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).

2014

Discovery of a Selective, Substrate-competitive Inhibitor of the Lysine Methyltransferase SETD8.

Ma A, Yu W, Li F, Bleich RM, Herold JM, Butler KV, Norris JL, Korboukh V, Tripathy A, Janzen WP, Arrowsmith CH, Frye SV, Vedadi M, Brown PJ, Jin J

J. Med. Chem.. 2014-7-17 . .doi: 10.1021/jm500871s

PMID: 25032507

RPRD1A and RPRD1B are human RNA polymerase II C-terminal domain scaffolds for Ser5 dephosphorylation.

Ni Z, Xu C, Guo X, Hunter GO, Kuznetsova OV, Tempel W, Marcon E, Zhong G, Guo H, Kuo WH, Li J, Young P, Olsen JB, Wan C, Loppnau P, El Bakkouri M, Senisterra GA, He H, Huang H, Sidhu SS, Emili A, Murphy S, Mosley AL, Arrowsmith CH, Min J, Greenblatt JF

Nat. Struct. Mol. Biol.. 2014-7-6 . .doi: 10.1038/nsmb.2853

PMID: 24997600

Trimethylation of Histone H3 Lysine 36 by Human Methyltransferase PRDM9.

Eram MS, Bustos SP, Lima-Fernandes E, Siarheyeva A, Senisterra G, Hajian T, Chau I, Duan S, Wu H, Dombrovski L, Schapira M, Arrowsmith CH, Vedadi M

J. Biol. Chem.. 2014-3-14 . .doi: 10.1074/jbc.M113.523183

PMID: 24634223

A Basic Post-SET Extension of NSDs Is Essential for Nucleosome Binding In Vitro.

Allali-Hassani A, Kuznetsova E, Hajian T, Wu H, Dombrovski L, Li Y, Gräslund S, Arrowsmith CH, Schapira M, Vedadi M

J Biomol Screen. 2014-3-4 . .doi: 10.1177/1087057114525854

PMID: 24595546

The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.

Camerino MA, Zhong N, Dong A, Dickson BM, James LI, Baughman BM, Norris JL, Kireev DB, Janzen WP, Arrowsmith CH, Frye SV

Medchemcomm. 2014-1-28 . 4(11):1501-1507 .doi: 10.1039/C3MD00197K

PMID: 24466405

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