Genetically selected cyclic-peptide inhibitors of AICAR transformylase homodimerization

Ali Tavassoli, Stephen J. Benkovic

Research output: Contribution to journalArticle

69 Scopus citations

Abstract

(Graph Presented) Finding the needle in a haystack need not be as troublesome as once thought. By coupling disruption of protein-protein (X-X) interactions to host-cell survival (see figure), inhibitors of ATIC (a key enzyme in the de novo purine biosynthetic pathway) were readily identified from a biosynthesized library of 107 small molecules. The activity and selectivity of nine cyclic peptides selected by this method were demonstrated in vivo and in vitro. AICAR=aminoimidazole-4-carboxamide ribonucleotide.

Original languageEnglish (US)
Pages (from-to)2760-2763
Number of pages4
JournalAngewandte Chemie - International Edition
Volume44
Issue number18
DOIs
StatePublished - Apr 29 2005

All Science Journal Classification (ASJC) codes

  • Catalysis
  • Chemistry(all)

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