monastyrskyi lab
monastyrskyi lab
Ghosh, P.; Schmitz, M.; Pandurangan, T.; Tadesse, S.; Chin Chan, S.; Mosior, J.; Luxin, S.; Palve, V.; Grassie, D.; Anand, K.; Frydman, S.; Roush, W.; Schönbrunn, E.; Geyer, M.; Duckett, D.; Monastyrskyi, A. Discovery and design of molecular glue enhancers of CDK12-DDB1 interactions for targeted degradation of CycK. RSC Chem. Biol., 2025, 6, 36–55.*
*selected as a front cover
Schmitz, M.; Kaltheuner, I. H.; Anand, K.; Duster, R.; Moecking, J.; Monastyrskyi, A.; Duckett, D.; Roush, W. R.; Geyer, M. The reversible inhibitor SR-4835 binds Cdk12/cyclin K in a noncanonical G-loop conformation. J Biol Chem 2024, 300 (1), 105501. PubMed PMID: 38016516; PMCID: PMC10767194.
Morozova, A.; Chan, S. C.; Bayle, S.; Sun, L.; Grassie, D.; Iermolaieva, A.; Kalaga, M. N.; Frydman, S.; Sansil, S.; Schönbrunn, E.; Duckett, D.; Monastyrskyi, A. Development of potent and selective ULK1/2 inhibitors based on 7-azaindole scaffold with favorable in vivo properties. Eur J Med Chem 2024, 266, 116101. PubMed PMID: 38232465.
Liao, Y.; Remsing Rix, L. L.; Li, X.; Fang, B.; Izumi, V.; Welsh, E. A.; Monastyrskyi, A.; Haura, E. B.; Koomen, J. M.; Doebele, R. C.; Rix, U.Differential network analysis of ROS1 inhibitors reveals lorlatinib polypharmacology through co-targeting PYK2. Cell Chem Biol 2024, 31 (2), 284-297 e210. PubMed PMID: 37848034; PMCID: PMC10922442.
Pedzisa, L.; Monastyrskyi, A.; Parker, C. D.; Roush, W. R. Enantio- and diastereoselective (Ipc) BOTf-mediated aldol reactions of morpholine carboxamides. Helv Chim Acta 2023, 106 (12) .PubMed PMID: WOS:001104700800001.
Nacheva, K.; Kulkarni, S. S.; Kassu, M.; Flanigan, D.; Monastyrskyi, A.; Iyamu, I. D.; Doi, K.; Barber, M.; Namelikonda, N.; Tipton, J. D.; Parvatkar, P.; Wang, H. G.; Manetsch, R. Going beyond binary: rapid identification of protein-protein interaction modulators using a multifragment kinetic target-guided synthesis approach. J Med Chem 2023, 66 (7), 5196-5207. PubMed PMID: 37000900; PMCID: PMC10620989.
Liao, Y.; Chin Chan, S.; Welsh, E. A.; Fang, B.; Sun, L.; Schönbrunn, E.; Koomen, J. M.; Duckett, D. R.; Haura, E. B.; Monastyrskyi, A.; Rix, U. Chemical Proteomics with Novel Fully Functionalized Fragments and Stringent Target Prioritization Identifies the Glutathione-Dependent Isomerase GSTZ1 as a Lung Cancer Target. ACS Chem Biol 2023, 18 (2), 251-264. PubMed PMID: 36630201.
Burger, K. L.; Fernandez, M. R.; Meads, M. B.; Sudalagunta, P.; Oliveira, P. S.; Renatino Canevarolo, R.; Alugubelli, R. R.; Tungsevik, A.; De Avila, G.; Silva, M.; Graeter, A. I.; Dai, H. A.; Vincelette, N. D.; Prabhu, A.; Magaletti, D.; Yang, C.; Li, W.; Kulkarni, A.; Hampton, O.; Koomen, J. M.; Roush, W. R.; Monastyrskyi, A.; Berglund, A. E.; Silva, A. S.; Cleveland, J. L.; Shain, K. H. CK1delta and CK1epsilon signaling sustains mitochondrial metabolism and cell survival in multiple myeloma. Cancer Res 2023, 83 (23), 3901-3919.PubMed PMID: 37702657; PMCID: PMC10690099.
Tadesse, S.; Duckett, D. R.; Monastyrskyi, A. The promise and current status of CDK12/13 inhibition for the treatment of cancer (Review). Future Med Chem 2021, 13 (2), 117-141. PubMed PMID: 33295810.
Monastyrskyi, A.; Brockmeyer, F.; LaCrue, A. N.; Zhao, Y.; Maher, S. P.; Maignan, J. R.; Padin-Irizarry, V.; Sakhno, Y. I.; Parvatkar, P. T.; Asakawa, A. H.; Huang, L.; Casandra, D.; Mashkouri, S.; Kyle, D. E.; Manetsch, R. Aminoalkoxycarbonyloxymethyl ether prodrugs with a pH-triggered release mechanism: a case study improving the solubility, bioavailability, and efficacy of antimalarial 4(1H)-quinolones with single dose cures. J Med Chem 2021, 64 (10), 6581-6595. PubMed PMID: 33979164; PMCID: PMC8904075.
Vena, F.; Bayle, S.; Nieto, A.; Quereda, V.; Aceti, M.; Frydman, S. M.; Sansil, S. S.; Grant, W.; Monastyrskyi, A.; McDonald, P.; Roush, W. R.; Teng, M.; Duckett, D*. Targeting casein kinase 1 delta sensitizes pancreatic and bladder cancer cells to gemcitabine treatment by upregulating deoxycytidine Kinase. Mol Cancer Ther 2020, 19 (8), 1623-1635. PubMed PMID: 32430484; PMCID: PMC7415672.
Maharaj, K.; Powers, J. J.; Achille, A.; Mediavilla-Varela, M.; Gamal, W.; Burger, K. L.; Fonseca, R.; Jiang, K.; Miskin, H. P.; Maryanski, D.; Monastyrskyi, A.; Duckett, D. R.; Roush, W. R.; Cleveland, J. L.; Sahakian, E.; Pinilla-Ibarz, J. The dual PI3Kdelta/CK1epsilon inhibitor umbralisib exhibits unique immunomodulatory effects on CLL T cells. Blood Adv 2020, 4 (13), 3072-3084. PubMed PMID: 32634240; PMCID: PMC7362385.
Quereda, V.; Bayle, S.; Vena, F.; Frydman, S. M.; Monastyrskyi, A.; Roush, W. R.; Duckett, D. Therapeutic targeting of CDK12/CDK13 in triple-negative breast cancer. Cancer Cell 2019, 36 (5), 545-558 e547. PubMed PMID: 31668947.
“Thiophenes and related heterocycles” in Progress in Heterocyclic Chemistry by Sean Chin Chan and Andrii Monastyrskyi, Elsevier, 2024.
Monastyrskyi, A.; Bayle, S.; Quereda, V.; Grant, W.; Cameron, M.D.; Duckett, D.R.; Roush, W.R. Discovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors. Bioorganic and Medicinal Chemistry Letters, 2018, 28, 400-404.
Monastyrskyi, A.; Nilchan, N.; Quereda, V.; Noguchi, Y.; Ruiz, C.; Grant, W.; Cameron, M.D.; Duckett, D.R.; Roush, W.R. Development of Dual Casein Kinase 1δ/1ε (CK1δ/ε) Inhibitors for Treatment of Breast Cancer, Bioorganic and Medicinal Chemistry, 2018, 26, 590-602.
Neelarapu, R.; Maignan, J.R.; Lichorowic, C.L.; Monastyrskyi, A.; LaCrue, A.N.; Mutka, T.S.; Blake, L.D.; Casandra, D.; Mashkouri, S.; Burrows, J.B.; Willis, P.A.; Kyle, D.E.; Manetsch, R. Design and synthesis of orally bioavailable piperazine substituted 4(1H)-quinolones with potent antimalarial activity: structure-activity and structure-property relationship studies, Journal of Medicinal Chemistry, 2017,61 (4), 1450-1473.
Namelikonda, N.K.; Monastyrskyi, A.; Manetsch, R. Gram scale synthesis of antimalarial 4(1H)-quinolones ELQ-300 and P4Q-391. European Journal of Organic Chemistry, 2017, 23, 3328-3334.
Monastyrskyi, A.; Namelikonda, N.K.; Manetsch, R. Metal-free arylation of ethyl acetoacetate with hypervalent diaryliodonium salts: an immediate access to diverse 3‑aryl-4(1H)‑quinolones. Journal of Organic Chemistry 2015, 80, 2513−2520.
Cross, R.M.; Flanigan, D.L.; Monastyrskyi, A.; LaCrue, A.N.; Maignan, J.M.; Mutka, T. S.; Guida, C.W.; White, K.L., Charman, S.A., Burrows, J.N.; Kyle, D. E.; Manetsch, R. Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium. Journal of Medicinal Chemistry 2014, 57 (21), 8860–8879.
Monastyrskyi, A.; Kyle, D. E.; Manetsch, R. 4(1H)-Pyridone and 4(1H)-quinolone derivatives as antimalarials with erythrocytic, exoerythrocytic, and transmission blocking activities. Current Topics in Medicinal Chemistry, 2014, 14, 1693-1705.
LaCrue, A. N.; Saenz, F. E.; Cross, R. M.; Udenze, K. O.; Monastyrskyi, A.; Stein, S.; Mutka, T. S.; Manetsch, R.; Kyle, D. E. 4(1H)-Quinolones with liver stage activity against Plasmodium berghei. Antimicrobial Agents and Chemotherapy, 2013, 57, 417-24.
Cross, R. M.; Monastyrskyi, A.; Mutka, T. S.; Burrows, J. N.; Kyle, D. E.; Manetsch, R. Endochin optimization: structure-activity and structure-property relationship studies of 3-substituted 2-methyl-4(1H)-quinolones with antimalarial activity. Journal of Medicinal Chemistry, 2010, 53, 7076-94.