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Type 2 Diabetes Mellitus and Glucagon Like Peptide-1 Receptor Signalling

Kanamarlapudi Aiysha Thompson, Venkat Kanamarlapudi Orcid Logo

Clinical & Experimental Pharmacology, Volume: 03, Issue: 04

Swansea University Author: Venkat Kanamarlapudi Orcid Logo

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DOI (Published version): 10.4172/2161-1459.1000138

Abstract

It has been estimated that approximately 8.4% of the world population currently live with diabetes mellitus and type 2 diabetes is the most common form. Type 2 diabetes increases the risk of complications such as heart attacks, blindness, amputations and kidney failure. Glucagon like Peptide-1 (GLP-...

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Published in: Clinical & Experimental Pharmacology
ISSN: 21611459
Published: 2013
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URI: https://cronfa.swan.ac.uk/Record/cronfa27395
first_indexed 2016-04-23T01:11:41Z
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spelling 2016-05-10T10:55:41.9107469 v2 27395 2016-04-22 Type 2 Diabetes Mellitus and Glucagon Like Peptide-1 Receptor Signalling 63741801137148abfa4c00cd547dcdfa 0000-0002-8739-1483 Venkat Kanamarlapudi Venkat Kanamarlapudi true false 2016-04-22 MEDS It has been estimated that approximately 8.4% of the world population currently live with diabetes mellitus and type 2 diabetes is the most common form. Type 2 diabetes increases the risk of complications such as heart attacks, blindness, amputations and kidney failure. Glucagon like Peptide-1 (GLP-1) is an effective insulinotropic agent and therefore its effects on insulin secretion have been greatly examined for more than two decades. It is a polypeptide hormone secreted by the intestinal L-cells into the blood in response to food uptake. GLP-1 has a very short half-life in vivo due to the rapid proteolytic degradation by Dipeptidyl Peptidase IV (DPP-IV). Therefore DPP-IV resistant GLP-1 analogues, Exenatide and Liraglutide, have been developed and are currently being used in the treatment of type 2 diabetes. GLP-1 agonist functions by binding to its receptor, GLP1R, on the cell surface.The GLP-1R belongs to the class B peptide receptor family based on its structure and function. The binding of GLP-1 to its receptor results in activation of Gαs coupled adenylyl cyclase and the production of cyclic Adenosine Monophosphate (cAMP), which enhances glucose-induced insulin secretion. Continuous GLP-1R activation also causes insulin secretion and pancreatic islet β-cell proliferation and neogenesis. The GLP-1R is internalised following its activation, which regulates the biological responsiveness of the receptor. Structurally the GLP-1R contains a large N-terminal extracellular domain (TM1-TM7) joined by three intracellular loops (ICL1, ICL2, ICL3) and three extracellular loops (ECL1, ECL2, ECL3), and an intracellular C-terminal domain. These domains play critical roles in GLP-1R trafficking to the cell surface, and also in agonist dependent activation and internalisation of the receptor. This review is focused on type 2 diabetes, its treatment with GLP-1, GLP-1R structure and function, and the physiological affects resulting from GLP-1R activation. Journal Article Clinical & Experimental Pharmacology 03 04 21611459 Diabetes mellitus; GLP-1; GLP-1R; GPCR; Insulin; Signalling 1 11 2013 2013-11-01 10.4172/2161-1459.1000138 © 2013 Thompson A, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. COLLEGE NANME Medical School COLLEGE CODE MEDS Swansea University 2016-05-10T10:55:41.9107469 2016-04-22T14:11:12.3634041 Faculty of Medicine, Health and Life Sciences Swansea University Medical School - Medicine Kanamarlapudi Aiysha Thompson 1 Venkat Kanamarlapudi 0000-0002-8739-1483 2 0027395-22042016142318.pdf GLP-1Rsignaldiabetes.pdf 2016-04-22T14:23:18.7470000 Output 1674802 application/pdf Version of Record true 2016-04-22T00:00:00.0000000 true
title Type 2 Diabetes Mellitus and Glucagon Like Peptide-1 Receptor Signalling
spellingShingle Type 2 Diabetes Mellitus and Glucagon Like Peptide-1 Receptor Signalling
Venkat Kanamarlapudi
title_short Type 2 Diabetes Mellitus and Glucagon Like Peptide-1 Receptor Signalling
title_full Type 2 Diabetes Mellitus and Glucagon Like Peptide-1 Receptor Signalling
title_fullStr Type 2 Diabetes Mellitus and Glucagon Like Peptide-1 Receptor Signalling
title_full_unstemmed Type 2 Diabetes Mellitus and Glucagon Like Peptide-1 Receptor Signalling
title_sort Type 2 Diabetes Mellitus and Glucagon Like Peptide-1 Receptor Signalling
author_id_str_mv 63741801137148abfa4c00cd547dcdfa
author_id_fullname_str_mv 63741801137148abfa4c00cd547dcdfa_***_Venkat Kanamarlapudi
author Venkat Kanamarlapudi
author2 Kanamarlapudi Aiysha Thompson
Venkat Kanamarlapudi
format Journal article
container_title Clinical & Experimental Pharmacology
container_volume 03
container_issue 04
publishDate 2013
institution Swansea University
issn 21611459
doi_str_mv 10.4172/2161-1459.1000138
college_str Faculty of Medicine, Health and Life Sciences
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hierarchy_top_id facultyofmedicinehealthandlifesciences
hierarchy_top_title Faculty of Medicine, Health and Life Sciences
hierarchy_parent_id facultyofmedicinehealthandlifesciences
hierarchy_parent_title Faculty of Medicine, Health and Life Sciences
department_str Swansea University Medical School - Medicine{{{_:::_}}}Faculty of Medicine, Health and Life Sciences{{{_:::_}}}Swansea University Medical School - Medicine
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description It has been estimated that approximately 8.4% of the world population currently live with diabetes mellitus and type 2 diabetes is the most common form. Type 2 diabetes increases the risk of complications such as heart attacks, blindness, amputations and kidney failure. Glucagon like Peptide-1 (GLP-1) is an effective insulinotropic agent and therefore its effects on insulin secretion have been greatly examined for more than two decades. It is a polypeptide hormone secreted by the intestinal L-cells into the blood in response to food uptake. GLP-1 has a very short half-life in vivo due to the rapid proteolytic degradation by Dipeptidyl Peptidase IV (DPP-IV). Therefore DPP-IV resistant GLP-1 analogues, Exenatide and Liraglutide, have been developed and are currently being used in the treatment of type 2 diabetes. GLP-1 agonist functions by binding to its receptor, GLP1R, on the cell surface.The GLP-1R belongs to the class B peptide receptor family based on its structure and function. The binding of GLP-1 to its receptor results in activation of Gαs coupled adenylyl cyclase and the production of cyclic Adenosine Monophosphate (cAMP), which enhances glucose-induced insulin secretion. Continuous GLP-1R activation also causes insulin secretion and pancreatic islet β-cell proliferation and neogenesis. The GLP-1R is internalised following its activation, which regulates the biological responsiveness of the receptor. Structurally the GLP-1R contains a large N-terminal extracellular domain (TM1-TM7) joined by three intracellular loops (ICL1, ICL2, ICL3) and three extracellular loops (ECL1, ECL2, ECL3), and an intracellular C-terminal domain. These domains play critical roles in GLP-1R trafficking to the cell surface, and also in agonist dependent activation and internalisation of the receptor. This review is focused on type 2 diabetes, its treatment with GLP-1, GLP-1R structure and function, and the physiological affects resulting from GLP-1R activation.
published_date 2013-11-01T06:57:47Z
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