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Trends Biochem Sci. 1998 Nov;23(11):418-22.

Agonist-independent regulation of constitutively active G-protein-coupled receptors.

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Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Vrije Universiteit, The Netherlands.


G-protein-coupled receptors constitute one of the largest protein super-families in mammals. Since the cloning of the encoding genes, these important drug targets have been subjected to thorough biochemical and pharmacological studies. It has become clear that G-protein-coupled receptors not only transmit signals after stimulation by agonists but can also spontaneously couple to signal-transduction pathways. Recent findings show that constitutively active G-protein-coupled receptors can also be regulated in an agonist-independent manner, which has important implications for the interpretation of the actions of (inverse) agonists and the results of site-directed-mutagenesis studies.

[Indexed for MEDLINE]

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