Literature DB >> 12511609

Somatostatin receptor subtype 5 regulates insulin secretion and glucose homeostasis.

Mathias Z Strowski1, Martin Kohler, Howard Y Chen, Myrna E Trumbauer, Zhihua Li, Deborah Szalkowski, Shobhna Gopal-Truter, Jill K Fisher, James M Schaeffer, Allan D Blake, Bei B Zhang, Hilary A Wilkinson.   

Abstract

Somatostatin (SRIF) regulates pancreatic insulin and glucagon secretion. In the present study we describe the generation of SRIF receptor subtype 5 knockout (sst(5) KO) mice to examine the role of SRIF receptor subtypes (sst) in regulating insulin secretion and glucose homeostasis. Mice deficient in sst(5) were viable, fertile, appeared healthy, and displayed no obvious phenotypic abnormalities. Pancreatic islets isolated from sst(5) KO mice displayed increased total insulin content as compared with islets obtained from wild-type (WT) mice. Somatostatin-28 (SRIF-28) and the sst(5)/sst(1)-selective agonist compound 5/1 potently inhibited glucose-stimulated insulin secretion from WT islets. SRIF-28 inhibited insulin secretion from sst(5) KO islets with 16-fold less potency while the maximal effect of compound 5/1 was markedly diminished when compared with its effects in WT islets. sst(5) KO mice exhibited decreased blood glucose and plasma insulin levels and increased leptin and glucagon concentrations compared with WT mice. Furthermore, sst(5) KO mice displayed decreased susceptibility to high fat diet-induced insulin resistance. The results of these studies suggest sst(5) mediates SRIF inhibition of pancreatic insulin secretion and contributes to the regulation of glucose homeostasis and insulin sensitivity. Our findings suggest a potential beneficial role of sst(5) antagonists for alleviating metabolic abnormalities associated with obesity and insulin resistance.

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Year:  2003        PMID: 12511609     DOI: 10.1210/me.2001-0035

Source DB:  PubMed          Journal:  Mol Endocrinol        ISSN: 0888-8809


  23 in total

1.  Discovery and Pharmacology of a Novel Somatostatin Subtype 5 (SSTR5) Antagonist: Synergy with DPP-4 Inhibition.

Authors:  Weiguo Liu; Pengcheng P Shao; Gui-Bai Liang; John Bawiec; Jiafang He; Susan D Aster; Margaret Wu; Garry Chicchi; John Wang; Kwei-Lan Tsao; Jin Shang; Gino Salituro; Yun-Ping Zhou; Cai Li; Taro E Akiyama; Daniel E Metzger; Beth Ann Murphy; Andrew D Howard; Ann E Weber; Joseph L Duffy
Journal:  ACS Med Chem Lett       Date:  2018-09-12       Impact factor: 4.345

Review 2.  International Union of Basic and Clinical Pharmacology. CV. Somatostatin Receptors: Structure, Function, Ligands, and New Nomenclature.

Authors:  Thomas Günther; Giovanni Tulipano; Pascal Dournaud; Corinne Bousquet; Zsolt Csaba; Hans-Jürgen Kreienkamp; Amelie Lupp; Márta Korbonits; Justo P Castaño; Hans-Jürgen Wester; Michael Culler; Shlomo Melmed; Stefan Schulz
Journal:  Pharmacol Rev       Date:  2018-10       Impact factor: 25.468

Review 3.  The role of somatostatin analogs in Cushing's disease.

Authors:  Joost van der Hoek; Steven W J Lamberts; Leo J Hofland
Journal:  Pituitary       Date:  2004       Impact factor: 4.107

4.  Somatostatin receptor subtype 5 modifies hypothalamic-pituitary-adrenal axis stress function.

Authors:  Masaaki Yamamoto; Anat Ben-Shlomo; Hiraku Kameda; Hidenori Fukuoka; Nan Deng; Yan Ding; Shlomo Melmed
Journal:  JCI Insight       Date:  2018-10-04

5.  Subtype selective interactions of somatostatin and somatostatin analogs with sst1, sst2, and sst5 in BON-1 cells.

Authors:  Eva Ludvigsen; Mats Stridsberg; John E Taylor; Michael D Culler; Kjell Oberg; Eva T Janson
Journal:  Med Oncol       Date:  2004       Impact factor: 3.064

6.  Microarray analysis of somatostatin receptor 5-regulated gene expression profiles in murine pancreas.

Authors:  Sanjeet G Patel; Guisheng Zhou; Shi-He Liu; Min Li; Jae-Wook Jeong; Francesco J DeMayo; Marie-Claude Gingras; Richard A Gibbs; William E Fisher; F Charles Brunicardi
Journal:  World J Surg       Date:  2009-04       Impact factor: 3.352

7.  Identification of a congenic mouse line with obesity and body length phenotypes.

Authors:  Craig H Warden; Steven Stone; Sally Chiu; Adam L Diament; Pablo Corva; Donna Shattuck; Robyn Riley; Steven C Hunt; Juliet Easlick; Janis S Fisler; Juan F Medrano
Journal:  Mamm Genome       Date:  2004-06       Impact factor: 2.957

Review 8.  Somatostatin-dopamine ligands in the treatment of pituitary adenomas.

Authors:  Alexandru Saveanu; Philippe Jaquet
Journal:  Rev Endocr Metab Disord       Date:  2008-07-24       Impact factor: 6.514

Review 9.  Use of somatostatin analogues in obesity.

Authors:  Themistoklis Tzotzas; Kostas Papazisis; Petros Perros; Gerasimos E Krassas
Journal:  Drugs       Date:  2008       Impact factor: 9.546

10.  SSTR2 is the functionally dominant somatostatin receptor in human pancreatic β- and α-cells.

Authors:  Balrik Kailey; Martijn van de Bunt; Stephen Cheley; Paul R Johnson; Patrick E MacDonald; Anna L Gloyn; Patrik Rorsman; Matthias Braun
Journal:  Am J Physiol Endocrinol Metab       Date:  2012-08-28       Impact factor: 4.310

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