Classification and nomenclature of somatostatin receptors

Hoyer, Daniel; Bell, G. I.; Berelowitz, Michael; Epelbaum, Jacques; Feniuk, W.; Humphrey, P. P. A.; O’Carroll, Anne-Marie; Patel, Yogesh C.; Schönbrunn, Agnes; Taylor, J. E.; Reisine, Terry

doi:10.1016/s0165-6147(00)88988-9

Cited by 533 publications

(351 citation statements)

References 23 publications

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“…Its biological actions are mediated by receptors belonging to the G-protein-coupled receptor (GPCR) family. Five SRIF receptor subtypes, termed somatostatin receptor (sst) 1-sst5, have been identified in mammals, with two splice variants of sst2 in mouse and rat, sst2A and sst2B (Hoyer et al, 1995). Sst1-sst4 are highly expressed in the cortex whereas sst5 receptor immunoreactivity is only sparsely present in neuronal perikarya and proximal dendrites limited to the rostral part of the brain (Stroh et al, 2000).…”

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confidence: 99%

Minocycline provides protection against β-amyloid(25-35)-induced alterations of the somatostatin signaling pathway in the rat temporal cortex

2008

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Minocycline provides protection against β-amyloid(25-35)-induced alterations of the somatostatin signaling pathway in the rat temporal cortex

2008

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“…We determined whether receptor-speci®c peptide phage could speci®cally bind to cells expressing the 7-TM receptor for the hormone, and, whether interaction was su cient for its selection via cell panning, and whether detection via ELISA or FACS was feasible. Further, in view of developing functional screening assays, the triggering activity of the phage particles on receptor function was tested.Somatostatin is a multifunctional peptide hormone, which regulates key cellular processes such as secretion, neurotransmission and proliferation, through interaction with at least ®ve somatostatin receptors (Somatostatin and its receptors, 1995;Hoyer et al, 1995). The ®ve cloned sst, all G protein-coupled seven-transmembrane receptors which are homologous in the transmembrane domains of the di erent receptor subtypes, appear to have similar pharmacological properties.…”

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“…Some antibodies have been made that recognize the denatured form of one of the ®ve receptors (Theveniau et al, 1994;Schonbrunn et al, 1995), but none recognize the native receptor on the cell surface. Sst subtype speci®c agonists have emerged recently, but subtype speci®c antagonists have not yet been identi®ed (Hoyer et al, 1995).We have built a model, using somatostatin and its receptors, that establish methods to display the hormone on phage, and procedures for cell panning of phage libraries, binding assays, and receptor activation assays. Somatostatin was displayed on the surface of phage particles via fusion to pIII and pVIII phage coat proteins.…”

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Somatostatin displayed on filamentous phage as a receptor‐specific agonist

Rousch

Lutgerink

Coote

et al. 1998

British J Pharmacology

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1 In search of methods to identify bio-active ligands speci®c for G protein-coupled receptors with seven transmembrane spanning regions, we have developed a ®lamentous phage-based selection and functional screening method. 2 First, methods for panning peptide phage on cells were established, using the hormone somatostatin as a model. Somatostatin was displayed on the surface of ®lamentous phage by cloning into phage(mid) vectors and fusion to either pIII or pVIII viral coat proteins. Peptide displaying phage bound to a polyclonal anti-somatostatin serum, and, more importantly, to several somatostatin receptor subtypes (Sst) expressed on transfected CHO-K1 cells, in a pattern which was dependent on the used display method. Binding was competed with somatostatin, with an IC50 in the nanomolar range. The phage were speci®cally enriched by panning on cells, establishing conditions for cell selections of phage libraries.3 Binding of somatostatin displaying phage to sst 2 on a reporter cell line, in which binding of natural ligand reduces secretion of alkaline phosphatase (via a cyclic AMP responsive element sensitive promoter), proved that the phage particles act as receptor-speci®c agonists. Less than 100 phage particles per cell were required for this activity, which is approximately 1000 fold less than soluble somatostatin, suggesting that phage binding interferes with normal receptor desensitization and/or recycling. 4 The combination of biopanning of phage libraries on cells with functional screening of phage particles for receptor triggering activity, may be used to select novel, bio-active ligands from phage libraries of random peptides, antibody fragments, or libraries based on the natural receptor ligand. Keywords: Filamentous phage; phage display; somatostatin receptors; G-protein coupled receptors; immunochemical detection; functional agonist; phage selection; receptor agonist IntroductionIn peptide phage display, methods to create vast libraries of peptide variants are linked to powerful selection strategies to isolate peptide ligands binding to any chosen antigen, including receptors, enzymes or viruses (Scott & Smith., 1990;Cwirla et al., 1990;Devlin et al., 1990;Winter et al., 1994). Its success hinges on the availability of highly puri®ed preparations of antigen, and on the development of very sensitive screening methods for testing the selected peptides. Indeed, peptides speci®c for many globular proteins or peptides (Cwirla et al., 1990;Devlin et al., 1990) and puri®ed domains of cell surface receptors (Doorbar & Winter 1994;Livnah et al., 1996) have been selected. Selections on impure antigens are signi®cantly more di cult, due to the problem of enriching phage peptides speci®c for non-relevant structures. This makes the procedure particularly di cult for membrane receptors, that may either not be puri®ed in quantities required for phage panning, or for which the target area is de®ned by multiple transmembrane regions. Nevertheless, there is a large group of receptors, the G-protein coupled recepto...

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“…SRIF mediates a variety of physiological and behavioral actions by interacting with five somatostatin receptor subtypes (sst 1-5 ; Hoyer et al, 1995). In the NAc, the sst 1 receptor has been reported to be an autoreceptor for SRIF (Vasilaki et al, 2004;Thermos et al, 2006), whereas the sst 2 receptor appears to be responsible for the actions of SRIF on dopamine release and dopaminemediated behaviors (Raynor et al, 1993;Thermos et al, 1996;Hathway et al, 1999).…”

Section: Introductionmentioning

confidence: 99%

Antidepressants Influence Somatostatin Levels and Receptor Pharmacology in Brain

Pallis

Vasilaki

Fehlmann

et al. 2008

Neuropsychopharmacol

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This study investigated how the administration (acute and chronic) of the antidepressants citalopram and desmethylimipramine (DMI) influences somatostatin (somatotropin release inhibitory factor, SRIF) levels and SRIF receptor density (sst 1-5 ) in rat brain. Animals received either of the following treatments: (1) saline for 21 days (control group), (2) saline for 20 days and citalopram or DMI for 1 day (citalopram or DMI acute groups), (3) citalopram or DMI for 21 days (citalopram or DMI chronic groups). Somatostatin levels were determined by radioimmunoassay. [ 125 I]LTT SRIF-28 binding in the absence (labeling of sst 1-5 ) or presence of 3 nM MK678 (labeling of sst 1/4 ) and [ 125 I]Tyr 3 octreotide (labeling of sst 2/5 ) binding with subsequent autoradiography was performed in brains of rats treated with both antidepressants. Somatostatin levels were increased after citalopram, but not DMI administration, in the caudate-putamen, hippocampus, nucleus accumbens, and prefrontal cortex. Autoradiography studies illustrated a significant decrease in receptor density in the superficial and deep layers of frontal cortex (sst 2 ), as well as a significant increase in the CA1 (sst 1/4 ) hippocampal field in brains of chronically citalopram-treated animals. DMI administration increased sst 1/4 receptors levels in the CA1 hippocampal region. These results suggest that citalopram and to a lesser extent DMI influence the function of the somatostatin system in brain regions involved in the emotional, motivational, and cognitive aspects of behavior.

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Classification and nomenclature of somatostatin receptors

Cited by 533 publications

References 23 publications

Minocycline provides protection against β-amyloid(25-35)-induced alterations of the somatostatin signaling pathway in the rat temporal cortex

Minocycline provides protection against β-amyloid(25-35)-induced alterations of the somatostatin signaling pathway in the rat temporal cortex

Somatostatin displayed on filamentous phage as a receptor‐specific agonist

Antidepressants Influence Somatostatin Levels and Receptor Pharmacology in Brain

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