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Mol Cell Endocrinol. 2008 May 14;286(1-2):35-9. Epub 2007 Oct 7.

Selective agonism in somatostatin receptor signaling and regulation.

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Department of Integrative Biology and Pharmacology, University of Texas-Houston, School of Medicine, Houston, TX 77225, USA.


The five somatostatin receptor subtypes, named sst1-sst5, activate both distinct and common signaling pathways and exhibit different patterns of receptor regulation. Until recently it was believed that once a particular somatostatin receptor was activated by an agonist, all the down-stream signaling and regulatory effects characteristic of that receptor subtype in that cellular environment would be triggered. Thus, differences in the actions of somatostatin analogs between tissues were attributed to variability in the nature and concentration of the sst receptor subtypes and effectors expressed in different targets. However, agonists have recently been shown to exhibit functional selectivity at individual sst receptors such that they can elicit a subset of that receptor's potential effects, a property known as biased agonism. This review will summarize the evidence for functionally selective somatostatin receptor agonists and discuss the implications and promise of these new findings.

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