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

2016

Discovery of a Potent, Selective and Cell-active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.

Shen Y, Szewczyk MM, Eram MS, Smil D, Kaniskan HÜ, de Freitas RF, Senisterra G, Li F, Schapira M, Brown PJ, Arrowsmith CH, Barsyte-Lovejoy D, Liu J, Vedadi M, Jin J

J. Med. Chem.. 2016-9-1 . .doi: 10.1021/acs.jmedchem.6b01033

PMID: 27584694

New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms.

Spurr SS, Bayle ED, Yu W, Li F, Tempel W, Vedadi M, Schapira M, Fish PV

Bioorg. Med. Chem. Lett.. 2016-7-21 . .doi: 10.1016/j.bmcl.2016.07.041

PMID: 27485386

Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening.

Ferreira de Freitas R, Eram MS, Smil D, Szewczyk MM, Kennedy S, Brown PJ, Santhakumar V, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M, Schapira M

J. Med. Chem.. 2016-7-8 . .doi: 10.1021/acs.jmedchem.6b00668

PMID: 27390919

Methyltransferase inhibitors for modulation of the epigenome and beyond.

Schapira M, Arrowsmith CH

Curr Opin Chem Biol. 2016-6-16 . 33:81-87 .doi: 10.1016/j.cbpa.2016.05.030

PMID: 27318562

An Integrative Proteomic Approach Identifies Novel Cellular SMYD2 Substrates.

Ahmed H, Duan S, Arrowsmith CH, Barsyte-Lovejoy D, Schapira M

J. Proteome Res.. 2016-5-10 . .doi: 10.1021/acs.jproteome.6b00220

PMID: 27163177

PR Domain-Containing Protein 7 (PRDM7) is a Histone 3 Lysine 4 Trimethyltransferase.

Blazer LL, Lima-Fernandes E, Gibson E, Eram MS, Loppnau P, Arrowsmith CH, Schapira M, Vedadi M

J. Biol. Chem.. 2016-4-29 . .doi: 10.1074/jbc.M116.721472

PMID: 27129774

Identification of small molecule inhibitors that block the Toxoplasma gondii rhoptry kinase ROP18.

Simpson C, Jones NG, Hull-Ryde EA, Kireev D, Stashko M, Tang K, Janetka J, Wildman SA, Zuercher WJ, Schapira M, Hui R, Janzen W, Sibley LD

ACS Infect Dis. 2016-3-11 . 2(3):194-206 .doi: 10.1021/acsinfecdis.5b00102

PMID: 27379343

Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1).

Getlik M, Smil D, Zepeda-Velázquez C, Bolshan Y, Poda G, Wu H, Dong A, Kuznetsova E, Marcellus R, Senisterra G, Dombrovski L, Hajian T, Kiyota T, Schapira M, Arrowsmith CH, Brown PJ, Vedadi M, Al-Awar R

J. Med. Chem.. 2016-3-9 . .doi: 10.1021/acs.jmedchem.5b01630

PMID: 26958703

Discovery of a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor.

Ferreira de Freitas R, Eram MS, Szewczyk MM, Steuber H, Smil D, Wu H, Li F, Senisterra G, Dong A, Brown PJ, Hitchcock M, Moosmayer D, Stegmann CM, Egner U, Arrowsmith C, Barsyte-Lovejoy D, Vedadi M, Schapira M

J. Med. Chem.. 2016-1-29 . .doi: 10.1021/acs.jmedchem.5b01772

PMID: 26824386