Fragment-based drug discovery as alternative strategy to the drug development for neglected diseases

Chem Biol Drug Des. 2017 Dec;90(6):1067-1078. doi: 10.1111/cbdd.13030. Epub 2017 Jul 3.

Abstract

Neglected diseases (NDs) affect large populations and almost whole continents, representing 12% of the global health burden. In contrast, the treatment available today is limited and sometimes ineffective. Under this scenery, the Fragment-Based Drug Discovery emerged as one of the most promising alternatives to the traditional methods of drug development. This method allows achieving new lead compounds with smaller size of fragment libraries. Even with the wide Fragment-Based Drug Discovery success resulting in new effective therapeutic agents against different diseases, until this moment few studies have been applied this approach for NDs area. In this article, we discuss the basic Fragment-Based Drug Discovery process, brief successful ideas of general applications and show a landscape of its use in NDs, encouraging the implementation of this strategy as an interesting way to optimize the development of new drugs to NDs.

Keywords: FBDD; drug design; fragment; hit; neglected diseases; screening.

Publication types

  • Review

MeSH terms

  • Cysteine Endopeptidases / chemistry
  • Cysteine Endopeptidases / metabolism*
  • Drug Design*
  • Drug Evaluation, Preclinical
  • Humans
  • Neglected Diseases / drug therapy*
  • Neglected Diseases / parasitology
  • Protozoan Proteins / antagonists & inhibitors
  • Protozoan Proteins / metabolism
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology
  • Small Molecule Libraries / therapeutic use*
  • Software
  • Trypanosoma brucei brucei / drug effects
  • Trypanosoma brucei brucei / metabolism

Substances

  • Protozoan Proteins
  • Small Molecule Libraries
  • Cysteine Endopeptidases
  • rhodesain