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Characterisation of somatostatin sst2 receptor splice variants
1Glaxo Institute of Applied Pharmacology, Department of Pharmacology, University of Cambridge, UK.
Abstract:
Somatostatin is a peptide with a multitude of functions in the central nervous system and the periphery. It mediates its actions by binding to high-affinity G-protein coupled receptors, genes for five of which (sst1-sst5) have recently been cloned. The somatostatin sst2 receptor exists as two splice variants, sst2(a) and sst2(b) receptors, which differ in length and composition of their intracellular carboxy-termini. In this review, we describe the localisation of the two receptor isoforms in the central nervous system, the periphery and also in tumour tissue. Furthermore, we summarise and discuss the data on the functional properties of the recombinant splice variants that have been generated so far, which include activation of extracellular acidification rates, inhibition of adenylate cyclase and activation of MAP-kinases as well as the transcription factor Elk-1.