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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: colland f. 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.
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: colland f. Nature. 2016 Oct 27;538(7626):477-482. doi: 10.1038/nature19830. Epub 2016 Oct 19. Nature. 2016. PMID: 27760111
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: colland f. Oncotarget. 2018 Apr 13;9(28):20075-20088. doi: 10.18632/oncotarget.24744. eCollection 2018 Apr 13. Oncotarget. 2018. PMID: 29732004 Free PMC article.
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: colland f. 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-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: colland f. 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
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: colland f. 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.
Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells.
Colland F, Formstecher E, Jacq X, Reverdy C, Planquette C, Conrath S, Trouplin V, Bianchi J, Aushev VN, Camonis J, Calabrese A, Borg-Capra C, Sippl W, Collura V, Boissy G, Rain JC, Guedat P, Delansorne R, Daviet L. Colland F, et al. Mol Cancer Ther. 2009 Aug;8(8):2286-95. doi: 10.1158/1535-7163.MCT-09-0097. Epub 2009 Aug 11. Mol Cancer Ther. 2009. PMID: 19671755
STAT2 is an essential adaptor in USP18-mediated suppression of type I interferon signaling.
Arimoto KI, Löchte S, Stoner SA, Burkart C, Zhang Y, Miyauchi S, Wilmes S, Fan JB, Heinisch JJ, Li Z, Yan M, Pellegrini S, Colland F, Piehler J, Zhang DE. Arimoto KI, et al. Among authors: colland f. Nat Struct Mol Biol. 2017 Mar;24(3):279-289. doi: 10.1038/nsmb.3378. Epub 2017 Feb 6. Nat Struct Mol Biol. 2017. PMID: 28165510 Free PMC article.
Histone acetyltransferase inhibitors block neuroblastoma cell growth in vivo.
Gajer JM, Furdas SD, Gründer A, Gothwal M, Heinicke U, Keller K, Colland F, Fulda S, Pahl HL, Fichtner I, Sippl W, Jung M. Gajer JM, et al. Among authors: colland f. Oncogenesis. 2015 Feb 9;4(2):e137. doi: 10.1038/oncsis.2014.51. Oncogenesis. 2015. PMID: 25664930 Free PMC article.
38 results