Faculty: Masoud Vedadi, PhD

Masoud Vedadi, PhDMasoud Vedadi, PhD
Assistant Professor, Pharmacology & Toxicology
Principal Investigator, Molecular Biophysics, Structural Genomics Consortium

General Research Area: Epigenetics - Chemical Probes for Drug Discovery.

In Molecular Biophysics group we characterize proteins produced by the SGC scientists in Toronto and also focus on developing new high throughput biophysical and biochemical characterization and screening methods. We are particularly interested in developing chemical probes for epigenetic targets. By screening proteins against customized chemical libraries, we identify small molecules that inhibit / bind to these proteins that could be used in developing chemical probes for epigenetic targets in collaboration with chemistry partners and other SGC groups.  Creating and comparing chemical profiles for members of each family of protein along with functional studies, we investigate the structure-function relationship and identify unique inhibitors that can discriminate among members of each family of protein.
 

Selected Publications:

Zhu J, Sammons MA, Donahue G, Dou Z, Vedadi M, Getlik M, Barsyte-Lovejoy D, Al-Awar R, Katona BW, Shilatifard A, Huang J, Hua X, Arrowsmith CH, Berger SL. (2015) Gain-of-function p53 mutants co-opt chromatin pathways to drive cancer growth. Nature. PMID: 26331536

Curry E, Green I, Chapman-Rothe N, Shamsaei E, Kandil S, Cherblanc FL, Payne L, Bell E, Ganesh T, Srimongkolpithak N, Caron J, Li F, Uren AG, Snyder JP, Vedadi M, Fuchter MJ, Brown R. (2015) Dual EZH2 and EHMT2 histone methyltransferase inhibition increases biological efficacy in breast cancer cells. Clin Epigenetics. PMID: 26300989

Grebien F, Vedadi M, Getlik M, Giambruno R, Grover A, Avellino R, Skucha A, Vittori S, Kuznetsova E, Smil D, Barsyte-Lovejoy D, Li F, Poda G, Schapira M, Wu H, Dong A, Senisterra G, Stukalov A, Huber KV, Schönegger A, Marcellus R, Bilban M, Bock C, Brown PJ, Zuber J, Bennett KL, Al-Awar R, Delwel R, Nerlov C, Arrowsmith CH, Superti-Furga G. (2015) Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia. Nat Chem Biol. PMID: 26167872

Eram MS, Kuznetsova E, Li F, Lima-Fernandes E, Kennedy S, Chau I, Arrowsmith CH, Schapira M, Vedadi M. (2015) Kinetic characterization of human histone H3 lysine 36 methyltransferases, ASH1L and SETD2. Biochim Biophys Acta. 1850(9):1842-1848. PMID: 26002201

Sweis RF, Wang Z, Algire M, Arrowsmith CH, Brown PJ, Chiang GG, Guo J, Jakob CG, Kennedy S, Li F, Maag D, Shaw B, Soni NB, Vedadi M, Pappano WN. (2015) Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2. ACS Med Chem Lett. PMID: 26101576

Nguyen H, Allali-Hassani A, Antonysamy S, Chang S, Chen LH, Curtis C, Emtage S, Fan L, Gheyi T, Li F, Liu S, Martin JR, Mendel D, Olsen JB, Pelletier L, Shatseva T, Wu S, Zhang FF, Arrowsmith CH, Brown PJ, Campbell RM, Garcia BA, Barsyte-Lovejoy D, Mader M, Vedadi M. (2015) LLY-507, a Cell-Active, Potent and Selective Inhibitor of Protein Lysine Methyltransferase SMYD2. J. Biol. Chem. PMID: 25825497.

David Smil, Mohammad S. Eram, Fengling Li, Steven Kennedy, Magdalena M. Szewczyk, Peter J. Brown, Dalia Barsyte-Lovejoy, Cheryl H. Arrowsmith, Masoud Vedadi, and Matthieu Schapira (2015) Discovery of a Dual PRMT5–PRMT7 Inhibitor. ACS Med. Chem. Lett., 2015, 6 (4), 408–412. PMID: 25893041.

Ümit Kaniskan, Magdalena M. Szewczyk, Zhengtian Yu, Mohammad S. Eram, Xiaobao Yang, Keith Schmidt, Xiao Luo, Miao Dai, Feng He, Irene Zang, Ying Lin, Steven Kennedy, Fengling Li, Elena Dobrovetsky, Aiping Dong, David Smil, Sun-Joon Min, Melissa Landon, Jennifer Lin-Jones, Xi-Ping Huang, Bryan L. Roth, Matthieu Schapira, Peter Atadja, Dalia Barsyte-Lovejoy, Cheryl H. Arrowsmith, Peter J. Brown, Kehao Zhao, Jian Jin and Masoud Vedadi (2015) A Potent, Selective and Cell-active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3). Angewandte Chemie. PMID:25728001

Srimongkolpithak N, Sundriyal S, Li F, Vedadi M, Fuchter MJ. (2014) Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors.Medchemcomm. 5(12):1821-1828. PMID: 25750706.

Xu B, On DM, Ma A, Parton T, Konze KD, Pattenden SG, Allison DF, Cai L, Rockowitz S, Liu S, Liu Y, Li F, Vedadi M, Frye SV, Garcia BA, Zheng D, Jin J, Wang GG. (2014) Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia. Blood. PMID: 25395428


Contact:

MaRS Centre, South Tower
101 College Street, 7th floor, Rm. 714 
Toronto, Ontario 
M5G 1L7 
Phone: 416-946-0897
FAX: 416-946-0588
Email: m.vedadi@utoronto.ca

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