Cheryl H. Arrowsmith

Cheryl H. Arrowsmith

SGC Toronto

Arrowsmith

Biography

Cheryl Arrowsmith is a Senior Scientist at the Princess Margaret Cancer Centre, Professor in the Department of Medical Biophysics, University of Toronto, and the Chief Scientist of the Structural Genomics Consortium (SGC) at the University of Toronto.  Her research focuses on the structural and chemical biology of chromatin and epigenetic regulatory factors especially as relates to cancer and drug discovery. In partnership with major pharmaceutical companies, she leads the SGC’s international open science program that is developing and distributing unencumbered Chemical Probes that support the discovery of new medicines. She received her Ph.D. from the University of Toronto and carried out postdoctoral research at Stanford University, and was co-founder of Affinium Pharmaceuticals, which developed a new medicine for multidrug resistant bacteria. She has published over 300 research articles and was recognized by Clarivate Analytics as being among the worlds top 1% of highly cited scientists in 2018, 2019 and 2022. She was elected an AAAS Fellow (2015), and a Fellow of the Royal Society of Canada (2020).

2013

Structure of the Catalytic Domain of EZH2 Reveals Conformational Plasticity in Cofactor and Substrate Binding Sites and Explains Oncogenic Mutations.

Wu H, Zeng H, Dong A, Li F, He H, Senisterra G, Seitova A, Duan S, Brown PJ, Vedadi M, Arrowsmith CH, Schapira M

PLoS ONE. 2013-12-19 . 8(12):e83737 .doi: 10.1371/journal.pone.0083737

PMID: 24367611

Discovery of an in vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP.

Liu F, Barsyte-Lovejoy D, Li F, Xiong Y, Korboukh VK, Huang X, Allali-Hassani A, Janzen WP, Roth BL, Frye SV, Arrowsmith CH, Brown PJ, Vedadi M, Jin J

J. Med. Chem.. 2013-10-8 . .doi: 10.1021/jm401480r

PMID: 24102134

Control of the Hippo Pathway by Set7-Dependent Methylation of Yap.

Oudhoff MJ, Freeman SA, Couzens AL, Antignano F, Kuznetsova E, Min PH, Northrop JP, Lehnertz B, Barsyte-Lovejoy D, Vedadi M, Arrowsmith CH, Nishina H, Gold MR, Rossi FM, Gingras AC, Zaph C

Dev. Cell. 2013-7-9 . .doi: 10.1016/j.devcel.2013.05.025

PMID: 23850191

An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1.

Konze KD, Ma A, Li F, Barsyte-Lovejoy D, Parton T, Macnevin CJ, Liu F, Gao C, Huang XP, Kuznetsova E, Rougie M, Jiang A, Pattenden SG, Norris JL, James LI, Roth BL, Brown PJ, Frye SV, Arrowsmith CH, Hahn KM, Wang GG, Vedadi M, Jin J

ACS Chem. Biol.. 2013-4-24 . .doi: 10.1021/cb400133j

PMID: 23614352

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

Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain.

James LI, Barsyte-Lovejoy D, Zhong N, Krichevsky L, Korboukh VK, Herold JM, Macnevin CJ, Norris JL, Sagum CA, Tempel W, Marcon E, Guo H, Gao C, Huang XP, Duan S, Emili A, Greenblatt JF, Kireev DB, Jin J, Janzen WP, Brown PJ, Bedford MT, Arrowsmith CH, Frye SV

Nat. Chem. Biol.. 2013-1-6 . .doi: 10.1038/nchembio.1157

PMID: 23292653

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

Nahuoic Acid A Produced by a Streptomyces sp. Isolated From a Marine Sediment Is a Selective SAM-Competitive Inhibitor of the Histone Methyltransferase SETD8.

Williams DE, Dalisay DS, Li F, Amphlett J, Maneerat W, Chavez MA, Wang YA, Matainaho T, Yu W, Brown PJ, Arrowsmith CH, Vedadi M, Andersen RJ

Org. Lett.. 2012-12-28 . .doi: 10.1021/ol303416k

PMID: 23272941