Chemistry and biology of chromatin remodeling agents: State of art and future perspectives of HDAC inhibitors

被引:62
|
作者
Rodriquez, M
Aquino, M
Bruno, I
De Martino, G
Taddei, M
Gomez-Paloma, L
机构
[1] Univ Salerno, Dipartimento Sci Farmaceut, I-84084 Salerno, Italy
[2] Univ Siena, Dipartimento Farmacochim Tecnol, I-53100 Siena, Italy
关键词
epigenetic therapy; histone deacetylase; histone acetyltransferase; HDAC inhibitors; antitumor; apoptosis; chromatin remodeling agents;
D O I
10.2174/092986706776360905
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Chromatin remodeling is a fundamental phenomenon in the life of eukaryotic cells, bearing implications to numerous physiological and pathological phenomena. This review outlines the chemistry of natural and synthetic agents endowed with the ability to interfere with such biological function, with a particular emphasis on histone deacetylase (HDAC) inhibitors. Other aspects covered in this article comprise structure activity relationships (SAR) and modes of action at molecular level, including the description of crystal structures of enzyme-inhibitor complexes.
引用
收藏
页码:1119 / 1139
页数:21
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