Heterobivalent ligands crosslink multiple cell-surface receptors: The human melanocortin-4 and δ-opioid receptors

Josef Vagner, Liping Xu, Heather L. Handl, Jatinder S. Josan, David L. Morse, Eugene A. Mash, Robert J. Gillies, Victor J. Hruby

Research output: Contribution to journalArticle

61 Scopus citations

Abstract

(Figure Presented) Together we bind: A series of synthetic heterobivalent ligands containing a fragment of melanocyte stimulating hormone analogue MSH(7) and the δ-opioid ligand deltorphin-II has been prepared. These ligands bind with higher affinity and with apparent cooperativity to cells expressing both hMC4R and d-opioid receptors. Binding affinities were evaluated using a lanthanide-based in-cyto time-resolved fluorescence binding assay.

Original languageEnglish (US)
Pages (from-to)1685-1688
Number of pages4
JournalAngewandte Chemie - International Edition
Volume47
Issue number9
DOIs
StatePublished - Feb 15 2008

Keywords

  • Binding assay
  • Fluorescence spectroscopy
  • Molecular dynamics
  • Peptidomimetics
  • Solid-phase synthesis

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)

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