Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function

Research output: Contribution to journalArticleResearchpeer-review

Abstract

Type 2 diabetes is a major global health problem and there is ongoing research for new treatments to manage the disease. The GLP-1R (glucagon-like peptide-1 receptor) controls the physiological response to the incretin peptide, GLP-1, and is currently a major target for the development of therapeutics owing to the broad range of potential beneficial effects in Type 2 diabetes. These include promotion of glucose-dependent insulin secretion, increased insulin biosynthesis, preservation of beta-cell mass, improved peripheral insulin sensitivity and promotion of weight loss. Despite this, our understanding of GLP-1R function is still limited, with the desired spectrum of GLP-1R-mediated signalling yet to be determined. We review the current understanding of GLP-1R function, in particular, highlighting recent contributions in the field on allosteric modulation, probe-dependence and ligand-directed signal bias and how these behaviours may influence future drug development.
Original languageEnglish
Pages (from-to)172 - 179
Number of pages8
JournalBiochemical Society Transactions
Volume41
Issue number1
DOIs
Publication statusPublished - 2013

Cite this

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title = "Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function",
abstract = "Type 2 diabetes is a major global health problem and there is ongoing research for new treatments to manage the disease. The GLP-1R (glucagon-like peptide-1 receptor) controls the physiological response to the incretin peptide, GLP-1, and is currently a major target for the development of therapeutics owing to the broad range of potential beneficial effects in Type 2 diabetes. These include promotion of glucose-dependent insulin secretion, increased insulin biosynthesis, preservation of beta-cell mass, improved peripheral insulin sensitivity and promotion of weight loss. Despite this, our understanding of GLP-1R function is still limited, with the desired spectrum of GLP-1R-mediated signalling yet to be determined. We review the current understanding of GLP-1R function, in particular, highlighting recent contributions in the field on allosteric modulation, probe-dependence and ligand-directed signal bias and how these behaviours may influence future drug development.",
author = "Koole, {Cassandra Renee} and Kavita Pabreja and Savage, {Emilia Elizabeth} and Wootten, {Denise Laura} and Furness, {Sebastian George Barton} and Miller, {Laurence J} and Arthur Christopoulos and Patrick Sexton",
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language = "English",
volume = "41",
pages = "172 -- 179",
journal = "Biochemical Society Transactions",
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publisher = "Portland Press",
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Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function. / Koole, Cassandra Renee; Pabreja, Kavita; Savage, Emilia Elizabeth; Wootten, Denise Laura; Furness, Sebastian George Barton; Miller, Laurence J; Christopoulos, Arthur; Sexton, Patrick.

In: Biochemical Society Transactions, Vol. 41, No. 1, 2013, p. 172 - 179.

Research output: Contribution to journalArticleResearchpeer-review

TY - JOUR

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AU - Koole, Cassandra Renee

AU - Pabreja, Kavita

AU - Savage, Emilia Elizabeth

AU - Wootten, Denise Laura

AU - Furness, Sebastian George Barton

AU - Miller, Laurence J

AU - Christopoulos, Arthur

AU - Sexton, Patrick

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AB - Type 2 diabetes is a major global health problem and there is ongoing research for new treatments to manage the disease. The GLP-1R (glucagon-like peptide-1 receptor) controls the physiological response to the incretin peptide, GLP-1, and is currently a major target for the development of therapeutics owing to the broad range of potential beneficial effects in Type 2 diabetes. These include promotion of glucose-dependent insulin secretion, increased insulin biosynthesis, preservation of beta-cell mass, improved peripheral insulin sensitivity and promotion of weight loss. Despite this, our understanding of GLP-1R function is still limited, with the desired spectrum of GLP-1R-mediated signalling yet to be determined. We review the current understanding of GLP-1R function, in particular, highlighting recent contributions in the field on allosteric modulation, probe-dependence and ligand-directed signal bias and how these behaviours may influence future drug development.

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