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Chemical Biology - Key Publications Over the Last Five Years

1. 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 PMID: 20644979. PMCID: PMC4612514. IF: 2.919

2. 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 PMID: 21148306. PMCID: PMC3059047. IF: 4.573  

3. 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 PMID: 21193311. PMCID: PMC3034307. IF: 2.420

4. Fragale A, Stellacci E, Ilari R, Remoli AL, Lanciotti A, Perrotti E, Shytaj I, Orsatti R, Lawrence HR, Lawrence NJ, Wu J, Rehli M, Ozato K, Battistini A. Critical role of IRF-8 in negative regulation of TLR3 expression by Src homology 2 domain-containing protein tyrosine phosphatase-2 activity in human myeloid dendritic cells. J Immunol 2011 Feb; 186: (4) 1951-1962 PMID: 21220691. PMCID: PMC4053178. IF: 4.922

5. Betzi S, Alam R, Martin M, Lubbers DJ, Han H, Jakkaraj SR, Georg GI, Schönbrunn E. Discovery of a potential allosteric ligand binding site in CDK2. Acs Chem Biol 2011 May; 6: (5) 492-501 PMID: 21291269. PMCID: PMC3098941. IF: 5.331

6. 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 PMID: 21536547. PMCID: PMC3156694. IF: 8.722

7. Chen F, Pisklakova A, Li M, Baz R, Sullivan DM, Nefedova Y. Gamma-secretase inhibitor enhances the cytotoxic effect of bortezomib in multiple myeloma. Cell Oncol (Dordr) 2011 Dec; 34: (6) 545-551 PMID: 21965140. PMCID: PMC3417352. IF: 3.032

8. 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 PMID: 22086850. PMCID: PMC3261351. IF: 9.329

9. Davis R, Pillai S, Lawrence N, Sebti S, Chellappan SP. TNF-α-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 PMID: 22185776. PMCID: PMC3272234. IF: 5.243

10. 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 PMID: 22220566. PMCID: PMC3530929. IF: 5.447

11. Alamanda V, Singh S, Lawrence NJ, Chellappan SP. Nicotine-mediated induction of E-selectin in aortic endothelial cells requires Src kinase and E2F1 transcriptional activity. Biochem Bioph Res Co 2012 Feb; 418: (1) 56-61 PMID: 22240023. PMCID: PMC3273677. IF: 2.297

12. 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 PMID: 22248356. PMCID: PMC4429595.IF: 5.331

13. 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) 2474-2478PMID: 22272748. PMCID: PMC4516226. IF: 5.447

14. 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 PMID: 22306001. PMCID: PMC3319810. IF: 5.621  

15. 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 PMID: 22311987. PMCID: PMC3323047. IF: 4.573

16. Mahajan K, Coppola D, Chen YA, Zhu W, Lawrence HR, Lawrence NJ, Mahajan NP. Ack1 tyrosine kinase activation correlates with pancreatic cancer progression. Am J Pathol 2012 Apr; 180: (4) 1386-1393 PMID: 22322295. PMCID: PMC3349895. IF: 4.591

17. Mahajan K, Coppola D, Rawal B, Chen YA, Lawrence HR, Engelman RW, Lawrence NJ, Mahajan NP. Ack1-mediated androgen receptor phosphorylation modulates radiation resistance in castration-resistant prostate cancer. J Biol Chem 2012 Jun; 287: (26) 22112-22122 PMID: 22566699.PMCID: PMC3381169. IF: 4.573

18. 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 PMID: 22761337. PMCID: PMC4557794. IF: 9.329

19. 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 Chem2012 Sep; 55: (17) 7392-7416 PMID: 22803810. PMCID: PMC4429609. IF: 5.447

20. 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 PMID: 22846914. PMCID: PMC3463757. IF: 9.329  

21. Martin MP, Alam R, Betzi S, Ingles DJ, Zhu JY, Schönbrunn E. A novel approach to the discovery of small-molecule ligands of CDK2. Chembiochem 2012 Sep; 13: (14) 2128-2136 PMID: 22893598. PMCID: PMC3483082. IF: 3.088

22. 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) 3250-3259PMID: 22894899. PMCID: PMC3466524. IF: 5.243

23. 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 PMID: 22901384. PMCID: PMC3432503. IF: 2.420

24. Wu S, Chen L, Becker A, Schonbrunn E, Chen J. Casein kinase 1α regulates an MDMX intramolecular interaction to stimulate p53 binding. Mol Cell Biol 2012 Dec; 32: (23) 4821-4832 PMID: 23028042. PMCID: PMC3497597. IF: 4.777

25. 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 PMID: 23272972. PMCID: PMC4052463. IF: 2.469  

26. 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 PMID: 23275831.PMCID: PMC3531244. IF: 2.495  

27. 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 PMID: 23322008. PMCID: PMC4030628. IF: 9.329  

28. Tecleab A, Sebti SM. Depletion of K-Ras promotes proteasome degradation of survivin. Cell Cycle 2013 Feb; 12: (3) 522-532 PMID: 23324341. PMCID: PMC3587453. IF: 5.243

29. 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 PMID: 23396364. PMCID: PMC3977753. IF: 8.459

30. 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 PMID: 23547706. PMCID: PMC3774303. IF: 5.447

31. 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 May; 56: (10) 3768-3782 PMID: 23600925. PMCID: PMC3714109. IF: 5.447

32. Olesen SH, Ingles DJ, Yang Y, Schönbrunn E. Differential antibacterial properties of the MurA inhibitors terreic acid and fosfomycin. J Basic Microbiol 2014 Apr; 54: (4) 322-326 PMID: 23686727. PMCID: PMC4610358. IF: 1.823

33. 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 PMID: 24073326. PMCID: PMC3780559. IF: 2.495  

34. 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 PMID: 24107447. PMCID: PMC3858536. IF: 5.683

35. Blaskovich MA, Yendluri V, Lawrence HR, Lawrence NJ, Sebti SM, Springett GM. Lysophosphatidic acid acyltransferase beta regulates mTOR signaling. PLoS One 2013 ; 8: (10) e78632- PMID: 24205284. PMCID: PMC3814986. IF: 3.234  

36. Remsing Rix LL, Kuenzi BM, Luo Y, Remily-Wood E, Kinose F, Wright G, Li J, Koomen JM, Haura EB, Lawrence HR, Rix U. GSK3 alpha and beta are new functionally relevant targets of tivantinib in lung cancer cells. Acs Chem Biol 2014 Feb; 9: (2) 353-358 PMID: 24215125. PMCID: PMC3944088. IF: 5.331

37. Kazi A, Ozcan S, Tecleab A, Sun Y, Lawrence HR, Sebti SM. Discovery of PI-1840, a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity. J Biol Chem 2014 Apr; 289: (17) 11906-11915 PMID: 24570003. PMCID: PMC4002098. IF: 4.573

38. Ember SW, Zhu JY, Olesen SH, Martin MP, Becker A, Berndt N, Georg GI, Schonbrunn E. Acetyl-lysine binding site of bromodomain-containing protein 4 (BRD4) interacts with diverse kinase inhibitors. Acs Chem Biol 2014 May; 9: (5) 1160-1171 PMID: 24568369. PMCID: PMC4032195. IF: 5.331

39. Tang CH, Ranatunga S, Kriss CL, Cubitt CL, Tao J, Pinilla-Ibarz JA, Del Valle JR, Hu CC. Inhibition of ER stress-associated IRE-1/XBP-1 pathway reduces leukemic cell survival. J Clin Invest 2014 Jun; 124: (6) 2585-2598 PMID: 24812669. PMCID: PMC4038575. IF: 13.215

40. Kurtyka CA, Chen L, Cress WD. E2F inhibition synergizes with paclitaxel in lung cancer cell lines. PLoS One 2014 ; 9: (5) e96357- PMID: 24831239. PMCID: PMC4022639. IF: 3.234

41. Yang H, Lawrence HR, Kazi A, Gevariya H, Patel R, Luo Y, Rix U, Schonbrunn E, Lawrence NJ, Sebti SM. Dual Aurora A and JAK2 kinase blockade effectively suppresses malignant transformation. Oncotarget 2014 May; 5: (10) 2947-2961 PMID: 24930769. PMCID: PMC4102782. IF: 6.359

42. Rebecca VW, Alicea GM, Paraiso KH, Lawrence H, Gibney GT, Smalley KS. Vertical inhibition of the MAPK pathway enhances therapeutic responses in NRAS-mutant melanoma. Pigment Cell Melanoma Res 2014 Nov; 27: (6) 1154-1158 PMID: 25130256. PMCID: PMC4211982. IF: 4.619

43. Mahajan K, Lawrence HR, Lawrence NJ, Mahajan NP. ACK1 tyrosine kinase interacts with histone demethylase KDM3A to regulate the mammary tumor oncogene HOXA1. J Biol Chem 2014 Oct; 289: (41) 28179-28191 PMID: 25148682. PMCID: PMC4192474. IF: 4.573

44. Kim YB, Kang CW, Ranatunga S, Yang H, Sebti SM, Del Valle JR. Imidazo[1,2-a]pyridine-based peptidomimetics as inhibitors of Akt. Bioorg Med Chem Lett 2014 Oct; 24: (19) 4650-4653 PMID: 25205195. PMCID: PMC4176526. IF: 2.420

45. Mishra NK, Urick AK, Ember S, Schonbrunn E, Pomerantz WC. Fluorinated aromatic amino acids are sensitive 19F NMR probes for bromodomain-ligand interactions. Acs Chem Biol 2014 Dec; 9: (12) 2755-2760 PMID: 25290579. PMCID: PMC4273984. IF: 5.331

46. Kang CW, Ranatunga S, Sarnowski MP, Del Valle JR. Solid-phase synthesis of tetrahydropyridazinedione-constrained peptides. Org Lett 2014 Oct; 16: (20) 5434-5437 PMID: 25295511. PMCID: PMC4201324. IF: 6.364

47. Li R, Cheng C, Balasis ME, Liu Y, Garner TP, Daniel KG, Li J, Qin Y, Gavathiotis E, Sebti SM. Design, synthesis and evaluation of marinopyrrole derivatives as selective inhibitors of Mcl-1 binding to pro-apoptotic Bim and dual Mcl-1/Bcl-xL inhibitors. Eur J Med Chem 2015 Jan; 90: 315-331 PMID: 25437618. PMCID: PMC4445146. IF: 3.447  

48. Betts BC, Sagatys EM, Veerapathran A, Lloyd MC, Beato F, Lawrence HR, Yue B, Kim J, Sebti SM, Anasetti C, Pidala J. CD4+ T cell STAT3 phosphorylation precedes acute GVHD, and subsequent Th17 tissue invasion correlates with GVHD severity and therapeutic response. J Leukoc Biol 2015 Apr; 97: (4) 807-819 PMID: 25663681. PMCID: PMC4370048. IF: 4.289

49. Lawrence HR, Mahajan K, Luo Y, Zhang D, Tindall N, Huseyin M, Gevariya H, Kazi S, Ozcan S, Mahajan N, Lawrence NJ. Development of novel ACK1/TNK2 inhibitors using a fragment-based approach. J Med Chem 2015 Mar; 58: (6) 2746-2763 PMID: 25699576. PMCID: PMC4605435. IF: 5.447

50. Schneeberger VE, Ren Y, Luetteke N, Huang Q, Chen L, Lawrence HR, Lawrence NJ, Haura EB, Koomen JM, Coppola D, Wu J. Inhibition of Shp2 suppresses mutant EGFR-induced lung tumors in transgenic mouse model of lung adenocarcinoma. Oncotarget 2015 Mar; 6: (8) 6191-6202PMID: 25730908. PMCID: PMC4467431. IF: 6.359

51. Chen L, Borcherds W, Wu S, Becker A, Schonbrunn E, Daughdrill GW, Chen J. Autoinhibition of MDMX by intramolecular p53 mimicry. Proc Natl Acad Sci U S A 2015 Apr; 112: (15) 4624-4629 PMID: 25825738. PMCID: PMC4403185. IF: 9.674

52. Grigson ER, Ozerova M, Pisklakova A, Liu H, Sullivan DM, Nefedova Y. Canonical Wnt pathway inhibitor ICG-001 induces cytotoxicity of multiple myeloma cells in Wnt-independent manner. PLoS One 2015 ; 10: (1) e0117693- PMID: 25635944. PMCID: PMC4311909. IF: 3.234

53. Brooks WH, Guida WC, Daniel KG. The significance of chirality in drug design and development. Curr Top Med Chem 2011 Apr; 11: (7) 760-770 PMID: 21291399. IF: 3.402

54. Zhu JY, Yang Y, Han H, Betzi S, Olesen SH, Marsilio F, Schönbrunn E. Functional consequence of covalent reaction of phosphoenolpyruvate with UDP-N-acetylglucosamine 1-carboxyvinyltransferase (MurA). J Biol Chem 2012 Apr; 287: (16) 12657-12667 PMID: 22378791. PMCID: PMC3339971. IF: 4.573

55. Santiago DN, Pevzner Y, Durand AA, Tran M, Scheerer RR, Daniel K, Sung SS, Woodcock HL, Guida WC, Brooks WH. Virtual target screening: validation using kinase inhibitors. J Chem Inf Model 2012 Aug; 52: (8) 2192-2203 PMID: 22747098. PMCID: PMC3488111. IF: 3.738  

56. Ranatunga S, Tang CH, Hu CC, Del Valle JR. Total synthesis and structural revision of lucentamycin A. J Org Chem 2012 Nov; 77: (21) 9859-9864 PMID: 23039096. IF: 4.721

57. Kang CW, Sun Y, Del Valle JR. Substituted imidazo[1,2-a]pyridines as β-strand peptidomimetics. Org Lett 2012 Dec; 14: (24) 6162-6165 PMID: 23210770. PMCID: PMC3528799. IF: 6.364

58. Martin MP, Olesen SH, Georg GI, Schonbrunn E. Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains. Acs Chem Biol 2013 Nov; 8: (11) 2360-2365 PMID: 24007471. PMCID: PMC3846258. IF: 5.331

59. 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-x(L) binding to Bim. Mar Drugs 2014 Mar; 12: (3) 1335-1348 PMID: 24608970. PMCID: PMC3967213. IF: 2.853

60. Ranatunga S, Tang CH, Kang CW, Kriss C, Kloppenburg B, Hu CC, Del Valle JR. Synthesis of novel tricyclic chromenone-based inhibitors of IRE-1 RNase activity. J Med Chem 2014 May; 57: (10) 4289-4301 PMID: 24749861. PMCID: PMC4032190. IF: 5.447

61. Condamine T, Kumar V, Ramachandran IR, Youn JI, Celis E, Finnberg N, El-Deiry WS, Winograd R, Vonderheide RH, English NR, Knight SC, Yagita H, McCaffrey JC, Antonia S, Hockstein N, Witt R, Masters G, Bauer T, Gabrilovich DI. ER stress regulates myeloid-derived suppressor cell fate through TRAIL-R-mediated apoptosis. J Clin Invest 2014 Jun; 124: (6) 2626-2639 PMID: 24789911. PMCID: PMC4038578. IF: 13.215  

62. Cheng C, Liu Y, Balasis ME, Garner TP, Li J, Simmons NL, Berndt N, Song H, Pan L, Qin Y, Nicolaou KC, Gavathiotis E, Sebti SM, Li R. Marinopyrrole derivatives with sulfide spacers as selective disruptors of Mcl-1 binding to pro-apoptotic protein Bim. Mar Drugs 2014 Aug; 12: (8) 4311-4325 PMID: 25076060. PMCID: PMC4145318. IF: 2.853

63. Olesen SH, Ingles DJ, Zhu JY, Martin MP, Betzi S, Georg GI, Tash JS, Schönbrunn E. Stability of the human Hsp90-p50Cdc37 chaperone complex against nucleotides and Hsp90 inhibitors, and the influence of phosphorylation by casein kinase 2. Molecules 2015 Oct; 20: (1) 1643-1660PMID: 25608045. PMCID: PMC4601640. IF: 2.416