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

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

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

Histone recognition by human malignant brain tumor domains.

Nady N, Krichevsky L, Zhong N, Duan S, Tempel W, Amaya MF, Ravichandran M, Arrowsmith CH

J. Mol. Biol.. 2012-11-9 . 423(5):702-18 .doi: 10.1016/j.jmb.2012.08.022

PMID: 22954662

Association of UHRF1 with methylated H3K9 directs the maintenance of DNA methylation.

Rothbart SB, Krajewski K, Nady N, Tempel W, Xue S, Badeaux AI, Barsyte-Lovejoy D, Martinez JY, Bedford MT, Fuchs SM, Arrowsmith CH, Strahl BD

Nat. Struct. Mol. Biol.. 2012-9-30 . 19(11):1155-60 .doi: 10.1038/nsmb.2391

PMID: 23022729

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

Sequence-specific recognition of a PxLPxI/L motif by an ankyrin repeat tumbler lock.

Xu C, Jin J, Bian C, Lam R, Tian R, Weist R, You L, Nie J, Bochkarev A, Tempel W, Tan CS, Wasney GA, Vedadi M, Gish GD, Arrowsmith CH, Pawson T, Yang XJ, Min J

Sci Signal. 2012-5-29 . 5(226):ra39 .doi: 10.1126/scisignal.2002979

PMID: 22649097