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Somatostatin receptors.
Lars Neisig Møller1, Carsten Enggaard Stidsen, Bolette Hartmann
1Department of Medical Physiology, The Panum Institute, University of Copenhagen, DK-2200 Copenhagen, Denmark.
Biochimica Et Biophysica Acta
|September 26, 2003
Summary
Somatostatin (SRIF) and cortistatin (CST) bind to SRIF receptors, acting as endogenous ligands. This review details SRIF receptor subtypes, signal transduction, and complex co-operative functions, including dimerization, impacting physiology.
Area of Science:
- Neuroendocrinology
- Molecular Pharmacology
- Cell Biology
Background:
- Somatostatin (SRIF) was discovered in 1972, leading to the identification of its receptors.
- Cortistatin (CST), a neuropeptide resembling SRIF, was later found to bind to SRIF receptors, acting as a third endogenous ligand.
- SRIF receptors are G protein-coupled receptors (GPCRs) with seven transmembrane segments.
Purpose of the Study:
- To review the mechanisms of signal transduction, pharmacology, and anatomical distribution of somatostatin receptors (sst).
- To explore the complexity of SRIF receptor subtypes (sst(1)-sst(5), including sst(2A/2B) splice variants) and their differential expression.
- To discuss the concept of receptor co-operation, including homo- and heterodimerization, and its impact on overall cellular signaling.
Main Methods:
- Literature review of studies on somatostatin and cortistatin.
- Analysis of receptor cloning data for five SRIF receptor subtypes.
- Examination of research on signal transduction pathways and pharmacological profiles.
Main Results:
- Five SRIF receptor subtypes (sst(1)-sst(5)) have been identified, with sst(2) having splice variants.
- Receptor subtypes are differentially expressed and co-expressed in a cell-specific manner.
- Receptor co-operation, including dimerization, creates complex signaling units with unique pharmacological properties.
Conclusions:
- SRIF receptor function is not solely determined by individual subtypes but by their collective and co-operative activity.
- Understanding receptor dimerization and co-expression is crucial for comprehending integrated physiological responses.
- Development of SRIF analogues, including subtype-selective agents, offers therapeutic potential.