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ACS Chem Biol. 2012 Mar 16;7(3):443-63. doi: 10.1021/cb200519y. Epub 2012 Feb 1.

Current chemical biology approaches to interrogate protein methyltransferases.

Author information

1
Molecular Pharmacology and Chemistry Program, Memorial Sloan-Kettering Cancer Center, New York, New York 10065, United States. luom@mskcc.org

Abstract

Protein methyltransferases (PMTs) play various physiological and pathological roles through methylating histone and nonhistone targets. However, most PMTs including more than 60 human PMTs remain to be fully characterized. The current approaches to elucidate the functions of PMTs have been diversified by many emerging chemical biology technologies. This review focuses on progress in these aspects and is organized into four discussion modules (assays, substrates, cofactors, and inhibitors) that are important to elucidate biological functions of PMTs. These modules are expected to provide general guidance and present emerging methods for researchers to select and combine suitable PMT-activity assays, well-defined substrates, novel SAM surrogates, and PMT inhibitors to interrogate PMTs.

PMID:
22220966
PMCID:
PMC3306480
DOI:
10.1021/cb200519y
[Indexed for MEDLINE]
Free PMC Article

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