Characterization of pancreatic somatostatin binding sites with a 125I-somatostatin 28 analog

Zeggari, M.; Viguerie, Nathalie; Susini, C.; Estève, Jean-Pierre; Vaysse, Nicole; Rivier, Jean; Wünsch, E; Ribet, A

doi:10.1016/0196-9781(86)90120-8

Cited by 17 publications

(14 citation statements)

References 27 publications

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“…The two radioligands S14 and S28 covalently labelled the same species on gel filtration columns, confirming binding results which demonstrated that the two radioligands interact with the same binding site [7,13]. SDS-PAGE analysis of membrane cross-linked receptors by three heterobifunctional reagents, ANB-NOS, N-succinimidyl 6-(azido-2'-nitropheny1amine)hexanoate and N-hydroxy-succinimidyl-4-azidobenzoate resulted in the labelling of a specific 88-kDa protein which displayed properties of the somatostatin receptor.…”

Section: Discussionsupporting

confidence: 66%

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Solubilization and characterization of guinea‐pig pancreatic somatostatin receptors

Zeggari

Viguerie

Susini

et al. 1987

European Journal of Biochemistry

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The solubilization of somatostatin receptors from guinea-pig pancreas by different non-denaturing detergents was investigated after stabilization of the receptors by prior binding of '"I-[Tyr' ']somatostatin or its analogue '251-[Leu8,~Trp22,Tyr25]somatostatin 28, to pancreatic plasma membranes.The somatostatin-receptor complexes were solubilized in a high yield by Zwittergent 3-14 (3-[tetradecyldimethylammoniol-1-propanesulfonate), a zwitterionic detergent. Other detergents, digitonin, Triton X-100, Chaps (3-[cholamidopropyldimethylammonio]-1 -propanesulfonate) and octyl P-D-glycopyranoside, achieved only partial solubilization. The recovery of receptor complexes was increased by glycerol.In order to characterize solubilized somatostatin-receptor complexes, membranes receptors were covalently labelled using N-5-azido-2-nitrobenzoyloxysuccinimide as cross-linking reagent before solubilization. Gel filtration chromatography analysis resulted in the identification of a major protein component of apparent MI = 93 000 which interacted with the two radioligands.In The solubilized somatostatin-receptor complex was adsorbed to wheat-germ agglutinin-agarose column and eluted by specific sugars.We concluded that the guinea-pig pancreatic somatostatin receptor in the membrane and in the non-denaturing detergent solution behaves as a protein monomer of apparent M I % 85000-90000. The somatostatin receptor is a glycoprotein which contains complex-type carbohydrate chains.Somatostatin, a tetradecapeptide (SI4) initially isolated from hypothalamus as an inhibitor of growth hormone secretion, has been found to exert inhibitory actions on various cellular processes in the central nervous system, gastrointestinal tract and pancreas [l]. High-affinity binding sites for somatostatin have been detected on plasma membranes or intact cells from various tissues including brain [2, 31, pituitaries [4, 51, adrenal cortex 16, 71 and endocrine pancreas [8]. We have recently demonstrated that pancreatic acinar cells possess specific somatostatin receptors [9, 101 which are involved in the inhibitory effect of the peptide on secretinstimulated cellular cyclic AMP [ll].

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Section: Discussionsupporting

confidence: 66%

“…We used two radioligands 1251-[Tyr' ']somatostatin and its analogue, 51-[Leu8,~TrpZ ',Tyr2 5]somatostatin 28 which have been demonstrated to interact with the same somatostatin binding sites [7,13,141. The Zwittergent 3-14 was found to be the most powerful detergent to solubilize labelled somatostatin receptors.…”

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confidence: 99%

Solubilization and characterization of guinea‐pig pancreatic somatostatin receptors

Zeggari

Viguerie

Susini

et al. 1987

European Journal of Biochemistry

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“…The inhibitory actions of SS-14 and SS-28 are initiated after binding to high-affinity receptors that have been identified on target tissues (5)(6)(7)(8)(9). SS-14 and SS-28 appear to exert their inhibitory effects by a dual mechanism involving receptor activation of Gi, the inhibitory guanine nucleotide-binding protein (10).…”

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confidence: 99%

Molecular cloning and functional expression of a brain-specific somatostatin receptor.

Bruno

Song

et al. 1992

Proc. Natl. Acad. Sci. U.S.A.

251

136

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The PCR and conventional library screening were used to clone the brain-specific somatostatin receptor rSSTR-4 from a rat genomic library. The deduced amino add sequence encodes a protein of 384 amino acids and displays structural and sequence homologies with members of the G protein-receptor superfamily. The , a cyclic tetradecapeptide, was originally isolated from ovine hypothalamus and found to have potent inhibitory effects on growth hormone and thyroidstimulating hormone secretion from the anterior pituitary (1, 2). SS-14 was subsequently found to have a widespread distribution, occurring primarily in the central nervous system and gut, where it exerts inhibitory effects on secretion, both exocrine and endocrine, as well as on neural function (3). As with many small peptides, SS-14 is synthesized as part of a larger precursor molecule, from which the mature hormone is proteolytically processed. In mammals, a single gene encodes the 92-amino acid common precursor to both SS-14 and somatostatin 28 (SS-28), a second biologically active NH2-terminally extended form of the tetradecapeptide (4).The inhibitory actions of SS-14 and SS-28 are initiated after binding to high-affinity receptors that have been identified on target tissues (5-9). SS-14 and SS-28 appear to exert their inhibitory effects by a dual mechanism involving receptor activation of Gi, the inhibitory guanine nucleotide-binding protein (10). In part, their effects are mediated through inhibition of stimulated adenylyl cyclase activity and reduction of cAMP production (11, 12). In addition, both peptides cause membrane hyperpolarization through effects on a voltage-dependent plasma-membrane potassium channel, leading to a decrease in Ca2+ influx and a reduction of cytosolic Ca2+ concentration (13

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“…Somatostatin exerts its biological effects by binding to specific membrane receptors (6)(7)(8). High-affinity somatostatin receptors (SSTRs) have been demonstrated in various tissues such as different brain regions, pancreas, adrenal cortex, and several tumors [e.g., endocrine breast, lung, or brain tumors (9)(10)(11)(12)].…”

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Cloning and characterization of a fourth human somatostatin receptor.

Rohrer

Raulf

Berthou

et al. 1993

Proc. Natl. Acad. Sci. U.S.A.

187

103

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We have isolated a gene coding for a fourth human somatostatin (somatotropin release-inhibiting factor) receptor. This additional somatostatin receptor (hSSTR4) is specifically expressed in human fetal and adult brain and lung tissue. The deduced amino acid sequence of the receptor displays both sequence and structural homology to three cloned somatostatin receptors as well as to other members of the family of GTP-binding-protein-coupled seven-helix transmembrane-spanning receptors. Pharmacological characterization of the expressed receptor reveals specific, high-affmity binding of somatostatin 14 and somatostatin 28. Surprisingly, several well-characterized synthetic somatostatin analogs fail to exhibit high-affinity binding to hSSTR4, indicating the existence of pharmacologically different receptor subtypes. Our data suggest that the diverse biological effects exerted by somatostatin are mediated by a family of receptors with discrete patterns of expression and different pharmacological properties.

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Characterization of pancreatic somatostatin binding sites with a 125I-somatostatin 28 analog

Cited by 17 publications

References 27 publications

Solubilization and characterization of guinea‐pig pancreatic somatostatin receptors

Solubilization and characterization of guinea‐pig pancreatic somatostatin receptors

Molecular cloning and functional expression of a brain-specific somatostatin receptor.

Cloning and characterization of a fourth human somatostatin receptor.

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