High throughput screening of a library based on kinase inhibitor scaffolds against Mycobacterium tuberculosis H37Rv

被引：82

作者：

Reynolds, Robert C. ^{[1
]}

Ananthan, Subramaniam ^{[1
]}

Faaleolea, Ellen ^{[2
]}

Hobrath, Judith V. ^{[1
]}

Kwong, Cecil D. ^{[1
]}

Maddox, Clinton ^{[1
]}

Rasmussen, Lynn ^{[1
]}

Sosa, Melinda I. ^{[1
]}

Thammasuvimol, Elizabeth ^{[2
]}

White, E. Lucile ^{[1
]}

Zhang, Wei ^{[1
]}

Secrist, John A., III ^{[1
]}

机构：

[1] So Res Inst, Birmingham, AL 35205 USA

[2] So Res Inst, Frederick, MD 21701 USA

来源：

TUBERCULOSIS | 2012年 / 92卷 / 01期

关键词：

TAACF; Antitubercular; High throughput screening methods; Medicinal chemistry analysis; Designed kinase inhibitor library; CYCLIN-DEPENDENT KINASES; PROTEIN-KINASES; 1,3,4-OXADIAZOLE DERIVATIVES; ANTIMYCOBACTERIAL ACTIVITY; STRUCTURE CLASSIFICATION; ANTITUBERCULAR ACTIVITY; MAP KINASE; AGENTS; POTENT; PHOSPHORYLATION;

D O I：

10.1016/j.tube.2011.05.005

中图分类号：

R392 [医学免疫学]; Q939.91 [免疫学];

学科分类号：

100102 ;

摘要：

Kinase targets are being pursued in a variety of diseases beyond cancer, including immune and metabolic as well as viral, parasitic, fungal and bacterial. In particular, there is a relatively recent interest in kinase and ATP-binding targets in Mycobacterium tuberculosis in order to identify inhibitors and potential drugs for essential proteins that are not targeted by current drug regimens. Herein, we report the high throughput screening results for a targeted library of approximately 26,000 compounds that was designed based on current kinase inhibitor scaffolds and known kinase binding sites. The phenotypic data presented herein may form the basis for selecting scaffolds/compounds for further enzymatic screens against specific kinase or other ATP-binding targets in Mycobacterium tuberculosis based on the apparent activity against the whole bacteria in vitro. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：72 / 83

页数：12

共 75 条

[1] High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv [J].