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

Academic Article

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┬ávitro.
  • Published In

  • Tuberculosis  Journal
  • Keywords

  • Antitubercular Agents, Drug Design, Humans, Immunologic Factors, Mycobacterium tuberculosis, Protein Kinase Inhibitors, Small Molecule Libraries, Tuberculosis, Multidrug-Resistant
  • Digital Object Identifier (doi)

    Author List

  • Reynolds RC; Ananthan S; Faaleolea E; Hobrath JV; Kwong CD; Maddox C; Rasmussen L; Sosa MI; Thammasuvimol E; White EL
  • Start Page

  • 72
  • End Page

  • 83
  • Volume

  • 92
  • Issue

  • 1