Literature DB >> 28689146

Chemical modulators for epigenome reader domains as emerging epigenetic therapies for cancer and inflammation.

Nilesh Zaware1, Ming-Ming Zhou2.   

Abstract

Site-specific lysine acetylation and methylation on histones are critical post-translational modifications (PTMs) that govern ordered gene transcription in chromatin. Mis-regulation of these histone PTM-mediated processes has been shown to be associated with human diseases. Since the 2010 landmark reports of small molecules (+)-JQ1 and I-BET762 that target the acetyl-lysine 'reader' Bromodomain and Extra Terminal domain (BET) proteins, there have been relentless efforts to develop epigenetic therapy with small molecules to modulate molecular interactions of epigenome reader domain proteins with PTMs. In addition to BET, the other emerging targets include non-BET acetyl-lysine and methyl-lysine reader domains. This review covers the key chemical modulators of the aforementioned epigenome reader proteins.
Copyright © 2017 Elsevier Ltd. All rights reserved.

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Year:  2017        PMID： 28689146      PMCID： PMC5581715          DOI： 10.1016/j.cbpa.2017.06.012

Source DB:  PubMed          Journal:  Curr Opin Chem Biol        ISSN： 1367-5931            Impact factor:   8.822


  61 in total

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Journal:  Nat Struct Mol Biol       Date:  2007-11-05       Impact factor: 15.369

5.  Structure and ligand of a histone acetyltransferase bromodomain.

Authors:  C Dhalluin; J E Carlson; L Zeng; C He; A K Aggarwal; M M Zhou
Journal:  Nature       Date:  1999-06-03       Impact factor: 49.962

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Journal:  Chem Biol       Date:  2006-01

7.  Structural basis of lysine-acetylated HIV-1 Tat recognition by PCAF bromodomain.

Authors:  Shiraz Mujtaba; Yan He; Lei Zeng; Amjad Farooq; Justin E Carlson; Melanie Ott; Eric Verdin; Ming-Ming Zhou
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Review 9.  Viral mechanisms involved in the transcriptional CBP/p300 regulation of inflammatory and immune responses.

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  14 in total

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3.  Domain-selective BET inhibition attenuates transcriptional and behavioral responses to cocaine.

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Review 6.  On top of biosynthetic gene clusters: How epigenetic machinery influences secondary metabolism in fungi.

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7.  The dCypher Approach to Interrogate Chromatin Reader Activity Against Posttranslational Modification-Defined Histone Peptides and Nucleosomes.

Authors:  Matthew R Marunde; Irina K Popova; Ellen N Weinzapfel; Michael-C Keogh
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Review 8.  Improved methods for targeting epigenetic reader domains of acetylated and methylated lysine.

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Review 9.  The Impact of obesity and diabetes mellitus on pancreatic cancer: Molecular mechanisms and clinical perspectives.

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