Real time differentiation of G-protein coupled receptor (GPCR) agonist and antagonist by two photon fluorescence laser microscopy

Minying Cai, Magda Stankova, Stephanie J.K. Pond, Alexander V. Mayorov, Joseph W. Perry, Henry I. Yamamura, Dev Trivedi, Victor J. Hruby

Research output: Contribution to journalArticle

29 Scopus citations

Abstract

Receptor-based signaling mechanisms are the primary source of cellular regulation. The superfamily of G protein-coupled receptors (GPCR) is the largest and most ubiquitous of the receptor-mediated processes. Desensitization of G-protein-coupled receptors is a fundamental mechanism regulating the cellular response to agonists. We have recently studied the agonist and antagonist of the human melanocortin receptors (hMC1, hMC3, hMC4, and hMC5 receptors), the human delta opioid receptor, and the human gluacagon receptor with the help of synthetic fluorescent labeled ligands and fluorescent protein-labeled β-arrestin-receptors that shed new insight on cellular signaling and rapid screening of drugs in real time. It was demonstrated that stimulation of these receptors by the cognate agonist triggers the rapid internalization of ligand-receptor complexes, while the interaction of the receptor with antagonists does not follow this pathway. Furthermore, receptor internalization is dependent upon β-arrestin, which has been shown to be responsible for the rapid desensitization of cAMP-signaling processes.

Original languageEnglish (US)
Pages (from-to)7160-7161
Number of pages2
JournalJournal of the American Chemical Society
Volume126
Issue number23
DOIs
StatePublished - Jun 16 2004

ASJC Scopus subject areas

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

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