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Trends Biochem Sci. 2008 Jul;33(7):314-9. doi: 10.1016/j.tibs.2008.05.001. Epub 2008 Jun 12.

Class-B GPCR activation: is ligand helix-capping the key?

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  • 1CEA, Institut de Biologie et Technologies de Saclay, URA CNRS 2096, Laboratoire des ProtĂ©ines Membranaires, 91191Gif sur Yvette Cedex, France.


The class B family of G-protein-coupled receptors (GPCRs) regulates essential physiological functions such as exocrine and endocrine secretions, feeding behaviour, metabolism, growth, and neuro- and immuno-modulations. These receptors are activated by endogenous peptide hormones including secretin, glucagon, vasoactive intestinal peptide, corticotropin-releasing factor and parathyroid hormone. We have identified a common structural motif that is encoded in all class B GPCR-ligand N-terminal sequences. We propose that this local structure, a helix N-capping motif, is formed upon receptor binding and constitutes a key element underlying class B GPCR activation. The folded backbone conformation imposed by the capping structure could serve as a template for a rational design of drugs targeting class B GPCRs in several diseases.

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