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Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7.
Marineau JJ, Hamman KB, Hu S, Alnemy S, Mihalich J, Kabro A, Whitmore KM, Winter DK, Roy S, Ciblat S, Ke N, Savinainen A, Wilsily A, Malojcic G, Zahler R, Schmidt D, Bradley MJ, Waters NJ, Chuaqui C. Marineau JJ, et al. Among authors: malojcic g. J Med Chem. 2022 Jan 27;65(2):1458-1480. doi: 10.1021/acs.jmedchem.1c01171. Epub 2021 Nov 2. J Med Chem. 2022. PMID: 34726887 Free article.
Selective inhibition of CDK7 reveals high-confidence targets and new models for TFIIH function in transcription.
Rimel JK, Poss ZC, Erickson B, Maas ZL, Ebmeier CC, Johnson JL, Decker TM, Yaron TM, Bradley MJ, Hamman KB, Hu S, Malojcic G, Marineau JJ, White PW, Brault M, Tao L, DeRoy P, Clavette C, Nayak S, Damon LJ, Kaltheuner IH, Bunch H, Cantley LC, Geyer M, Iwasa J, Dowell RD, Bentley DL, Old WM, Taatjes DJ. Rimel JK, et al. Among authors: malojcic g. Genes Dev. 2020 Nov 1;34(21-22):1452-1473. doi: 10.1101/gad.341545.120. Epub 2020 Oct 15. Genes Dev. 2020. PMID: 33060135 Free PMC article.
Discovery and Optimization of Highly Selective Inhibitors of CDK5.
Daniels MH, Malojcic G, Clugston SL, Williams B, Coeffet-Le Gal M, Pan-Zhou XR, Venkatachalan S, Harmange JC, Ledeboer M. Daniels MH, et al. Among authors: malojcic g. J Med Chem. 2022 Feb 24;65(4):3575-3596. doi: 10.1021/acs.jmedchem.1c02069. Epub 2022 Feb 10. J Med Chem. 2022. PMID: 35143203
Discovery of a Potent and Selective TRPC5 Inhibitor, Efficacious in a Focal Segmental Glomerulosclerosis Model.
Yu M, Ledeboer MW, Daniels M, Malojcic G, Tibbitts TT, Coeffet-Le Gal M, Pan-Zhou XR, Westerling-Bui A, Beconi M, Reilly JF, Mundel P, Harmange JC. Yu M, et al. Among authors: malojcic g. ACS Med Chem Lett. 2019 Oct 22;10(11):1579-1585. doi: 10.1021/acsmedchemlett.9b00430. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749913 Free PMC article.
Transplanted organoids empower human preclinical assessment of drug candidate for the clinic.
Westerling-Bui AD, Fast EM, Soare TW, Venkatachalan S, DeRan M, Fanelli AB, Kyrychenko S, Hoang H, Corriea GM, Zhang W, Yu M, Daniels M, Malojcic G, Pan-Zhou XR, Ledeboer MW, Harmange JC, Emani M, Tibbitts TT, Reilly JF, Mundel P. Westerling-Bui AD, et al. Among authors: malojcic g. Sci Adv. 2022 Jul 8;8(27):eabj5633. doi: 10.1126/sciadv.abj5633. Epub 2022 Jul 6. Sci Adv. 2022. PMID: 35857479 Free PMC article.
Structural basis of TRPC4 regulation by calmodulin and pharmacological agents.
Vinayagam D, Quentin D, Yu-Strzelczyk J, Sitsel O, Merino F, Stabrin M, Hofnagel O, Yu M, Ledeboer MW, Nagel G, Malojcic G, Raunser S. Vinayagam D, et al. Among authors: malojcic g. Elife. 2020 Nov 25;9:e60603. doi: 10.7554/eLife.60603. Elife. 2020. PMID: 33236980 Free PMC article.
17 results