药物基因组学和药物蛋白质组学杂志

抽象的

G-Protein Coupled Receptors Dimerization: Diversity in Somatostatin Receptors Subtypes

Ujendra Kumar

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.