Oligo-benzamide-based peptide mimicking tools for modulating biology

Chia Yuan Chen, Scott Elmore, Ismail Lalami, Henry Neal, Ratna K. Vadlamudi, Ganesh V. Raj, Jung Mo Ahn

Research output: Chapter in Book/Report/Conference proceedingChapter

Abstract

The oligo-benzamide scaffold is a rigid organic framework that can hold 2–3 functional groups as O-alkyl substituents on its benzamide units, mirroring their natural arrangement in an α-helix. Oligo-benzamides demonstrated outstanding α-helix mimicry and can be readily synthesized by following high yielding and iterative reaction steps in both solution-phase and solid-phase. A number of oligo-benzamides have been designed to emulate α-helical peptide segments in biologically active proteins and showed strong protein binding, in turn effectively disrupting protein-protein interactions in vitro and in vivo. In this chapter, the design of oligo-benzamides for mimicking α-helices, efficient synthetic routes for producing them, and their biomedical studies showing remarkable potency in inhibiting protein functions are discussed.

Original languageEnglish (US)
Title of host publicationMethods in Enzymology
PublisherAcademic Press Inc.
DOIs
StateAccepted/In press - 2024

Publication series

NameMethods in Enzymology
ISSN (Print)0076-6879
ISSN (Electronic)1557-7988

Keywords

  • LXXLL motif
  • Nuclear receptor-coregulator interaction
  • Oligo-benzamides
  • Peptidomimetics
  • Prostate and breast cancer
  • Protein-protein interaction
  • α-Helix mimetics

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology

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