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. 2012 Jan;92(1):72-83.
doi: 10.1016/j.tube.2011.05.005. Epub 2011 Jun 25.

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

Robert C Reynolds  1 , Subramaniam Ananthan, Ellen Faaleolea, Judith V Hobrath, Cecil D Kwong, Clinton Maddox, Lynn Rasmussen, Melinda I Sosa, Elizabeth Thammasuvimol, E Lucile White, Wei Zhang, John A Secrist 3rd
Affiliations

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

Robert C Reynolds et al. Tuberculosis (Edinb). 2012 Jan.

Abstract

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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