Journal
MOLECULAR AND CELLULAR ENDOCRINOLOGY
Volume 286, Issue 1-2, Pages 35-39Publisher
ELSEVIER IRELAND LTD
DOI: 10.1016/j.mce.2007.09.009
Keywords
somatostatin receptors; receptor signaling; receptor internalization; receptor desensitization; somatostatin analogs; biased agonism; stimulus trafficking
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Funding
- NIDDK NIH HHS [R01 DK032234, R56 DK032234, DK-32234, R01 DK032234-21A1, R01 DK032234-20] Funding Source: Medline
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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. (C) 2007 Elsevier Ireland Ltd. All rights reserved.
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