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

共 50 条

[1] Identification of Cystathionine -Synthase Inhibitors Using a Hydrogen Sulfide Selective Probe
Thorson, Megan K.
Majtan, Tomas
Kraus, Jan P.
Barrios, Amy M.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2013, 52 (17) : 4641 - 4644
[2] A novel high-throughput cellular screening assay for the discovery of HIV-1 integrase inhibitors
Van Loock, M.
Meersseman, G.
Van Acker, K.
Van Den Eynde, C.
Jochmans, D.
Van Schoubroeck, B.
Dams, G.
Heyndrickx, L.
Clayton, R. F.
JOURNAL OF VIROLOGICAL METHODS, 2012, 179 (02) : 396 - 401
[3] Rapid Discovery of a Photocatalyst for Air Purification by High-Throughput Screening
Sun, Song
Zhang, Fan
Qi, Zeming
Ding, Jianjun
Bao, Jun
Gao, Chen
CHEMCATCHEM, 2014, 6 (09) : 2535 - 2539
[4] Label-Free High-Throughput Screening via Mass Spectrometry: A Single Cystathionine Quantitative Method for Multiple Applications
Holt, Tom G.
Choi, Bernard K.
Geoghagen, Neil S.
Jensen, Kristian K.
Luo, Qi
LaMarr, William A.
Makara, Gergely M.
Malkowitz, Lorraine
Ozbal, Can C.
Xiong, Yusheng
Dufresne, Claude
Luo, Ming-Juan
ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES, 2009, 7 (05) : 495 - 506
[5] Development and Application of Activity-based Fluorescent Probes for High-Throughput Screening
Cheng, Juan
Li, Xin
CURRENT MEDICINAL CHEMISTRY, 2022, 29 (10) : 1739 - 1756
[6] A multifunctional cross-validation high-throughput screening protocol enabling the discovery of new SHP2 inhibitors
Song, Yihui
Zhao, Min
Wu, Yahong
Yu, Bin
Liu, Hong-Min
ACTA PHARMACEUTICA SINICA B, 2021, 11 (03) : 750 - 762
[7] High-Throughput Screening Methodology to Identify Alpha-Synuclein Aggregation Inhibitors
Pujols, Jordi
Pena-Diaz, Samuel
Conde-Gimenez, Maria
Pinheiro, Francisca
Navarro, Susanna
Sancho, Javier
Ventura, Salvador
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 2017, 18 (03):
[8] High-Throughput Screening for Growth Inhibitors Using a Yeast Model of Familial Paraganglioma
Bancos, Irina
Bida, John Paul
Tian, Defeng
Bundrick, Mary
John, Kristen
Holte, Molly Nelson
Her, Yeng F.
Evans, Debra
Saenz, Dyana T.
Poeschla, Eric M.
Hook, Derek
Georg, Gunda
Maher, L. James
PLOS ONE, 2013, 8 (02):
[9] An Innovative High-Throughput Screening Approach for Discovery of Small Molecules That Inhibit TNF Receptors
Lo, Chih Hung
Vunnam, Nagamani
Lewis, Andrew K.
Chiu, Ting-Lan
Brummel, Benjamin E.
Schaaf, Tory M.
Grant, Benjamin D.
Bawaskar, Prachi
Thomas, David D.
Sachs, Jonathan N.
SLAS DISCOVERY, 2017, 22 (08) : 950 - 961
[10] Identification of a Class of WNK Isoform-Specific Inhibitors Through High-Throughput Screening
Chlebowicz, Julita
Akella, Radha
Humphreys, John M.
He, Haixia
Kannangara, Ashari R.
Wei, Shuguang
Posner, Bruce
Goldsmith, Elizabeth J.
DRUG DESIGN DEVELOPMENT AND THERAPY, 2023, 17 : 93 - 105

← 1 2 3 4 5 →