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Updated: May 31, 2026
System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis
Published on: April 5, 2017
High throughput screening of a library based on kinase inhibitor scaffolds against Mycobacterium tuberculosis H37Rv
Robert C Reynolds1, Subramaniam Ananthan, Ellen Faaleolea
1Southern Research Institute, 2000 Ninth Avenue South, Birmingham, AL 35205, USA. reynolds@SouthernResearch.org
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.
Insights
Researchers screened 26,000 compounds targeting kinase and ATP-binding proteins in Mycobacterium tuberculosis. This study identifies potential drug candidates for tuberculosis treatment by screening against whole bacteria.
Area of Science:
- Medicinal Chemistry
- Infectious Diseases
- Biochemistry
Background:
- Kinase inhibitors are explored for various diseases, including infectious agents.
- Mycobacterium tuberculosis presents unique kinase and ATP-binding targets for novel drug development.
- Current drug regimens do not target essential proteins in M. tuberculosis.
Purpose of the Study:
- To screen a targeted library of kinase inhibitor scaffolds against Mycobacterium tuberculosis.
- To identify compounds with phenotypic activity against whole bacteria.
- To provide a basis for selecting drug candidates for further enzymatic screening.
Main Methods:
- High-throughput screening of approximately 26,000 compounds.
- Compounds designed based on known kinase inhibitor scaffolds and binding sites.
- Phenotypic screening against whole Mycobacterium tuberculosis bacteria in vitro.
Main Results:
- Screening identified compounds with apparent activity against M. tuberculosis.
- Phenotypic data provides a foundation for further drug discovery efforts.
- The results guide the selection of scaffolds for specific kinase or ATP-binding targets.
Conclusions:
- The high-throughput screening successfully identified potential inhibitors of M. tuberculosis.
- This approach facilitates the discovery of novel anti-tubercular agents.
- The findings support further investigation of kinase and ATP-binding targets for tuberculosis therapy.
