An endogenous ligand for the central sulfonylurea receptor

Virsolvy, Anne; Brück, Monika; Dufour, Marie Noëlle; Cauvin, Annick; Lupo, B.; Bataille, D.

doi:10.1016/0014-5793(88)80986-4

Cited by 25 publications

(16 citation statements)

References 12 publications

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“…Heron et al (1998) recently reported that ␣-endosulfine may act as an endogenous regulator of ␤-cell K ATP channel activity and insulin secretion. ␣-Endosulfine is a peptide that was purified from bovine brain in the quest for an endogenous ligand for the SUR in brain (Virsolvy-Vergine et al, 1988). In the present study, we have shown that the endogenous ligand for PPAR-␥ 15-deoxy-⌬ 12,14 -PGJ 2 may bind to SUR and inhibit K ATP channels.…”

Section: Discussionmentioning

confidence: 54%

Fenofibrate, Troglitazone, and 15-Deoxy-Δ^12,14-prostaglandin J₂Close K_ATPChannels and Induce Insulin Secretion

Shimomura

Shimizu²,

Ikeda³

et al. 2004

J Pharmacol Exp Ther

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It is known that peroxisome proliferator-activated receptor-␥ (PPAR-␥) ligands stimulate acute-phase insulin secretion with a rapid Ca 2ϩ influx into pancreatic ␤-cells, but the precise mechanisms are not clear. The effects of PPAR-␣ ligands on pancreatic ␤-cells also remain unclear. We investigated the effects of PPAR-␣ ligands (fenofibrate and fenofibric acid), a PPAR-␥ ligand (troglitazone), and an endogenous ligand of PPAR-␥ [15-deoxy-⌬ 12,14 -prostaglandin J 2 (15-deoxy-⌬ 12,14 -PGJ 2 )] on K ATP channel activity in clonal hamster insulinoma cell line, HIT-T15 cells. As assessed by whole-cell patch clamp, fenofibrate, fenofibric acid, troglitazone, and 15-deoxy-⌬ 12,14 -PGJ 2 reduced the K ATP channel currents, and inhibition continued after washout of these agents. The concentration-response curves of fenofibrate, fenofibric acid, troglitazone, and 15-deoxy-⌬ 12,14

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Section: Discussionmentioning

confidence: 54%

Fenofibrate, Troglitazone, and 15-Deoxy-Δ^12,14-prostaglandin J₂Close K_ATPChannels and Induce Insulin Secretion

Shimomura

Shimizu²,

Ikeda³

et al. 2004

J Pharmacol Exp Ther

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“…Tissues from adult Wistar rats were boiled and extracted in 10 ml 0.5 mol/l acetic acid for each gram of tissue, as previously described [12]. Rat blood samples were collected into glass tubes containing EDTA (15%) and 250 KIU aprotinin (Interchim, Montlucon, France) and centrifuged at 800 g for 10 min at 4°C.…”

Section: Methodsmentioning

confidence: 99%

Localization of α-endosulphine in pancreatic somatostatin δ cells and expression during rat pancreas development

et al. 2002

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Aims/hypothesis. α-Endosulphine, a protein that belongs to the cAMP-regulated-phosphoprotein family, has been reported to modulate insulin secretion in vitro through interaction with the pancreatic beta-cell ATP-sensitive potassium (K ATP ) channel. In this study, we analysed the tissue distribution of α-endosulphine and determined its pancreatic cellular localization. Methods. Quantitative tissue distribution of α-endosulphine was studied by RIA on tissue extracts and cellular/subcellular localization was done using immunocytochemistry, morphometry and western blot analysis. α-Endosulphine and somatostatin release from RINT-3 somatostatin-secreting cells was quantified by RIA. Results. α-Endosulphine, concentrated particularly in the central nervous system, was also detected in a wide variety of tissues including the pancreas. Immunohistochemistry analysis of adult rat pancreatic sections showed that α-endosulphine localized in somatostatin δ cells, where its expression increased during post-natal development. Immunoreactive cells were detected from foetal age E19, and the number of somatostatin cells co-expressing α-endosulphine increased with developmental age from E19 until adult. α-Endosulphine, highly expressed in the cytoplasm of RINT3 somatostatin-secreting cell line, was recovered in the particulate fraction of RINT3 cell extracts but was not co-secreted with somatostatin. Conclusion/interpretation. α-Endosulphine is expressed in all tissues tested including pancreas and is also detected in plasma. Pancreatic α-endosulphine is specifically localized in somatostatin δ cells. This cytosolic protein is not co-secreted with somatostatin and could be physically associated with particulate components of the cells. These findings are not in favour of an endocrine/paracrine effect of α-endosulphine on the beta-cell K ATP channel. [Diabetologia (2002) 45:703-710]

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“…1C). When comparing these data to those obtained with rat brain extracts (23), the following observations may be made: (i) from both aliphatic bonded phases, rat (22) and ovine (see Fig. 1 A and B) endosulfines were eluted as a main peak; (ii) rat and ovine endosulfines displayed slightly different retention times in these systems (see Fig.…”

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confidence: 97%

“…In the CNS, the potential endogenous ligand is likely to be present near the receptor. We have shown that such a ligand exists in the rat brain (22). We describe the presence in and the purification from ovine brain of two peptides, representing most likely two forms of the same entity, for which we propose the name "'endosulfine.…”

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confidence: 99%

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Endosulfine, an endogenous peptidic ligand for the sulfonylurea receptor: purification and partial characterization from ovine brain.

Virsolvy

Leray

Kuroki

et al. 1992

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

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Antidiabetic sulfonylureas act through receptors coupled to ATP-dependent potassium channels. Using the binding of [3Hjglibenclamide, a highly potent sulfonylurea, to rat brain membranes to follow the purification procedure, we extracted from ovine brain, purified, and partially characterized two peptides that are endogenous ligands for the central nervous system sulfonylurea receptors. These peptides, referred to as a and (3 endosulfme, differ by their isoelectric points, the (3 form being more basic. Each form of endosulfine is recognized equally by the sulfonylurea receptors from the central nervous system and from insulin-secreting m3 cells. In the same concentration range that is active on the receptors, 13 endosulfine releases insulin from a 13-cell line. Endosulfine is a good candidate for being implicated in the physiology of 13 cells and their disorders (e.g., type H diabetes) and in certain pathologies related to modifications of ion fluxes.The antidiabetic sulfonylureas (1) are widely used in the management of non-insulin-dependent diabetes mellitus (NIDDM), also referred to as type II diabetes (2). These drugs (3, 4) stimulate insulin secretion from the islets of Langerhans, which in diabetes display a decreased insulin content (5) and an impaired response to glucose (6). The sulfonylureas act at the cell surface of the 13 cell (7) through interaction with specific binding sites (or receptors) present in membranes from insulin-secreting cells or tissues (8-13). Receptors with similar characteristics were also observed in the central nervous system (CNS; refs. 10,14,and 15) and in the myocardial tissue (16). The sulfonylurea receptor is closely associated to ATP-dependent potassium channels (17-19), also involved in glucose-induced insulin secretion (20). The existence of such a receptor led us to suggest that it represents a recognition site for an endogenous ligand (14) that would regulate physiological processes through mechanisms triggered, in a pharmacological context, by the sulfonylureas. Such an approach for the binding sites for morphine led to the discovery of the endorphines (21). In the CNS, the potential endogenous ligand is likely to be present near the receptor. We have shown that such a ligand exists in the rat brain (22). We describe the presence in and the purification from ovine brain of two peptides, representing most likely two forms of the same entity, for which we propose the name "'endosulfine. " Endosulfine is present in the brain of rat and sheep at similar concentrations-i.e., ca 0.1 pmol of glibenclamide equivalent per g of tissue-and in the rat pancreas. Highly purified endosulfine is like sulfonylureas in that, at concentrations where it interacts with the receptors, it is able to induce insulin release from JTC cells in culture.MATERIALS AND METHODS Sulfonylureas. Glibenclamide was provided by the Guidotti laboratory.[3H]Glibenclamide (40)(41)(42)(43)(44)(45)(46)(47)(48)(49)(50) Ci/mmol; 1 Ci = 37 GBq) was purchased from Hoechst Pharmaceuticals or DuPont.Binding ...

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An endogenous ligand for the central sulfonylurea receptor

Cited by 25 publications

References 12 publications

Fenofibrate, Troglitazone, and 15-Deoxy-Δ^12,14-prostaglandin J₂Close K_ATPChannels and Induce Insulin Secretion

Fenofibrate, Troglitazone, and 15-Deoxy-Δ^12,14-prostaglandin J₂Close K_ATPChannels and Induce Insulin Secretion

Localization of α-endosulphine in pancreatic somatostatin δ cells and expression during rat pancreas development

Endosulfine, an endogenous peptidic ligand for the sulfonylurea receptor: purification and partial characterization from ovine brain.

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An endogenous ligand for the central sulfonylurea receptor

Cited by 25 publications

References 12 publications

Fenofibrate, Troglitazone, and 15-Deoxy-Δ12,14-prostaglandin J2Close KATPChannels and Induce Insulin Secretion

Fenofibrate, Troglitazone, and 15-Deoxy-Δ12,14-prostaglandin J2Close KATPChannels and Induce Insulin Secretion

Localization of α-endosulphine in pancreatic somatostatin δ cells and expression during rat pancreas development

Endosulfine, an endogenous peptidic ligand for the sulfonylurea receptor: purification and partial characterization from ovine brain.

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Fenofibrate, Troglitazone, and 15-Deoxy-Δ^12,14-prostaglandin J₂Close K_ATPChannels and Induce Insulin Secretion

Fenofibrate, Troglitazone, and 15-Deoxy-Δ^12,14-prostaglandin J₂Close K_ATPChannels and Induce Insulin Secretion