Matthieu Schapira

Matthieu Schapira

SGC Toronto

Schapira

Matthieu Schapira

MaRS Centre, South Tower, 101 College St., Suite 700, Toronto, ON, M5G 1L7, Canada

Affiliations

Biography

Matthieu Schapira, PhD is a Professor in the Department of Pharmacology and Toxicology, UofT, and is the head of computational chemistry, protein bioinformatics, and data management at the SGC-Toronto. He leads the CACHE initiative for benchmarking computational ‘hit finding’. Dr. Schapira is a recognized authority in the structural chemistry of drug target classes such as chromatin regulators, ubiquitylation pathways and WDR proteins, and has created popular online informatics resources for these targets such as Chromohub, Ubihub and ChemBioPort. He is interested in novel strategies to expand and ML tools to exploit the accessible chemistry space. His trainees have gone on to become important innovators in AI-driven drug discovery at Toronto-born biotechs such as Atomwise and Cyclica.

Positions available

2013

Bromo-deaza-SAH: A potent and selective DOT1L inhibitor.

Yu W, Smil D, Li F, Tempel W, Fedorov O, Nguyen KT, Bolshan Y, Al-Awar R, Knapp S, Arrowsmith CH, Vedadi M, Brown PJ, Schapira M

Bioorg. Med. Chem.. 2013-4-1 . 21(7):1787-94 .doi: 10.1016/j.bmc.2013.01.049

PMID: 23433670

Synthesis, Optimization, and Evaluation of Novel Small Molecules as Antagonists of WDR5-MLL Interaction.

Bolshan Y, Getlik M, Kuznetsova E, Wasney GA, Hajian T, Poda G, Nguyen KT, Wu H, Dombrovski L, Dong A, Senisterra G, Schapira M, Arrowsmith CH, Brown PJ, Al-Awar R, Vedadi M, Smil D

ACS Med Chem Lett. 2013-3-14 . 4(3):353-7 .doi: 10.1021/ml300467n

PMID: 24900672

Exploiting an Allosteric Binding Site of PRMT3 Yields Potent and Selective Inhibitors.

Liu F, Li F, Ma A, Dobrovetsky E, Dong A, Gao C, Korboukh I, Liu J, Smil D, Brown PJ, Frye SV, Arrowsmith CH, Schapira M, Vedadi M, Jin J

J. Med. Chem.. 2013-3-14 . 56(5):2110-24 .doi: 10.1021/jm3018332

PMID: 23445220

Strategy to Target the Substrate Binding site of SET Domain Protein Methyltransferases.

Nguyen KT, Li F, Poda G, Smil D, Vedadi M, Schapira M

J Chem Inf Model. 2013-3-1 . .doi: 10.1021/ci300596x

PMID: 23410263

Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5.

Senisterra G, Wu H, Allali-Hassani A, Wasney GA, Barsyte-Lovejoy D, Dombrovski L, Dong A, Nguyen KT, Smil D, Bolshan Y, Hajian T, He H, Seitova A, Chau I, Li F, Poda G, Couture JF, Brown PJ, Al-Awar R, Schapira M, Arrowsmith CH, Vedadi M

Biochem. J.. 2013-1-1 . 449(1):151-9 .doi: 10.1042/BJ20121280

PMID: 22989411

2012

Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.

Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, Wienholds E, Li F, Pineda J, Estiu G, Shatseva T, Hajian T, Al-Awar R, Dick JE, Vedadi M, Brown PJ, Arrowsmith CH, Bradner JE, Schapira M

Nat Commun. 2012-12-18 . 3:1288 .doi: 10.1038/ncomms2304

PMID: 23250418

Sinefungin derivatives as inhibitors and structure probes of protein lysine methyltransferase SETD2.

Zheng W, Ibáñez G, Wu H, Blum G, Zeng H, Dong A, Li F, Hajian T, Allali-Hassani A, Amaya MF, Siarheyeva A, Yu W, Brown PJ, Schapira M, Vedadi M, Min J, Luo M

J. Am. Chem. Soc.. 2012-10-31 . 134(43):18004-14 .doi: 10.1021/ja307060p

PMID: 23043551

ChromoHub: a data hub for navigators of chromatin-mediated signalling.

Liu L, Zhen XT, Denton E, Marsden BD, Schapira M

Bioinformatics. 2012-8-15 . 28(16):2205-6 .doi: 10.1093/bioinformatics/bts340

PMID: 22718786

An allosteric inhibitor of protein arginine methyltransferase 3.

Siarheyeva A, Senisterra G, Allali-Hassani A, Dong A, Dobrovetsky E, Wasney GA, Chau I, Marcellus R, Hajian T, Liu F, Korboukh I, Smil D, Bolshan Y, Min J, Wu H, Zeng H, Loppnau P, Poda G, Griffin C, Aman A, Brown PJ, Jin J, Al-Awar R, Arrowsmith CH, Schapira M, Vedadi M

Structure. 2012-8-8 . 20(8):1425-35 .doi: 10.1016/j.str.2012.06.001

PMID: 22795084