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通过使用荧光硫醇探针进行高通量筛选发现选择性胱硫醚β-合酶抑制剂。

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

作者信息

Niu Weining, Wu Ping, Chen Fei, Wang Jun, Shang Xiaoya, Xu Chunlan

机构信息

Key Laboratory for Space Bioscience and Space Biotechnology , School of Life Sciences , Northwestern Polytechnical University , Xi'an , 710072 , China . Email:

出版信息

Medchemcomm. 2016 Nov 15;8(1):198-201. doi: 10.1039/c6md00493h. eCollection 2017 Jan 1.

DOI:10.1039/c6md00493h
PMID:30108705
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6072345/
Abstract

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

摘要

开发了一种高通量检测方法来鉴定胱硫醚β-合酶（CBS）的抑制剂，CBS是参与硫化氢生物合成的三种关键酶之一。对6491种天然化合物进行筛选，鉴定出几种选择性CBS抑制剂，这些抑制剂能抑制HT29癌细胞的增殖，其半数抑制浓度（IC）值小于10μM。

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本文引用的文献

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Pharmacol Res. 2016 Nov;113(Pt A):18-37. doi: 10.1016/j.phrs.2016.08.016. Epub 2016 Aug 10.
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ACS Cent Sci. 2016 Apr 27;2(4):242-52. doi: 10.1021/acscentsci.6b00019. Epub 2016 Mar 9.
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