Structure of the PRC2 complex and application to drug discovery

The polycomb repressive complexes 2 （PRC2） complex catalyzes tri-methylation of histone H3 lysine 27 （H3K27）, a repressive chromatin marker associated with gene silencing. Overexpression and mutations of PRC2 are found in a wide variety of cancers, making the catalytic activity of PRC2 an important...

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Bibliographic Details
Published in:Acta pharmacologica Sinica 2017-07, Vol.38 (7), p.963-976
Main Authors: Shi, Yi, Wang, Xiao-xi, Zhuang, You-wen, Jiang, Yi, Melcher, Karsten, Xu, H Eric
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biomedical and Life Sciences
Biomedicine
Cancer
Cancer therapies
Catalytic activity
Cell cycle
Chromatin
DNA methylation
Drug Discovery
Epigenetics
Gene expression
Gene silencing
Histone H3
Humans
Immunology
Internal Medicine
Lysine
Medical Microbiology
Methylation
Mutation
Neoplasms - drug therapy
Neoplasms - metabolism
Peptides
Pharmacology/Toxicology
Polycomb group proteins
Polycomb Repressive Complex 2 - antagonists & inhibitors
Polycomb Repressive Complex 2 - chemistry
Polycomb Repressive Complex 2 - metabolism
Proteins
R&D
Research & development
Review
Small Molecule Libraries - chemistry
Small Molecule Libraries - pharmacology
Vaccine
体结构
催化活性
基因沉默
复合物
应用
癌症治疗
组蛋白H3
药物发现
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Description
Summary:The polycomb repressive complexes 2 （PRC2） complex catalyzes tri-methylation of histone H3 lysine 27 （H3K27）, a repressive chromatin marker associated with gene silencing. Overexpression and mutations of PRC2 are found in a wide variety of cancers, making the catalytic activity of PRC2 an important target of cancer therapy. This review highlights recent structural breakthroughs of the human PRC2 complex bound to the H3K27 peptide and a small molecule inhibitor, which provide critically needed insight into PRC2-targeted drug discovery.
ISSN:1671-4083
1745-7254
DOI:10.1038/aps.2017.7