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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
Structure-Activity Relationship of Azaindole-Based Glucokinase Activators.
Paczal A, Bálint B, Wéber C, Szabó ZB, Ondi L, Theret I, De Ceuninck F, Bernard C, Ktorza A, Perron-Sierra F, Kotschy A. Paczal A, et al. Among authors: kotschy a. J Med Chem. 2016 Jan 28;59(2):687-706. doi: 10.1021/acs.jmedchem.5b01594. Epub 2016 Jan 15. J Med Chem. 2016. PMID: 26685731
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
Establishing Drug Discovery and Identification of Hit Series for the Anti-apoptotic Proteins, Bcl-2 and Mcl-1.
Murray JB, Davidson J, Chen I, Davis B, Dokurno P, Graham CJ, Harris R, Jordan A, Matassova N, Pedder C, Ray S, Roughley SD, Smith J, Walmsley C, Wang Y, Whitehead N, Williamson DS, Casara P, Le Diguarher T, Hickman J, Stark J, Kotschy A, Geneste O, Hubbard RE. Murray JB, et al. Among authors: kotschy a. ACS Omega. 2019 May 23;4(5):8892-8906. doi: 10.1021/acsomega.9b00611. eCollection 2019 May 31. ACS Omega. 2019. PMID: 31459977 Free PMC article.
Aromatic Foldamer Helices as α-Helix Extended Surface Mimetics.
Zwillinger M, Reddy PS, Wicher B, Mandal PK, Csékei M, Fischer L, Kotschy A, Huc I. Zwillinger M, et al. Among authors: kotschy a. Chemistry. 2020 Dec 23;26(72):17366-17370. doi: 10.1002/chem.202004064. Epub 2020 Nov 30. Chemistry. 2020. PMID: 32910480 Free PMC article.
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
41 results