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Protein methyltransferase inhibitors as personalized cancer therapeutics

Authors
Journal
Drug Discovery Today Therapeutic Strategies
1740-6773
Publisher
Elsevier
Volume
9
Identifiers
DOI: 10.1016/j.ddstr.2011.08.001
Disciplines
  • Biology
  • Chemistry
  • Medicine

Abstract

The protein methyltransferases (PMTs) have emerged as a novel target class, especially for oncology indications where specific genetic alterations, affecting PMT activity, drive cancer tumorigenesis. This target class has proved quite druggable; small molecule inhibitors (PMTis) of several PMT enzymes have been reported, that display a diversity of chemical structures and target binding modalities. Here we review recent progress in identifying, characterizing and optimizing PMTis for eventual use as personally targeted cancer therapeutics.

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