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Towards novel therapeutics for HIV through fragment-based screening and drug design

Academic Article
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Overview

authors

  • Tiefenbrunn Sample, Theresa
  • Stout, C. David

publication date

  • November 2014

journal

  • Progress in Biophysics & Molecular Biology  Journal

abstract

  • Fragment-based drug discovery has been applied with varying levels of success to a number of proteins involved in the HIV (Human Immunodeficiency Virus) life cycle. Fragment-based approaches have led to the discovery of novel binding sites within protease, reverse transcriptase, integrase, and gp41. Novel compounds that bind to known pockets within CCR5 have also been identified via fragment screening, and a fragment-based approach to target the TAR-Tat interaction was explored. In the context of HIV-1 reverse transcriptase (RT), fragment-based approaches have yielded fragment hits with mid-μM activity in an in vitro activity assay, as well as fragment hits that are active against drug-resistant variants of RT. Fragment-based drug discovery is a powerful method to elucidate novel binding sites within proteins, and the method has had significant success in the context of HIV proteins.

subject areas

  • Anti-Retroviral Agents
  • Drug Design
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors
  • HIV
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Research

keywords

  • Allosteric sites
  • FBDD
  • Fragment-based screening
  • HIV-1
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Identity

International Standard Serial Number (ISSN)

  • 0079-6107

Digital Object Identifier (DOI)

  • 10.1016/j.pbiomolbio.2014.09.009

PubMed ID

  • 25455312
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Additional Document Info

start page

  • 124

end page

  • 140

volume

  • 116

issue

  • 2-3

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