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Phone: (843) 588-2001
Edgar Allan Poe/Sullivan's Island Library
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Phone: (843) 883-3914
West Ashley Library
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Wando Mount Pleasant Library
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Village Library
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Phone: (843) 884-9741
St. Paul's/Hollywood Library
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McClellanville Library
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Keith Summey North Charleston Library
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Hurd/St. Andrews Library
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G protein-coupled receptors: signalling and regulation by lipid agonists for improved glucose homoeostasis.
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- Author(s): Moran, Brian; Flatt, Peter; McKillop, Aine
- Source:
Acta Diabetologica; Apr2016, Vol. 53 Issue 2, p177-188, 12p- Subject Terms:
- Source:
- Additional Information
- Abstract: G protein-coupled receptors (GPCRs) play a pivotal role in cell signalling, controlling many processes such as immunity, growth, cellular differentiation, neurological pathways and hormone secretions. Fatty acid agonists are increasingly recognised as having a key role in the regulation of glucose homoeostasis via stimulation of islet and gastrointestinal GPCRs. Downstream cell signalling results in modulation of the biosynthesis, secretion, proliferation and anti-apoptotic pathways of islet and enteroendocrine cells. GPR40 and GPR120 are activated by long-chain fatty acids (>C12) with both receptors coupling to the Gαq subunit that activates the Ca-dependent pathway. GPR41 and GPR43 are stimulated by short-chain fatty acids (C2-C5), and activation results in binding to Gαi that inhibits the adenylyl cyclase pathway attenuating cAMP production. In addition, GPR43 also couples to the Gαq subunit augmenting intracellular Ca and activating phospholipase C. GPR55 is specific for cannabinoid endogenous agonists (endocannabinoids) and non-cannabinoid fatty acids, which couples to Gα and Gαq proteins, leading to enhancing intracellular Ca, extracellular signal-regulated kinase 1/2 (ERK) phosphorylation and Rho kinase. GPR119 is activated by fatty acid ethanolamides and binds to Gαs utilising the adenylate cyclase pathway, which is dependent upon protein kinase A. Current research indicates that GPCR therapies may be approved for clinical use in the near future. This review focuses on the recent advances in preclinical diabetes research in the signalling and regulation of GPCRs on islet and enteroendocrine cells involved in glucose homoeostasis. [ABSTRACT FROM AUTHOR]
- Abstract: Copyright of Acta Diabetologica is the property of Springer Nature and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)
- Abstract:
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