  • Xu XQ, McGuire TF, Blaskovich MA, Sebti SM, Romero G. Lovastatin inhibits the stimulation of mitogen-activated protein kinase by insulin in HIRcB fibroblasts. Arch Biochem Biophys. 1996 Feb;326(2):233-237. Pubmedid: 8611028.
  • Qian Y, Vogt A, Sebti SM, Hamilton AD. Design and synthesis of non-peptide Ras CAAX mimetics as potent farnesyltransferase inhibitors. J Med Chem. 1996 Jan;39(1):217-223. Pubmedid: 8568811.
  • Xu X, McGuire T, Blaskovitch M, Sebti S, Romero G. Effects of lovastatin on the stimulation of mitogen-activated protein (MAP) kinase by insulin in HIRcB fibroblasts. Arch Biochem Biophys. 1996;326:233-237. Pubmedid: 08611028.
  • Qian Y, Vogt A, Sebti S, Hamilton A. Design and synthesis of non-peptide Ras CAAX mimetics as potent farnesyltransferase inhibitors. J Med Chem. 1996;39:217-233. Pubmedid: 08568811.
  • Bernhard E, Kao G, Cox A, Sebti S, Hamilton A, Muschel R, McKenna W. The farnesyltransferase inhibitor FTI-277 radiosensitizes Ras (H)-transformed rat embryo fibroblasts. Cancer Res. 1996;56:1727-1730. Pubmedid: 08620483.
  • Vogt A, Qian Y, McGuire T, Hamilton A, Sebti S. Protein geranylgeranylation, not farnesylation, is required for the G1 to S phase transition in mouse fibroblasts. Oncogene. 1996;13:1991-1999. Pubmedid: 08934546.
  • Der C, Cox A, Sebti S, Hamilton A. Farnesyltransferase inhibitors: anti-Ras drugs for cancer treatment?. Anticancer Drugs. 1996;7:165-172.
  • Pei Z, Sebti S. Cys (102) and His (398) are required for bleomycin-inactivating activity but not for hexamer formation of yeast bleomycin hydrolase. Biochemistry. 1996;35:10751-10756. Pubmedid: 08718865.
  • McGuire T, Qian Y, Hamilton A, Sebti S. Platelet derived growth factor receptor tyrosine phosphorylation reqiures protein geranylgeranylation and not farnesylation. J Biol Chem. 1996;271:27402-27407. Pubmedid: 08910319.
  • Sebti S, Hamilton A. Rational design of Ras prenyltransferase inhibitors as potential anticancer drugs. Biochem Soc Trans. 1996;24:692-699. Pubmedid: 08878828.
  • Lerner EC, Qian Y, Hamilton AD, Sebti SM. Disruption of oncogenic K-Ras4B processing and signaling by a potent geranylgeranyltransferase I inhibitor. J Biol Chem. 1995 Nov;270(45):26770-26773. Pubmedid: 7592913.
  • Kauffmann RC, Qian Y, Vogt A, Sebti SM, Hamilton AD, Carthew RW. Activated Drosophila Ras1 is selectively suppressed by isoprenyl transferase inhibitors. Proc Natl Acad Sci U S A. 1995 Nov;92(24):10919-10923. Pubmedid: 7479910. Pmcid: PMC40542.
  • Lerner EC, Qian Y, Blaskovich MA, Fossum RD, Vogt A, Sun J, Cox AD, Der CJ, Hamilton AD, Sebti SM. Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras-Raf complexes. J Biol Chem. 1995 Nov;270(45):26802-26806. Pubmedid: 7592920.
  • Vogt A, Sun J, Qian Y, Tan-Chiu E, Hamilton AD, Sebti SM. Burkitt lymphoma Daudi cells contain two distinct farnesyltransferases with different divalent cation requirements. Biochemistry-Us. 1995 Sep;34(38):12398-12403. Pubmedid: 7547984.
  • Vogt A, Qian Y, Blaskovich M, Fossum R, Hamilton A, Sebti S. A non-peptide mimetic of Ras CAAX: selective inhibition of farnesyltransferase and Ras processing. J Biol Chem. 1995;270:660-664. Pubmedid: 07822292.
  • Lerner E, Qian Y, Hamilton A, Sebti S. Disruption of oncogenic K-Ras 4B processing and signaling by a potent Geranylgcranyltransferase I inhibitor. J Biol Chem. 1995;270:26770-26773. Pubmedid: 07592913.
  • Pei Z, Calmels T, Creutz C, Sebti S. Yeast cysteine proteinase YCP1 gene induces bleomycin resistance in mammalian cells. Mol Pharmacol. 1995;48:676-681. Pubmedid: 07476893.
  • Lerner E, Qian Y, Blaskovitch S, FOssum R, Vogt A, Cox A, Der C, Hamilton A, Sebti S. Ras CAAX peptidomimetic FTI 277 selectively blocks oncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras/Raf complexes. J Biol Chem. 1995;270:26802-26806. Pubmedid: 07592920.
  • McGuire T, Qian Y, Blaskovich M, Fossum R, Sun J, Marlowe T, Corey S, Wathen S, Vogt A, Hamilton A, Sebti S. CAAX peptidomimetic FTI-244 decreases platelet-dervied growth factor receptor tyrosine phosphorylation levels and inhibits stimulation of phosphatidylinositol 3-kinase but not mitogen-activated protein kinase. Biochem Biophys Res Commun. 1995;214:295-303. Pubmedid: 07669049.
  • Vogt A, Sun J, Qian Y, Hamilton A, Sebti S. Burkitt lymphoma Daudi cells contain two district farnesyltransferases with different divalent cation requirements. Biochemistry. 1995;34:12398-12403. Pubmedid: 07547984.
  • Kauffman R, Qian Y, Vogt A, Sebti S, Hamilton A, Carthew R. Activated drosophila Ras 1 is selectively suppressed by isoprenylthransferase inhibitors. Proc Natl Acad Sci U S A. 1995;92:10919-10923. Pubmedid: 07479910.
  • Sun J, Qian Y, Hamilton A, Sebti S. Ras CAAX peptidomimetic FTI 276 selectively blocks tumor growth in nude mice of a human lung carcinoma with K-Ras mutation and p53 deletion. Cancer Res. 1995;55:4243-4247. Pubmedid: 07671229.
  • McGuire TF, Xu XQ, Corey SJ, Romero GG, Sebti SM. Lovastatin disrupts early events in insulin signaling: a potential mechanism of lovastatin's anti-mitogenic activity. Biochem Bioph Res Co. 1994 Oct;204(1):399-406. Pubmedid: 7524501.
  • Weng W, Reynolds IJ, Jani JP, Blaskovich M, Sebti SM, Davies P, Pitt BR. Desensitization of 5HT2 receptors by protein kinase C activation in distal pulmonary vascular smooth muscle cells in culture. Microcirculation. 1994 Jul;1(2):129-135. Pubmedid: 8790584.
  • McGuire T, Xu X, Corey S, Romero G, Sebti S. Lovastatin disrupts early events in insulin signaling: A potential mechanism of lovastatin's anti-mitogenic activity. Biochem Biophys Res Commun. 1994;204:399-406.
  • Qian Y, Blaskovich M, Saleem M, Wathen S, Hamilton A, Sebti S. Design and structural requirements of potent peptidomimetic inhibitors of p21ras Farnesyl transferase. J Biol Chem. 1994;269:12410-12413.
  • McGuire T, Corey S, Sebti S. Lovastatin inhibits PDGF stimulation of phosphatidyl inositol 3-kinase activity as well as the association of p85 subunit to tyrosine-phosphorylated PDGF receptor. J Biol Chem. 1993;268:22227-22230.
  • Nigam M, Seong C, Qian Y, Hamilton A, Sebti S. Potent inhibition of human tumor p21 ras farnesyl transferase by A(1)A(2)-lacking CA(1)A(2)X peptidominetics. J Biol Chem. 1993;268:20695-20698.
  • Jani JP, Mistry JS, Morris G, Davies P, Lazo JS, Sebti SM. In vivo circumvention of human colon carcinoma resistance to bleomycin. Cancer Res. 1992 May;52(10):2931-2937. Pubmedid: 1374681.
  • Morris G, Mistry J, Jani J, Mignano J, Sebti S, Lazo J. Neutralization of bleomycin hydrolase by an epitope-specific antibody. Mol Pharmacol. 1992;42:57-62.
  • Mistry J, Jani J, Morris G, Mujumdar R, Reynolds J, Sebti S, Lazo J. Synthesis and evaluation of a novel fluorescence-labelled derivative of talismycin S (10b) as a probe for identifying bleomycin-resistant cells. Cancer Res. 1992;52:709-718.
  • Jani J, Mistry J, Morris G, Lazo J, Sebti S. In vivo circumvention of human colon carcinoma resistance to bleomycin. Cancer Res. 1992;52:2931-2937.
  • Jani JP, Mistry JS, Morris G, Lazo JS, Sebti SM. In vivo sensitization of human lung carcinoma to bleomycin by the cysteine proteinase inhibitor E-64. Oncol Res. 1992;4(2):59-63. Pubmedid: 1375852.
  • Morris G, Mistry JS, Jani JP, Sebti SM, Lazo JS. Cysteine proteinase inhibitors and bleomycin-sensitive and -resistant cells. Biochem Pharmacol. 1991 Jun;41(11):1559-1566. Pubmedid: 1710457.
  • Sebti SM, Jani JP, Mistry JS, Gorelik E, Lazo JS. Metabolic inactivation: a mechanism of human tumor resistance to bleomycin. Cancer Res. 1991 Jan;51(1):227-232. Pubmedid: 1703034.
  • Mistry JS, Sebti SM, Lazo JS. Separation of bleomycins and their deamido metabolites by high-performance cation-exchange chromatography. Ai Zheng. 1990 Aug;514(1):86-90. Pubmedid: 1698802.
  • Baird WM, Sebti SM, Reinsvold LA. Metabolic activation of benzo(a)pyrene in SENCAR and BALB/c mouse embryo cell cultures. Environ Health Persp. 1986 Sep;68:45-52. Pubmedid: 3780631. Pmcid: PMC1474259.
  • Sebti SM, Moynihan CG, Anderson JN, Baird WM. Benzo[a]pyrene-DNA adduct formation in target and activator cells in a Wistar rat embryo cell-mediated V79 cell mutation assay. Carcinogenesis. 1985 Jul;6(7):983-988. Pubmedid: 4017178.
  • Sebti SM, Pruess-Schwartz D, Baird WM. Species- and length of exposure-dependent differences in the benzo(a)pyrene:DNA adducts formed in embryo cell cultures from mice, rats, and hamsters. Cancer Res. 1985 Apr;45(4):1594-1600. Pubmedid: 3978626.
  • Pruess-Schwartz D, Sebti SM, Gilham PT, Baird WM. Analysis of benzo(a)pyrene:DNA adducts formed in cells in culture by immobilized boronate chromatography. Cancer Res. 1984 Sep;44(9):4104-4110. Pubmedid: 6331665.
  • Sebti SM, Baird WM. Rat liver homogenate (S9)-mediated binding of benzo[alpha]pyrene to DNA in V79 cells, V79 cell nuclei and aqueous solution. Mutat Res-Fund Mol M. 1984 Feb;125(2):307-314. Pubmedid: 6321977.
  • Sebti SM, Baird WM, Knowles BB, Diamond L. Benzo[a]pyrene--DNA adduct formation in target cells in a cell-mediated mutation assay. Carcinogenesis. 1982;3(11):1317-1320. Pubmedid: 6817937.
  • Lazo J, Hoyt D, Sebti S, Pitt B. The use of bleomycin in model systems to study the pathogenesis of interstitial pulmonary fibrosis. In: Gram T, ed. International encyclopedia of pharmacology and therapeutics. Oxford. Pregmon Press, Ltd; 1992;271-287.
  • Husain K, Centeno BA, Chen DT, Fulp WJ, Perez M, Zhang Lee G, Luetteke N, Hingorani SR, Sebti SM, Malafa MP. Prolonged survival and delayed progression of pancreatic intraepithelial neoplasia in LSL-KrasG12D/+;Pdx-1-Cre mice by vitamin E ?-tocotrienol. Carcinogenesis. 2013 Apr;34(4):858-863. Pubmedid: 23302291. Pmcid: PMC3616675.
  • Sebti S, Lazo J. Bleomycin hydrolase and tumor resistance to bleomycin. In: Sartorelli A, Powis P, eds. International Encyclopedia of Pharmacology and Therapeutics. Oxford. Pergamon Press Ltd; 1994;387-396.
  • Husain K, Centeno BA, Chen DT, Hingorani S, Sebti SM, Malafa MP. Vitamin E ?-Tocotrienol Prolongs Survival in the LSL-KrasG12D/+;LSL-Trp53R172H/+;Pdx-1-Cre (KPC) Transgenic Mouse Model of Pancreatic Cancer. Cancer Prev Res (Phila). 2013 Oct;6(10):1074-1083. Pubmedid: 23963802.
  • Lazo J, Sebti S. Bleomycin. In: Pindeo H, Longo D, Chabner B, et al, eds. Cancer chemotherapy and Biological Response Modifiers. 17 ed. Amsterdam. Elsevier Science Publishers B.V. (Biochemical Division); 1997;40-45.
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