Research progress of selective small molecule bromodomain-containing protein 9 inhibitors

Ma Hui; Zhang Jian; Zheng Peiyuan; Wu Zhenwei; Zhang Huibin

doi:10.4155/fmc-2017-0243

Research progress of selective small molecule bromodomain-containing protein 9 inhibitors

Future Med Chem. 2018 Apr 1;10(8):895-906. doi: 10.4155/fmc-2017-0243. Epub 2018 Apr 5.

Authors

Ma Hui¹, Zhang Jian¹, Zheng Peiyuan¹, Wu Zhenwei¹, Zhang Huibin¹

Affiliation

¹ Center of Drug Discovery, Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease, China Pharmaceutical University, Nanjing 210009, PR China.

PMID: 29620420
DOI: 10.4155/fmc-2017-0243

Abstract

The bromodomain proteins, known as the key targets in epigenetics, are 'readers' of acetylated lysine of histones. As a member of bromodomain proteins, bromodomain-containing protein 9 (BRD9) is a subunit of mammalian SWI/SNF chromatin remodeling complexes. However, the biological functions and the potential application in therapeutics of BRD9 remain ambiguous due to a lack of selective small molecule inhibitors of BRD9. Recently, series of chemical ligands against BRD9 were developed by different research institutes. Here, we reviewed the development and characterization of reported BRD9 inhibitors, which will be the foundation of further chemical design and biological evaluation.

Keywords: BRD9 inhibitors; bromodomain-containing protein 9; epigenetics.

Publication types

Review

MeSH terms

Animals
Drug Discovery* / methods
Epigenesis, Genetic / drug effects
Humans
Models, Molecular
Small Molecule Libraries / chemistry*
Small Molecule Libraries / pharmacology*
Transcription Factors / antagonists & inhibitors*
Transcription Factors / chemistry
Transcription Factors / genetics
Transcription Factors / metabolism

Substances

BRD9 protein, human
Small Molecule Libraries
Transcription Factors