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Abstract
Five specific receptor subtypes namely somatostatin receptor 1-5 (SSTR1-5) that are differentially expressed in central and peripheral tissue in selective manner have different role in many human pathological conditions. SSTRs possess seven-transmembrane spanning domains and are linked to G-proteins; therefore, belong to the superfamily of G-protein coupled receptors (GPCRs). There is a preponderance of evidence suggesting the importance of GPCR dimerization in receptor-biogenesis, regulation and pharmacology. SSTR subtypes dimerization, with specific interest on the formation of heterodimers within the family or other related receptors, generates novel receptors with unique pharmacological, biochemical and enhanced signaling properties distinct from those of the native receptor existing as monomers or dimers. An understanding of the molecular mechanisms involve in SSTR dimerization could offer a rationale in future drug design. Importantly, gaining insights on the structure, function and signaling pathways of SSTR subtypes would represent a major advance in improving the treatment of various diseases such as neurodegenerative diseases and the tumors of various origins. In addition to discuss the significance of SSTR subtypes homo-and heterodimerization in particular, this review first describes the concept of GPCRs dimerization and the role of key membrane associated signaling proteins.
Highlights
G-protein coupled receptors (GPCRs) constitute the largest members of cell surface transmembrane signaling proteins that exert critical role and form the basis of the most important signaling pathways
C known as the glutamate family includes metabotropic glutamate receptor family, the GABAB receptor and the calcium-sensing receptor (CaSR) and taste receptors (TRs) [1]
Somatostatin receptors homodimerization: The distributional pattern, presence of multiple receptors on a single cell and pharmacological properties of SSTR subtypes or other members of GPCRs family provide the first evidence that these receptors might function in a concert to enhance the receptor function or even might blunt the cell responses upon agonist binding
Summary
G-protein coupled receptors (GPCRs) constitute the largest members of cell surface transmembrane signaling proteins that exert critical role and form the basis of the most important signaling pathways. These two techniques have been used extensively to determine protein-protein interaction and contributed significantly to structure, function and regulation of GPCRs. the data discussed here regarding SSTR homo-and heterodimerization are generated by using pb-FRET analysis and classical biochemical methodologies.
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