Target discovery focused approaches to overcome bottlenecks in the exploitation of antimycobacterial natural products

Rafael Baptista, Sumana Bhowmick, Robert J. Nash, Les Baillie, Luis Mur

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Abstract

Tuberculosis is a major global health hazard. The search for new antimycobacterials has focused on such as screening combinational chemistry libraries or designing chemicals to target predefined pockets of essential bacterial proteins. The relative ineffectiveness of these has led to a reappraisal of natural products for new antimycobacterial drug leads. However, progress has been limited, we suggest through a failure in many cases to define the drug target and optimize the hits using this information. We highlight methods of target discovery needed to develop a drug into a candidate for clinical trials. We incorporate these into suggested analysis pipelines which could inform the research strategies to accelerate the development of new drug leads from natural products
Original languageEnglish
JournalFuture Medicinal Chemistry
Volume10
Issue number7
Early online date23 Mar 2018
DOIs
Publication statusPublished - 01 Apr 2018

Keywords

  • natural products
  • target discovery
  • tuberculosis

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