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Chemical Inhibition of Protein Methyltransferases

Published:2016-09 Issue:9 Volume:23 Page:1067-1076
ISSN:2451-9456
Container-title:Cell Chemical Biology
language:en
Short-container-title:Cell Chemical Biology

Author:

Schapira Matthieu

Funder

AbbVie

Bayer Pharma AG

Boehringer Ingelheim

Canada Foundation for Innovation

Eshelman Institute for Innovation

Genome Canada

Innovative Medicines Initiative

ULTRA-DD

Janssen, Merck & Co.

Novartis Pharma AG

Ontario Ministry of Economic Development and Innovation

Pfizer

São Paulo Research Foundation

Takeda

Wellcome Trust

Publisher

Elsevier BV

Subject

Clinical Biochemistry,Drug Discovery,Pharmacology,Molecular Biology,Molecular Medicine,Biochemistry

Reference71 articles.

1. Epigenetic protein families: a new frontier for drug discovery;Arrowsmith;Nat. Rev. Drug Discov.,2012

2. Structural and biochemical insights into MLL1 core complex assembly;Avdic;Structure,2011

3. Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors;Baker;Oncotarget,2015

4. (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells;Barsyte-Lovejoy;Proc. Natl. Acad. Sci. USA,2014

5. Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L;Basavapathruni;Chem. Biol. Drug Des.,2012

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