Systematic Targeting of Protein–Protein Interactions

Ashley E. Modell, Sarah L. Blosser, Paramjit S. Arora

Research output: Contribution to journalReview article

Abstract

Over the past decade, protein–protein interactions (PPIs) have gone from being neglected as ‘undruggable’ to being considered attractive targets for the development of therapeutics. Recent advances in computational analysis, fragment-based screening, and molecular design have revealed promising strategies to address the basic molecular recognition challenge: how to target large protein surfaces with specificity. Several systematic and complementary workflows have been developed to yield successful inhibitors of PPIs. Here we review the major contemporary approaches utilized for the discovery of inhibitors and focus on a structure-based workflow, from the selection of a biological target to design.

Original languageEnglish (US)
Pages (from-to)702-713
Number of pages12
JournalTrends in Pharmacological Sciences
Volume37
Issue number8
DOIs
StatePublished - Aug 1 2016

Keywords

  • fragment-based design
  • inhibitors
  • protein-domain mimics
  • protein–protein interactions
  • rational design
  • screening

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology

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