Faculty: Matthieu Schapira, PhD
Matthieu Schapira, PhD
Associate Professor
General Research Area: Computational Chemistry.
Matthieu holds a M.Sc degree in chemistry from the National Superior Chemistry School, Nancy, France, and a Ph.D in biochemistry from Ecole Normale Superieure, Paris. After graduating in 1995, he completed a couple post-docs in protein crystallography and computational chemistry at New York University Medical Center. In 2000, he joined Molsoft, a San-Diego based biotech, as senior research scientist. In 2003, he moved to Lyon, France, to lead structure-based drug design at Aptanomics/Imaxio, a drug discovery start-up. In 2007, he joined the SGC (Structural Genomics Consortium) as head of research informatics. Matthieu holds an Associate Professor cross-appointment with the Department of Pharmacology and Toxicology at University of Toronto, and an adjunct Associate Professor position with the Department of Pharmacology at New York University.
SGC Toronto’s Research Informatics group has three distinct roles. (1) Research: we apply computational chemistry tools to analyze protein structures and support the development of chemical inhibitors. We also analyze cancer genomics data. (2) Tools: we develop web interfaces, such as Chromohub, to easily navigate structural, chemical and genomic data. (3) Databases: we manage the wealth of biological and chemical data generated at SGC-Toronto.
Selected Publications:
Open laboratory notebooks: good for science, good for society, good for scientists
Schapira M, The Open Lab Notebook Consortium, Harding R
F1000Research. 2019 . doi: 10.12688/f1000research.17710.1
Identification and Structure-Activity Relationship of HDAC6 Zinc-Finger Ubiquitin Binding Domain Inhibitors.
Ferreira de Freitas R, Harding RJ, Franzoni I, Ravichandran M, Mann MK, Ouyang H, Lautens M, Santhakumar V, Arrowsmith CH, Schapira M
J. Med. Chem. 2018. doi: 10.1021/acs.jmedchem.8b00258
PMID: 29741882
WD40 repeat domain proteins: a novel target class?
Schapira M, Tyers M, Torrent M, Arrowsmith CH
Nat Rev Drug Discov. 2017 . doi: 10.1038/nrd.2017.179
PMID: 29026209
Disease Association and Druggability of WD40 Repeat Proteins.
Song R, Wang ZD, Schapira M
J. Proteome Res.. 2017 . doi: 10.1021/acs.jproteome.7b00451
PMID: 28956604
Chemical Inhibition of Protein Methyltransferases.
Schapira M
Cell Chem Biol. 2016 . doi: 10.1016/j.chembiol.2016.07.014
PMID: 27569753
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. doi: 10.1021/acs.jmedchem.6b00668
PMID: 27390919
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. doi: 10.1021/acs.jmedchem.5b01772
PMID: 26824386
Probing the epigenome.
Huston A, Arrowsmith CH, Knapp S, Schapira M
Nat. Chem. Biol. 2015. 11(8):542-5. doi: 10.1038/nchembio.1871
PMID: 26196765
Discovery of a Dual PRMT5-PRMT7 Inhibitor.
Smil D, Eram MS, Li F, Kennedy S, Szewczyk MM, Brown PJ, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M, Schapira M
ACS Med Chem Lett. 2015 6(4):408-12. doi: 10.1021/ml500467h
PMID: 25893041
Structural Chemistry of Human RNA Methyltransferases.
Schapira M
ACS Chem. Biol. 2015. doi: 10.1021/acschembio.5b00781
PMID: 26566070
STRUCTURAL BIOLOGY. Chromatin complex, crystal clear.
Schapira M
Science. 2015 350(6258):278-9. doi: 10.1126/science.aad5203
PMID: 26472895
Structural diversity of the epigenetics pocketome.
Cabaye A, Nguyen KT, Liu L, Pande V, Schapira M
Proteins. 2015 . doi: 10.1002/prot.24830
PMID: 25974248
Structural biology and chemistry of protein arginine methyltransferases.
Schapira M, Ferreira de Freitas R
Medchemcomm. 2014 5(12):1779-1788. doi: 10.1039/c4md00269e
PMID: 26693001
A global assessment of cancer genomic alterations in epigenetic mechanisms.
Shah MA, Denton EL, Arrowsmith CH, Lupien M, Schapira M
Epigenetics Chromatin. 2014 7(1):29. doi: 10.1186/1756-8935-7-29
PMID: 25484917
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 . doi: 10.1021/ci300596x
PMID: 23410263
ChromoHub V2: Cancer Genomics.
Shah MA, Denton EL, Liu L, Schapira M
Bioinformatics. 2013 . doi: 10.1093/bioinformatics/btt710
PMID: 24319001
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 21(7):1787-94. doi: 10.1016/j.bmc.2013.01.049
PMID: 23433670
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 3:1288. doi: 10.1038/ncomms2304
PMID: 23250418
Epigenetic protein families: a new frontier for drug discovery.
Arrowsmith CH, Bountra C, Fish PV, Lee K, Schapira M
Nat Rev Drug Discov. 2012 11(5):384-400. doi: 10.1038/nrd3674
PMID: 22498752
ChromoHub: a data hub for navigators of chromatin-mediated signalling.
Liu L, Zhen XT, Denton E, Marsden BD, Schapira M
Bioinformatics. 2012 28(16):2205-6. doi: 10.1093/bioinformatics/bts340
PMID: 22718786
Druggability of methyl-lysine binding sites.
Santiago C, Nguyen K, Schapira M
J. Comput. Aided Mol. Des.. 2011 25(12):1171-8. doi: 10.1007/s10822-011-9505-2
PMID: 22146969
Structural biology of human metal-dependent histone deacetylases.
Schapira M
Handb Exp Pharmacol. 2011 206:225-40. doi: 10.1007/978-3-642-21631-2_10
PMID: 21879452
Structural Chemistry of Human SET Domain Protein Methyltransferases.
Schapira M
Curr Chem Genomics. 2011 5(Suppl 1):85-94. doi: 10.2174/1875397301005010085
PMID: 21966348
Structural chemistry of the histone methyltransferases cofactor binding site.
Campagna-Slater V, Mok MW, Nguyen KT, Feher M, Najmanovich R, Schapira M
J Chem Inf Model. 2011 51(3):612-23. doi: 10.1021/ci100479z
PMID: 21366357
Structural genomics of histone tail recognition.
Wang M, Mok MW, Harper H, Lee WH, Min J, Knapp S, Oppermann U, Marsden B, Schapira M
Bioinformatics. 2010 26(20):2629-30. doi: 10.1093/bioinformatics/btq491
PMID: 20739309
Finding Inspiration in the Protein Data Bank to Chemically Antagonize Readers of the Histone Code.
Campagna-Slater V, Schapira M
Mol Inform. 2010 29(4):322-31. doi: 10.1002/minf.201000018
PMID: 27463059
Pharmacophore screening of the protein data bank for specific binding site chemistry.
Campagna-Slater V, Arrowsmith AG, Zhao Y, Schapira M
J Chem Inf Model. 2010 50(3):358-67. doi: 10.1021/ci900427b
PMID: 20112952
Structural biology of human H3K9 methyltransferases.
Wu H, Min J, Lunin VV, Antoshenko T, Dombrovski L, Zeng H, Allali-Hassani A, Campagna-Slater V, Vedadi M, Arrowsmith CH, Plotnikov AN, Schapira M
PLoS ONE. 2010 5(1):e8570. doi: 10.1371/journal.pone.0008570
PMID: 20084102
Evaluation of virtual screening as a tool for chemical genetic applications.
Campagna-Slater V, Schapira M
J Chem Inf Model. 2009 49(9):2082-91. doi: 10.1021/ci900219u
PMID: 19702241
Contact:
Structural Genomics Consortium
101 College St. , South Tower, Rm 713
Toronto, Ontario
M5G 1L6
Phone: 416-978-3092
Email: matthieu.schapira@utoronto.ca