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Page 1
Selective inhibition of mutant isocitrate dehydrogenase 1 (IDH1) via disruption of a metal binding network by an allosteric small molecule.
Deng G, Shen J, Yin M, McManus J, Mathieu M, Gee P, He T, Shi C, Bedel O, McLean LR, Le-Strat F, Zhang Y, Marquette JP, Gao Q, Zhang B, Rak A, Hoffmann D, Rooney E, Vassort A, Englaro W, Li Y, Patel V, Adrian F, Gross S, Wiederschain D, Cheng H, Licht S. Deng G, et al. Among authors: marquette jp. J Biol Chem. 2015 Jan 9;290(2):762-74. doi: 10.1074/jbc.M114.608497. Epub 2014 Nov 12. J Biol Chem. 2015. PMID: 25391653 Free PMC article.
Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
Certal V, Carry JC, Halley F, Virone-Oddos A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Karlsson A, Charrier V, Delorme C, Rak A, Abecassis PY, Amara C, Vincent L, Bonnevaux H, Nicolas JP, Mathieu M, Bertrand T, Marquette JP, Michot N, Benard T, Perrin MA, Lemaitre O, Guerif S, Perron S, Monget S, Gruss-Leleu F, Doerflinger G, Guizani H, Brollo M, Delbarre L, Bertin L, Richepin P, Loyau V, Garcia-Echeverria C, Lengauer C, Schio L. Certal V, et al. Among authors: marquette jp. J Med Chem. 2014 Feb 13;57(3):903-20. doi: 10.1021/jm401642q. Epub 2014 Jan 15. J Med Chem. 2014. PMID: 24387221
Discovery of (2S)-8-[(3R)-3-methylmorpholin-4-yl]-1-(3-methyl-2-oxobutyl)-2-(trifluoromethyl)-3,4-dihydro-2H-pyrimido[1,2-a]pyrimidin-6-one: a novel potent and selective inhibitor of Vps34 for the treatment of solid tumors.
Pasquier B, El-Ahmad Y, Filoche-Rommé B, Dureuil C, Fassy F, Abecassis PY, Mathieu M, Bertrand T, Benard T, Barrière C, El Batti S, Letallec JP, Sonnefraud V, Brollo M, Delbarre L, Loyau V, Pilorge F, Bertin L, Richepin P, Arigon J, Labrosse JR, Clément J, Durand F, Combet R, Perraut P, Leroy V, Gay F, Lefrançois D, Bretin F, Marquette JP, Michot N, Caron A, Castell C, Schio L, McCort G, Goulaouic H, Garcia-Echeverria C, Ronan B. Pasquier B, et al. Among authors: marquette jp. J Med Chem. 2015 Jan 8;58(1):376-400. doi: 10.1021/jm5013352. Epub 2014 Nov 26. J Med Chem. 2015. PMID: 25402320
Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
Certal V, Halley F, Virone-Oddos A, Delorme C, Karlsson A, Rak A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Carry JC, Abecassis PY, Lejeune P, Vincent L, Bonnevaux H, Nicolas JP, Bertrand T, Marquette JP, Michot N, Benard T, Below P, Vade I, Chatreaux F, Lebourg G, Pilorge F, Angouillant-Boniface O, Louboutin A, Lengauer C, Schio L. Certal V, et al. Among authors: marquette jp. J Med Chem. 2012 May 24;55(10):4788-805. doi: 10.1021/jm300241b. Epub 2012 May 2. J Med Chem. 2012. PMID: 22524426
A highly potent and selective Vps34 inhibitor alters vesicle trafficking and autophagy.
Ronan B, Flamand O, Vescovi L, Dureuil C, Durand L, Fassy F, Bachelot MF, Lamberton A, Mathieu M, Bertrand T, Marquette JP, El-Ahmad Y, Filoche-Romme B, Schio L, Garcia-Echeverria C, Goulaouic H, Pasquier B. Ronan B, et al. Among authors: marquette jp. Nat Chem Biol. 2014 Dec;10(12):1013-9. doi: 10.1038/nchembio.1681. Epub 2014 Oct 19. Nat Chem Biol. 2014. PMID: 25326666
Automated harvesting and processing of protein crystals through laser photoablation.
Zander U, Hoffmann G, Cornaciu I, Marquette JP, Papp G, Landret C, Seroul G, Sinoir J, Röwer M, Felisaz F, Rodriguez-Puente S, Mariaule V, Murphy P, Mathieu M, Cipriani F, Márquez JA. Zander U, et al. Among authors: marquette jp. Acta Crystallogr D Struct Biol. 2016 Apr;72(Pt 4):454-66. doi: 10.1107/S2059798316000954. Epub 2016 Mar 24. Acta Crystallogr D Struct Biol. 2016. PMID: 27050125 Free PMC article.
KRAS G12C fragment screening renders new binding pockets.
Mathieu M, Steier V, Fassy F, Delorme C, Papin D, Genet B, Duffieux F, Bertrand T, Delarbre L, Le-Borgne H, Parent A, Didier P, Marquette JP, Lowinski M, Houtmann J, Lamberton A, Debussche L, Alexey R. Mathieu M, et al. Among authors: marquette jp. Small GTPases. 2022 Jan;13(1):225-238. doi: 10.1080/21541248.2021.1979360. Epub 2021 Sep 24. Small GTPases. 2022. PMID: 34558391 Free PMC article.
15 results