Discovery of selective cystathionine β-synthase inhibitors by high-throughput screening with a fluorescent thiol probe

被引：22

作者：

Niu, Weining ^{[1
]}

Wu, Ping ^{[1
]}

Chen, Fei ^{[1
]}

Wang, Jun ^{[1
]}

Shang, Xiaoya ^{[1
]}

Xu, Chunlan ^{[1
]}

机构：

[1] Northwestern Polytech Univ, Sch Life Sci, Key Lab Space Biosci & Space Biotechnol, Xian 710072, Peoples R China

来源：

MEDCHEMCOMM | 2017年 / 8卷 / 01期

基金：

中国国家自然科学基金;

关键词：

HYDROGEN-SULFIDE; COLON-CANCER; HOMOCYSTINURIA; MUTATIONS; THERAPY;

D O I：

10.1039/c6md00493h

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：

A high-throughput assay was developed to identify inhibitors of cystathionine beta-synthase (CBS), which is one of three key enzymes involved in H2S biosynthesis. Screening of 6491 natural compounds identified several selective CBS inhibitors, which suppressed the proliferation of HT29 cancer cells, with IC50 values of less than 10 mu M.

引用

页码：198 / 201

页数：4

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