Journal
EPIGENOMICS
Volume 7, Issue 8, Pages 1327-1338Publisher
FUTURE MEDICINE LTD
DOI: 10.2217/epi.15.87
Keywords
chemical probe; MOA; off-target effects; PKMT; PRMT; target engagement
Categories
Funding
- NIGMS [1R01GM096056]
- NIH Director's New Innovator Award Program [1DP2-OD007335]
- NIH/NCI Cancer Center Support Grant [5P30 CA008748-44]
- Starr Cancer Consortium
- WH Goodwin and A Goodwin Commonwealth
- Foundation for Cancer Research
- Experimental Therapeutics Center of Memorial Sloan Kettering Cancer Center
- Tri-I Therapeutics Discovery Grant
- Sohn Conference Foundation
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Protein methyltransferases (PMT)s play essential roles in many biological processes through methylation of histones and diverse nonhistone substrates. Dysregulation of these enzymes has been implicated in many diseases including cancers. While PMT-associated biology can be probed via genetic perturbation, this approach targets full-length PMTs rather than their methyltransferase activities and often lacks temporal, spatial and dose controls (timing, location and amount of dosed compounds). By contrast, small-molecule inhibitors of PMTs can be designed to specifically target the methyltransferase domains in a temporal, spatial and dose-dependent manner. This utility has motivated the development of hundreds of PMT inhibitors, but meanwhile can make it challenging to select the most suitable PMT inhibitors to interrogate PMT-associated biology. This perspective aims to provide timely guidance to evaluate these PMT inhibitors in their relevant biological contexts.
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