Informed development of drugs acting at Family B G protein-coupled receptors

Research output: Chapter in Book/Report/Conference proceedingConference contribution

2 Scopus citations


Rational refinement and development of receptor-active ligands can come from high-resolution insights into the structures of these potential drug targets. Structural insights for Family A G protein-coupled receptors (GPCRs) have been advanced substantially with the recently reported crystal structure of the intact β2-adrenergic receptor. While high-resolution structural insights for Family B GPCRs are also advancing, this is currently limited to the functionally important extracellular amino-terminal tail domain of those receptors. The current report describes how these structures can provide leads for the development of small-molecule agonist drugs acting at Family B GPCRs. Endogenous agonist activity within the amino terminus of these receptors could be key for the development of such drugs.

Original languageEnglish (US)
Title of host publicationNeural Signaling Opportunities for Novel Diagnostic Approaches and Therapies
PublisherBlackwell Publishing Inc.
Number of pages7
ISBN (Print)9781573317047
StatePublished - Nov 2008

Publication series

NameAnnals of the New York Academy of Sciences
ISSN (Print)0077-8923
ISSN (Electronic)1749-6632


  • Activation mechanisms
  • G protein-coupled receptors
  • Ligand binding
  • Receptor structure
  • Secretin receptor

ASJC Scopus subject areas

  • Neuroscience(all)
  • Biochemistry, Genetics and Molecular Biology(all)
  • History and Philosophy of Science


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