Plucking the high hanging fruit: A systematic approach for targeting protein-protein interactions

Monika Raj, Brooke N. Bullock, Paramjit S. Arora

Research output: Contribution to journalArticle

Abstract

Development of specific ligands for protein targets that help decode the complexities of protein-protein interaction networks is a key goal for the field of chemical biology. Despite the emergence of powerful in silico and experimental high-throughput screening strategies, the discovery of synthetic ligands that selectively modulate protein-protein interactions remains a challenge for bioorganic and medicinal chemists. This Perspective discusses emerging principles for the rational design of PPI inhibitors. Fundamentally, the approach seeks to adapt nature's protein recognition principles for the design of suitable secondary structure mimetics.

Original languageEnglish (US)
Pages (from-to)4051-4057
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume21
Issue number14
DOIs
StatePublished - Jul 15 2013

Keywords

  • Computational design
  • Hot spot residues
  • Protein-protein interactions
  • Rational design
  • Secondary structure mimics

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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