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Tuberculosis (Edinb) ; 92(1): 72-83, 2012 Jan.
Article in English | MEDLINE | ID: mdl-21708485

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.


Subject(s)
Antitubercular Agents/pharmacology , Immunologic Factors/pharmacology , Mycobacterium tuberculosis/drug effects , Protein Kinase Inhibitors/pharmacology , Tuberculosis, Multidrug-Resistant/drug therapy , Antitubercular Agents/antagonists & inhibitors , Drug Design , Humans , Immunologic Factors/antagonists & inhibitors , Mycobacterium tuberculosis/genetics , Protein Kinase Inhibitors/antagonists & inhibitors , Small Molecule Libraries , Tuberculosis, Multidrug-Resistant/genetics
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