High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv

Tuberculosis (Edinb). 2009 Sep;89(5):334-53. doi: 10.1016/j.tube.2009.05.008. Epub 2009 Sep 15.

Abstract

There is an urgent need for the discovery and development of new antitubercular agents that target new biochemical pathways and treat drug resistant forms of the disease. One approach to addressing this need is through high-throughput screening of medicinally relevant libraries against the whole bacterium in order to discover a variety of new, active scaffolds that will stimulate new biological research and drug discovery. Through the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (www.taacf.org), a large, medicinally relevant chemical library was screened against M. tuberculosis strain H37Rv. The screening methods and a medicinal chemistry analysis of the results are reported herein.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Antitubercular Agents / pharmacology*
  • Bacterial Proteins / drug effects*
  • Dose-Response Relationship, Drug
  • Drug Design
  • Drug Evaluation, Preclinical*
  • Humans
  • Immunologic Factors / pharmacology*
  • Immunotherapy / methods*
  • Mycobacterium tuberculosis / drug effects*
  • Mycobacterium tuberculosis / isolation & purification
  • Small Molecule Libraries
  • Tuberculosis / drug therapy*
  • Tuberculosis / genetics
  • Tuberculosis / therapy

Substances

  • Antitubercular Agents
  • Bacterial Proteins
  • Immunologic Factors
  • Small Molecule Libraries