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).

2019

A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function.

Fagan V, Johansson C, Gileadi C, Monteiro O, Dunford JE, Nibhani R, Philpott M, Malzahn J, Wells G, Farham R, Cribbs A, Halidi N, Li F, Chau I, Greschik H, Velupillai S, Allali-Hassani A, Bennett JM, Christott T, Giroud C, Lewis AM, Huber KVM, Athanasou N, Bountra C, Jung M, Schüle R, Vedadi M, Arrowsmith CH, Xiong Y, Jin J, Fedorov O, Farnie G, Brennan PE, Oppermann UCT

J. Med. Chem.. 2019-9-24 . .doi: 10.1021/acs.jmedchem.9b00562

PMID: 31550156

Selective, small molecule co-factor binding site inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax (SET) domain containing lysine methyltransferase.

Taylor AP, Szewczyk MM, Kennedy S, Trush VV, Wu H, Zeng H, Dong A, de Freitas RF, Tatlock JH, Kumpf RA, Wythes M, Casimiro-Garcia A, Denny RA, Parikh MD, Li F, Barsyte-Lovejoy D, Schapira M, Vedadi M, Brown P, Arrowsmith CH, Owen DR

J. Med. Chem.. 2019-8-15 . .doi: 10.1021/acs.jmedchem.9b00112

PMID: 31415173

Therapeutic Targeting of RNA Splicing Catalysis through Inhibition of Protein Arginine Methylation.

Fong JY, Pignata L, Goy PA, Kawabata KC, Lee SC, Koh CM, Musiani D, Massignani E, Kotini AG, Penson A, Wun CM, Shen Y, Schwarz M, Low DH, Rialdi A, Ki M, Wollmann H, Mzoughi S, Gay F, Thompson C, Hart T, Barbash O, Luciani GM, Szewczyk MM, Wouters BJ, Delwel R, Papapetrou EP, Barsyte-Lovejoy D, Arrowsmith CH, Minden MD, Jin J, Melnick A, Bonaldi T, Abdel-Wahab O, Guccione E

Cancer Cell. 2019-8-12 . 36(2):194-209.e9 .doi: 10.1016/j.ccell.2019.07.003

PMID: 31408619

The MLL1 trimeric catalytic complex is a dynamic conformational ensemble stabilized by multiple weak interactions.

Kaustov L, Lemak A, Wu H, Faini M, Fan L, Fang X, Zeng H, Duan S, Allali-Hassani A, Li F, Wei Y, Vedadi M, Aebersold R, Wang Y, Houliston S, Arrowsmith CH

Nucleic Acids Res.. 2019-8-10 . .doi: 10.1093/nar/gkz697

PMID: 31400120

Identification and characterization of the first fragment hits for SETDB1 Tudor domain.

Mader P, Mendoza-Sanchez R, Iqbal A, Dong A, Dobrovetsky E, Corless VB, Liew SK, Houliston SR, De Freitas RF, Smil D, Sena CCD, Kennedy S, Diaz DB, Wu H, Dombrovski L, Allali-Hassani A, Min J, Schapira M, Vedadi M, Brown PJ, Santhakumar V, Yudin AK, Arrowsmith CH

Bioorg. Med. Chem.. 2019-7-12 . .doi: 10.1016/j.bmc.2019.07.020

PMID: 31327677

Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3.

Böttcher J, Dilworth D, Reiser U, Neumüller RA, Schleicher M, Petronczki M, Zeeb M, Mischerikow N, Allali-Hassani A, Szewczyk MM, Li F, Kennedy S, Vedadi M, Barsyte-Lovejoy D, Brown PJ, Huber KVM, Rogers CM, Wells CI, Fedorov O, Rumpel K, Zoephel A, Mayer M, Wunberg T, Böse D, Zahn S, Arnhof H, Berger H, Reiser C, Hörmann A, Krammer T, Corcokovic M, Sharps B, Winkler S, Häring D, Cockcroft XL, Fuchs JE, Müllauer B, Weiss-Puxbaum A, Gerstberger T, Boehmelt G, Vakoc CR, Arrowsmith CH, Pearson M, McConnell DB

Nat. Chem. Biol.. 2019-7-8 . .doi: 10.1038/s41589-019-0310-x

PMID: 31285596

Target 2035: probing the human proteome.

Carter AJ, Kraemer O, Zwick M, Mueller-Fahrnow A, Arrowsmith CH, Edwards AM

Drug Discov. Today. 2019-7-3 . .doi: 10.1016/j.drudis.2019.06.020

PMID: 31278990

Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1).

Xiong Y, Greschik H, Johansson C, Seifert L, Bacher J, Park KS, Babault N, Martini ML, Fagan V, Li F, Chau I, Christott T, Dilworth D, Barsyte-Lovejoy D, Vedadi M, Arrowsmith CH, Brennan PE, Fedorov O, Jung M, Farnie G, Liu J, Oppermann UCT, Schüle R, Jin J

J. Med. Chem.. 2019-7-1 . .doi: 10.1021/acs.jmedchem.9b00522

PMID: 31260300

Structural basis of HMCES interactions with abasic DNA and multivalent substrate recognition.

Halabelian L, Ravichandran M, Li Y, Zeng H, Rao A, Aravind L, Arrowsmith CH

Nat. Struct. Mol. Biol.. 2019-6-24 . .doi: 10.1038/s41594-019-0246-6

PMID: 31235913

Discovery of selective activators of PRC2 mutant EED-I363M.

Suh JL, Barnash KD, Abramyan TM, Li F, The J, Engelberg IA, Vedadi M, Brown PJ, Kireev DB, Arrowsmith CH, James LI, Frye SV

Sci Rep. 2019-4-25 . 9(1):6524 .doi: 10.1038/s41598-019-43005-z

PMID: 31024026