Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function
Autor: | Cassandra Koole, Patrick M. Sexton, Laurence J. Miller, Arthur Christopoulos, Kavita Pabreja, Sebastian G.B. Furness, Emilia Elizabeth Savage, Denise Wootten |
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Rok vydání: | 2013 |
Předmět: |
endocrine system
medicine.medical_specialty medicine.medical_treatment Molecular Sequence Data Incretin Type 2 diabetes Bioinformatics Biochemistry Incretins Glucagon-Like Peptide-1 Receptor Allosteric Regulation Glucagon-Like Peptide 1 Insulin receptor substrate Internal medicine medicine Receptors Glucagon Humans Amino Acid Sequence Glucagon-like peptide 1 receptor Insulin-like growth factor 1 receptor biology Sequence Homology Amino Acid Insulin digestive oral and skin physiology Molecular Mimicry medicine.disease Insulin receptor Endocrinology Drug development Diabetes Mellitus Type 2 biology.protein hormones hormone substitutes and hormone antagonists Signal Transduction |
Zdroj: | Biochemical Society transactions. 41(1) |
ISSN: | 1470-8752 |
Popis: | 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 β-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. |
Databáze: | OpenAIRE |
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