Systematic analysis of helical protein interfaces reveals targets for synthetic inhibitors

Andrea L. Jochim, Paramjit S. Arora

Research output: Contribution to journalArticle

Abstract

Synthetic inhibitors of protein-protein interactions are being discovered despite the inherent challenge in targeting large contact surfaces with small molecules. An analysis of available examples identifies common features of complexes that make them tractable for small molecules. We deduced that relative disposition and energetic contributions of "hot spot" residues provide a predictive scale for the potential of protein-protein interactions to be inhibited by small molecules. On the basis of this model, we analyzed the full set of helical protein interfaces in the Protein Data Bank to identify those that are potentially suitable candidates for synthetic ligands.

Original languageEnglish (US)
Pages (from-to)919-923
Number of pages5
JournalACS Chemical Biology
Volume5
Issue number10
DOIs
StatePublished - Oct 15 2010

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine

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