High throughput screening of a library based on kinase inhibitor scaffolds against Mycobacterium tuberculosis H37Rv.
High throughput screening of a library based on kinase inhibitor scaffolds against Mycobacterium tuberculosis H37Rv.
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DOI：
10.1016/j.tube.2011.05.005
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发表时间：
2012-01
期刊：
影响因子：
--
通讯作者：
Secrist JA 3rd
中科院分区：
文献类型：
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作者：
Reynolds RC;Ananthan S;Faaleolea E;Hobrath JV;Kwong CD;Maddox C;Rasmussen L;Sosa MI;Thammasuvimol E;White EL;Zhang W;Secrist JA 3rd
激酶靶点正在癌症以外的各种疾病中寻求，包括免疫和代谢以及病毒，寄生虫，真菌和细菌。特别是，有一个相对较新的兴趣在结核分枝杆菌的激酶和ATP结合的目标，以确定抑制剂和潜在的药物，目前的药物治疗方案不针对必需的蛋白质。在此，我们报告了基于当前激酶抑制剂支架和已知激酶结合位点设计的约26，000种化合物的靶向文库的高通量筛选结果。本文提供的表型数据可以形成基于体外对全细菌的表观活性选择支架/化合物用于针对结核分枝杆菌中的特异性激酶或其他ATP结合靶标的进一步酶筛选的基础。
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.
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影响因子：
2.7
作者：
Foroumadi, A;Kargar, Z;Shafiee, A
通讯作者：
Shafiee, A
影响因子：
6.7
作者：
Carta, A;Sanna, P;Loddo, R
通讯作者：
Loddo, R
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7.3
作者：
Geronikaki, A.;Eleftheriou, P.;Saxena, A. K.
通讯作者：
Saxena, A. K.
通过结核分枝杆菌的相互作用组分析发现新的信号蛋白和潜在的药物靶点
影响因子：
4.4
作者：
Cui T;Zhang L;Wang X;He ZG
通讯作者：
He ZG
影响因子：
--
作者：
Holcakova, Jitka;Tomasec, Peter;Vojtesek, Borivoj
通讯作者：
Vojtesek, Borivoj