α-Helix mimetics: Outwards and upwards

Madura K.P. Jayatunga, Sam Thompson, Andrew D. Hamilton

Research output: Contribution to journalReview article

Abstract

α-Helices are common secondary structural elements forming key parts of the large, generally featureless interfacial regions of many therapeutically-relevant protein-protein interactions (PPIs). The rational design of helix mimetics is an appealing small-molecule strategy for the mediation of aberrant PPIs, however the first generation of scaffolds presented a relatively small number of residues on a single recognition surface. Increasingly, helices involved in PPIs are found to have more complex binding modes, utilizing two or three recognition surfaces, or binding with extended points of contact. To address these unmet needs the design and synthesis of new generations of multi-sided, extended, and supersecondary structures are underway.

Original languageEnglish (US)
Pages (from-to)717-724
Number of pages8
JournalBioorganic and Medicinal Chemistry Letters
Volume24
Issue number3
DOIs
StatePublished - Feb 1 2014

Keywords

  • Peptidomimetic
  • Protein-protein interaction
  • Proteomimetic
  • Rational design

ASJC Scopus subject areas

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

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