Review
Function and regulation of the β3-adrenoceptor

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Abstract

The cloning, sequencing and expression in model systems of the previously unidentified β3-adrenoceptor recently led to an extensive functional characterization. Ligand binding and adenylate cyclase activation studies helped define a specific profile that is quite distinct from that of the β1- and β2-adrenoceptors, but strongly reminiscent of most of the ‘atypical’ β-adrenoceptor-mediated responses reported in earlier pharmacological studies. More recently, a naturally occurring variation in the human β3-adrenoceptor has been correlated with hereditary obesity and with increased dynamic capacity to add on weight and develop non-insulin dependent diabetes in Western obese patients. Donny Strosberg and France Pietri-Rouxel describe how results now provide a consistent picture of an important role for the human β3-adrenoceptor in the regulation of lipid metabolism and as an obvious target for drugs to treat some forms of obesity and diabetes.

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