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Structure-Guided Discovery of Potent and Selective DYRK1A Inhibitors.
Weber C, Sipos M, Paczal A, Balint B, Kun V, Foloppe N, Dokurno P, Massey AJ, Walmsley DL, Hubbard RE, Murray J, Benwell K, Edmonds T, Demarles D, Bruno A, Burbridge M, Cruzalegui F, Kotschy A. Weber C, et al. Among authors: kotschy a. J Med Chem. 2021 May 27;64(10):6745-6764. doi: 10.1021/acs.jmedchem.1c00023. Epub 2021 May 12. J Med Chem. 2021. PMID: 33975430
Fragment-Derived Selective Inhibitors of Dual-Specificity Kinases DYRK1A and DYRK1B.
Lee Walmsley D, Murray JB, Dokurno P, Massey AJ, Benwell K, Fiumana A, Foloppe N, Ray S, Smith J, Surgenor AE, Edmonds T, Demarles D, Burbridge M, Cruzalegui F, Kotschy A, Hubbard RE. Lee Walmsley D, et al. Among authors: kotschy a. J Med Chem. 2021 Jul 8;64(13):8971-8991. doi: 10.1021/acs.jmedchem.1c00024. Epub 2021 Jun 18. J Med Chem. 2021. PMID: 34143631 Free article.
The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models.
Kotschy A, Szlavik Z, Murray J, Davidson J, Maragno AL, Le Toumelin-Braizat G, Chanrion M, Kelly GL, Gong JN, Moujalled DM, Bruno A, Csekei M, Paczal A, Szabo ZB, Sipos S, Radics G, Proszenyak A, Balint B, Ondi L, Blasko G, Robertson A, Surgenor A, Dokurno P, Chen I, Matassova N, Smith J, Pedder C, Graham C, Studeny A, Lysiak-Auvity G, Girard AM, Gravé F, Segal D, Riffkin CD, Pomilio G, Galbraith LC, Aubrey BJ, Brennan MS, Herold MJ, Chang C, Guasconi G, Cauquil N, Melchiore F, Guigal-Stephan N, Lockhart B, Colland F, Hickman JA, Roberts AW, Huang DC, Wei AH, Strasser A, Lessene G, Geneste O. Kotschy A, et al. Nature. 2016 Oct 27;538(7626):477-482. doi: 10.1038/nature19830. Epub 2016 Oct 19. Nature. 2016. PMID: 27760111
Structure-Guided Discovery of a Selective Mcl-1 Inhibitor with Cellular Activity.
Szlávik Z, Ondi L, Csékei M, Paczal A, Szabó ZB, Radics G, Murray J, Davidson J, Chen I, Davis B, Hubbard RE, Pedder C, Dokurno P, Surgenor A, Smith J, Robertson A, LeToumelin-Braizat G, Cauquil N, Zarka M, Demarles D, Perron-Sierra F, Claperon A, Colland F, Geneste O, Kotschy A. Szlávik Z, et al. Among authors: kotschy a. J Med Chem. 2019 Aug 8;62(15):6913-6924. doi: 10.1021/acs.jmedchem.9b00134. Epub 2019 Jul 24. J Med Chem. 2019. PMID: 31339316
Discovery of S64315, a Potent and Selective Mcl-1 Inhibitor.
Szlavik Z, Csekei M, Paczal A, Szabo ZB, Sipos S, Radics G, Proszenyak A, Balint B, Murray J, Davidson J, Chen I, Dokurno P, Surgenor AE, Daniels ZM, Hubbard RE, Le Toumelin-Braizat G, Claperon A, Lysiak-Auvity G, Girard AM, Bruno A, Chanrion M, Colland F, Maragno AL, Demarles D, Geneste O, Kotschy A. Szlavik Z, et al. Among authors: kotschy a. J Med Chem. 2020 Nov 25;63(22):13762-13795. doi: 10.1021/acs.jmedchem.0c01234. Epub 2020 Nov 4. J Med Chem. 2020. PMID: 33146521
The Effect of Core Replacement on S64315, a Selective MCL-1 Inhibitor, and Its Analogues.
Sipos S, Bálint B, Szabó ZB, Ondi L, Csékei M, Szlávik Z, Proszenyák Á, Murray JB, Davidson J, Chen I, Dokurno P, Surgenor AE, Pedder C, Hubbard RE, Maragno AL, Chanrion M, Colland F, Geneste O, Kotschy A. Sipos S, et al. Among authors: kotschy a. ACS Omega. 2021 Aug 18;6(34):22073-22102. doi: 10.1021/acsomega.1c02595. eCollection 2021 Aug 31. ACS Omega. 2021. PMID: 34497901 Free PMC article.
41 results