A new class of ghrelin O-acyltransferase inhibitors incorporating triazole-linked lipid mimetic groups

Feifei Zhao, Joseph E. Darling, Richard A. Gibbs, James L. Hougland

Research output: Contribution to journalArticle

11 Scopus citations

Abstract

Inhibitors of ghrelin O-acyltransferase (GOAT) have untapped potential as therapeutics targeting obesity and diabetes. We report the first examples of GOAT inhibitors incorporating a triazole linkage as a biostable isosteric replacement for the ester bond in ghrelin and amide bonds in previously reported GOAT inhibitors. These triazole-containing inhibitors exhibit sub-micromolar inhibition of the human isoform of GOAT (hGOAT), and provide a foundation for rapid future chemical diversification and optimization of hGOAT inhibitors.

Original languageEnglish (US)
Pages (from-to)2800-2803
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number14
DOIs
StatePublished - Jun 4 2015

Keywords

  • 1,2,3-Triazole
  • Ghrelin
  • Ghrelin O-acyltransferase
  • Peptidomimetic
  • Serine acylation

ASJC Scopus subject areas

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

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