Delineating Somatostatin's Neuronal Actions

Authors: Blake A.D.; Badway A.C.; Strowsk M.Z.

Source: Current Drug Targets-CNS & Neurological Disorders, Volume 3, Number 2, April 2004 , pp. 153-160(8)

Publisher: Bentham Science Publishers

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Abstract:

Somatostatin (somatotropin release inhibitory factor; SRIF) initiates its biological activity by interacting with a family of highly homologous integral membrane receptors (sst1 -sst5). SRIF neuronal actions regulate protein phosphorylation levels, control second messenger production and modulate neuronal membrane potential. Recently, our understanding of SRIF neurobiology has been driven by new pharmacological and molecular biological tools. SRIF receptor subtype specific antibodies have identified a distinctive, yet overlapping, expression pattern for this receptor family, with multiple subtypes co-localizing in the central and peripheral nervous system. This complex expression profile has confounded efforts to establish each receptor's role in the nervous system in part by the possible homo- and heteroligomerization of the receptor proteins. However, the recent discovery of SRIF receptor subtype selective ligands, supplemented by in vitro and in vivo models with inactivated SRIF receptor genes, now provides opportunities to clearly delineate each receptor's neuronal role. The convergence of these pharmacologic, immunologic and molecular biologic approaches extend our understanding of SRIF neurobiology while promising new therapeutic avenues for SRIF research.

Keywords: somatostatin; central nervous system; somatostatin receptors; non-peptidyl agonists; monophosphate; alzheimers disease; huntingtons disease; parkinsons disease; multiple sclerosis; epilepsy

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1568007043482534

Affiliations: 1: Department of Biology, Seton Hall University, South Orange, NJ 07079, USA.

Publication date: 2004-04-01

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CNS & Neurological Disorders - Drug Targets aims to cover all the latest and outstanding developments on the medicinal chemistry, pharmacology, molecular biology, genomics and biochemistry of contemporary molecular targets involved in neurological and central nervous system (CNS) disorders e.g. disease specific proteins, receptors, enzymes, genes. Each issue of the journal will contain a series of timely in-depth reviews written by leaders in the field covering a range of current topics on drug targets involved in neurological and CNS disorders. As the discovery, identification, characterization and validation of novel human drug targets for neurological and CNS drug discovery continues to grow; this journal will be essential reading for all pharmaceutical scientists involved in drug discovery and development.

Delineating Somatostatin's Neuronal Actions

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