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Page 1
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. Among authors: geneste o. Nature. 2016 Oct 27;538(7626):477-482. doi: 10.1038/nature19830. Epub 2016 Oct 19. Nature. 2016. PMID: 27760111
Synergistic action of the MCL-1 inhibitor S63845 with current therapies in preclinical models of triple-negative and HER2-amplified breast cancer.
Merino D, Whittle JR, Vaillant F, Serrano A, Gong JN, Giner G, Maragno AL, Chanrion M, Schneider E, Pal B, Li X, Dewson G, Gräsel J, Liu K, Lalaoui N, Segal D, Herold MJ, Huang DCS, Smyth GK, Geneste O, Lessene G, Visvader JE, Lindeman GJ. Merino D, et al. Among authors: geneste o. Sci Transl Med. 2017 Aug 2;9(401):eaam7049. doi: 10.1126/scitranslmed.aam7049. Sci Transl Med. 2017. PMID: 28768804
Combining BH3-mimetics to target both BCL-2 and MCL1 has potent activity in pre-clinical models of acute myeloid leukemia.
Moujalled DM, Pomilio G, Ghiurau C, Ivey A, Salmon J, Rijal S, Macraild S, Zhang L, Teh TC, Tiong IS, Lan P, Chanrion M, Claperon A, Rocchetti F, Zichi A, Kraus-Berthier L, Wang Y, Halilovic E, Morris E, Colland F, Segal D, Huang D, Roberts AW, Maragno AL, Lessene G, Geneste O, Wei AH. Moujalled DM, et al. Among authors: geneste o. Leukemia. 2019 Apr;33(4):905-917. doi: 10.1038/s41375-018-0261-3. Epub 2018 Sep 10. Leukemia. 2019. PMID: 30214012 Free PMC article.
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: geneste o. 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: geneste o. 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
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. Among authors: geneste o. Oncotarget. 2018 Apr 13;9(28):20075-20088. doi: 10.18632/oncotarget.24744. eCollection 2018 Apr 13. Oncotarget. 2018. PMID: 29732004 Free PMC article.
Cotargeting BCL-2 and MCL-1 in high-risk B-ALL.
Moujalled DM, Hanna DT, Hediyeh-Zadeh S, Pomilio G, Brown L, Litalien V, Bartolo R, Fleming S, Chanrion M, Banquet S, Maragno AL, Kraus-Berthier L, Schoumacher M, Mullighan CG, Georgiou A, White CA, Lessene G, Huang DCS, Roberts AW, Geneste O, Rasmussen L, Davis MJ, Ekert PG, Wei A, Ng AP, Khaw SL. Moujalled DM, et al. Among authors: geneste o. Blood Adv. 2020 Jun 23;4(12):2762-2767. doi: 10.1182/bloodadvances.2019001416. Blood Adv. 2020. PMID: 32569380 Free PMC article.
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: geneste o. 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.
[The Bcl-2 family of proteins as drug targets].
Mazars A, Geneste O, Hickman J. Mazars A, et al. Among authors: geneste o. J Soc Biol. 2005;199(3):253-65. doi: 10.1051/jbio:2005027. J Soc Biol. 2005. PMID: 16471266 Review. French.
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: geneste o. 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.
40 results