Novel pyrrolopyrimidine-based α-helix mimetics: Cell-permeable inhibitors of protein-protein interactions

Ji Hoon Lee, Qi Zhang, Sunhwan Jo, Sergio C. Chai, Misook Oh, Wonpil Im, Hua Lu, Hyun Suk Lim

Research output: Contribution to journalArticle

97 Scopus citations

Abstract

There is considerable interest in developing non-peptidic, small-molecule α-helix mimetics to disrupt α-helix-mediated protein-protein interactions. Herein, we report the design of a novel pyrrolopyrimidine-based scaffold for such α-helix mimetics with increased conformational rigidity. We also developed a facile solid-phase synthetic route that is amenable to divergent synthesis of a large library. Using a fluorescence polarization-based assay, we identified cell-permeable, dual MDMX/MDM2 inhibitors, demonstrating that the designed molecules can act as a-helix mimetics.

Original languageEnglish (US)
Pages (from-to)676-679
Number of pages4
JournalJournal of the American Chemical Society
Volume133
Issue number4
DOIs
StatePublished - Feb 2 2011

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ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)
  • Biochemistry
  • Colloid and Surface Chemistry

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