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S55746 is a novel orally active BCL-2 selective and potent inhibitor that impairs hematological tumor growth.
Casara P, Davidson J, Claperon A, Le Toumelin-Braizat G, Vogler M, Bruno A, Chanrion M, Lysiak-Auvity G, Le Diguarher T, Starck JB, Chen I, Whitehead N, Graham C, Matassova N, Dokurno P, Pedder C, Wang Y, Qiu S, Girard AM, Schneider E, Gravé F, Studeny A, Guasconi G, Rocchetti F, Maïga S, Henlin JM, Colland F, Kraus-Berthier L, Le Gouill S, Dyer MJS, Hubbard R, Wood M, Amiot M, Cohen GM, Hickman JA, Morris E, Murray J, Geneste O. Casara P, et al. Oncotarget. 2018 Apr 13;9(28):20075-20088. doi: 10.18632/oncotarget.24744. eCollection 2018 Apr 13. Oncotarget. 2018. PMID: 29732004 Free PMC article.
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: casara p. 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.
Bax activation by engagement with, then release from, the BH3 binding site of Bcl-xL.
Gautier F, Guillemin Y, Cartron PF, Gallenne T, Cauquil N, Le Diguarher T, Casara P, Vallette FM, Manon S, Hickman JA, Geneste O, Juin P. Gautier F, et al. Among authors: casara p. Mol Cell Biol. 2011 Feb;31(4):832-44. doi: 10.1128/MCB.00161-10. Epub 2010 Dec 20. Mol Cell Biol. 2011. PMID: 21173168 Free PMC article.
Characterization of novel checkpoint kinase 1 inhibitors by in vitro assays and in human cancer cells treated with topoisomerase inhibitors.
Ferry G, Studeny A, Bossard C, Kubara PM, Zeyer D, Renaud JP, Casara P, de Nanteuil G, Wierzbicki M, Pfeiffer B, Prudhomme M, Leonce S, Pierré A, Boutin JA, Golsteyn RM. Ferry G, et al. Among authors: casara p. Life Sci. 2011 Aug 15;89(7-8):259-68. doi: 10.1016/j.lfs.2011.06.010. Epub 2011 Jun 29. Life Sci. 2011. PMID: 21736880
40 results