Synthesis and screening of small-molecule α-helix mimetic libraries targeting protein-protein interactions

Heejo Moon, Hyun Suk Lim

Research output: Contribution to journalReview article

28 Scopus citations

Abstract

α-Helices are the most common protein secondary structure and play a key role in mediating many protein-protein interactions (PPIs) by serving as recognition motifs. Given that aberrant α-helix-mediated PPIs are linked to various disease states, targeting such interactions with small-molecules represents an attractive strategy to develop therapeutic candidates for the related diseases. Over the last decade, significant efforts have been directed toward developing α-helix mimetic small-molecules that can modulate α-helix-mediated PPIs. In this review, we will highlight recent advances in the development of non-peptidic, small-molecule α-helix mimetics with a focus on library synthesis and screening methods to efficiently discover small-molecule α-helix mimetics.

Original languageEnglish (US)
Pages (from-to)38-47
Number of pages10
JournalCurrent Opinion in Chemical Biology
Volume24
DOIs
StatePublished - Feb 1 2015

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry

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