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Andrii Monastyrskyi, PhD

Academic Rank: Assistant Member

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Overview

    The Monastyrskyi lab harnesses the power of organic chemistry and chemical biology to develop new tools for studying the function and therapeutic potential of cancer targets.          


Discipline

    • Drug Discovery
    • Breast Oncology
    • Neuro-Oncology
    • Chemical Biology and Molecular Medicine Program

Education & Training

Fellowship:

  • University of South Florida, PhD - Organic Chemistry
  • The Scripps Research Institute, Fellow - Chemistry
Research

  Our laboratory uses the tools of synthetic organic chemistry, medicinal chemistry, and chemical biology to further develop small molecules for studying and modulating therapeutically relevant cancer targets. One aspect of current work focuses on the development of IND safety assessment candidates that inhibit the transcriptional kinases CDK12 and CDK13, the Wnt/beta-catenin regulators CK1d and CK1e, and the autophagy kinase ULK1. Further, developmental projects in the laboratory include campaigns to develop small molecules that disrupt key protein-protein interactions (e.g., those of Myc and Max) and RNA biogenesis.    

Publications

  • Quereda V, Bayle S, Vena F, Frydman SM, Monastyrskyi A, Roush WR, Duckett DR. Therapeutic Targeting of CDK12/CDK13 in Triple-Negative Breast Cancer. Cancer Cell. 2019 Oct.36(5):545-558.e7. Pubmedid: 31668947.
  • Monastyrskyi A, Nilchan N, Quereda V, Noguchi Y, Ruiz C, Grant W, Cameron M, Duckett D, Roush W. Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer. Bioorg Med Chem. 2018 Feb;26(3):590-602. Pubmedid: 29289448. Pmcid: PMC5803353.
  • Monastyrskyi A, Bayle S, Quereda V, Grant W, Cameron M, Duckett D, Roush W. Discovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors. Bioorg Med Chem Lett. 2018 Feb;28(3):400-404. Pubmedid: 29277458. Pmcid: PMC5999544.
  • Neelarapu R, Maignan JR, Lichorowic CL, Monastyrskyi A, Mutka TS, LaCrue AN, Blake LD, Casandra D, Mashkouri S, Burrows JN, Willis PA, Kyle DE, Manetsch R. Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure-Activity and Structure-Property Relationship Studies. J Med Chem. 2018 Feb;61(4):1450-1473. Pubmedid: 29215279. Pmcid: PMC6610884.
  • Monastyrskyi A, Namelikonda NK, Manetsch R. Metal-free arylation of ethyl acetoacetate with hypervalent diaryliodonium salts: an immediate access to diverse 3-aryl-4(1H)-quinolones. J Org Chem. 2015 Mar;80(5):2513-2520. Pubmedid: 25558982. Pmcid: PMC4479256.
  • Monastyrskyi A, Kyle DE, Manetsch R. 4(1H)-pyridone and 4(1H)-quinolone derivatives as antimalarials with erythrocytic, exoerythrocytic, and transmission blocking activities. Curr Top Med Chem. 2014 Sep;14(14):1693-1705. Pubmedid: 25116582. Pmcid: PMC4479281.
  • Cross RM, Flanigan DL, Monastyrskyi A, LaCrue AN, Sáenz FE, Maignan JR, Mutka TS, White KL, Shackleford DM, Bathurst I, Fronczek FR, Wojtas L, Guida WC, Charman SA, Burrows JN, Kyle DE, Manetsch R. Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium. J Med Chem. 2014 Nov;57(21):8860-8879. Pubmedid: 25148516. Pmcid: PMC4234439.
  • Lacrue AN, Sáenz FE, Cross RM, Udenze KO, Monastyrskyi A, Stein S, Mutka TS, Manetsch R, Kyle DE. 4(1H)-Quinolones with liver stage activity against Plasmodium berghei. Antimicrob Agents Chemother. 2013 Jan;57(1):417-424. Pubmedid: 23129047. Pmcid: PMC3535941.
  • Cross RM, Monastyrskyi A, Mutka TS, Burrows JN, Kyle DE, Manetsch R. Endochin optimization: structure-activity and structure-property relationship studies of 3-substituted 2-methyl-4(1H)-quinolones with antimalarial activity. J Med Chem. 2010 Oct;53(19):7076-7094. Pubmedid: 20828199.