Design and modular parallel synthesis of a MCR derived α-helix mimetic protein-protein interaction inhibitor scaffold

Walfrido Antuch, Sanjay Menon, Quin-Zene Chen, Yingchun Lu, Sukumar Sakamuri, Barbara Beck, Vesna Schauer-Vukašinović, Seema Agarwal, Sibylle Hess, Alexander Dömling

Research output: Contribution to journalArticleAcademicpeer-review

48 Citations (Scopus)

Abstract

A terphenyl α-helix mimetic scaffold recognized to be capable of disrupting protein-protein interactions was structurally morphed into an easily amenable and versatile multicomponent reaction (MCR) backbone. The design, modular in-parallel library synthesis, initial cell based biological data, and preliminary in vitro screening for the disruption of the Bcl-w/Bak protein-protein interaction by representatives of the MCR derived scaffold are presented.
Original languageEnglish
Pages (from-to)1740-1743
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number6
DOIs
Publication statusPublished - 15-Mar-2006

Keywords

  • Apoptosis
  • Bcl family
  • Cancer
  • Isocyanide
  • Multicomponent reaction
  • Protein interaction antagonist
  • imidazole
  • terphenyl derivative
  • alpha helix
  • apoptosis
  • article
  • cell proliferation
  • enzyme inhibition
  • protein protein interaction
  • protein structure
  • protein synthesis

Cite this