International Union of Pharmacology. XLVI. G Protein-Coupled Receptor List

Foord, Steven M.; Bonner, Tom I.; Neubig, Richard R.; Rosser, Edward M.; Pin, Jean‐Philippe; Davenport, Anthony P.; Spedding, Michael; Harmar, Anthony J.

doi:10.1124/pr.57.2.5

Cited by 460 publications

(350 citation statements)

References 18 publications

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“…GPCRs are grouped into four main classes based on sequence similarity, they are classes A, B, C (previously referred to as Class 1, 2 and 3 respectively) and the frizzled family (Foord et al, 2005;NC-IUPHAR). GLP-1R is a member of the Class B family consisting of many classical hormone receptors (Harmar, 2001).…”

Section: Glp-1r In the Pancreasmentioning

confidence: 99%

“…GLP-1R is a member of the Class B family consisting of many classical hormone receptors (Harmar, 2001). Within Class B the receptors for the peptide hormones form a subclass of the glucagon receptor family which also include receptors for glucagon, GLP-2, GIP, growth hormone releasing hormone (GHRH), and secretin (Foord et al, 2005;Harmar, 2004;Mayo et al, 2003). GLP-1, GLP-2 and glucagon are encoded by the same gene and result from post-translational modifications of the proglucagon molecule (Bell, 1986).…”

Section: Glp-1r In the Pancreasmentioning

confidence: 99%

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Mechanisms of action of glucagon-like peptide 1 in the pancreas

Doyle

Egan

2007

Pharmacology & Therapeutics

557

448

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Glucagon-like peptide-1 is a hormone that is encoded in the proglucagon gene. It is mainly produced in enteroendocrine L cells of the gut and is secreted into the blood stream when food containing fat, protein hydrolysate and/or glucose enters the duodenum. Its particular effects on insulin and glucagon secretion have generated a flurry of research activity over the past twenty years culminating in a naturally occurring GLP-1 receptor agonist, exendin-4, now being used to treat type 2 diabetes. GLP-1 engages a specific G-protein coupled receptor that is present in tissues other than the pancreas (brain, kidney, lung, heart, major blood vessels). The most widely studied cell activated by GLP-1 is the insulin-secreting beta cell where its defining action is augmentation of glucose-induced insulin secretion. Upon GLP-1 receptor activation, adenylyl cyclase is activated and cAMP generated, leading, in turn, to cAMP-dependent activation of second messenger pathways, such as the PKA and Epac pathways. As well as short-term effects of enhancing glucose-induced insulin secretion, continuous GLP-1 receptor activation also increases insulin synthesis, and beta cell proliferation and neogenesis. Although these latter effects cannot be currently monitored in humans, there are substantial improvements in glucose tolerance and increases in both first phase and plateau phase insulin secretory responses in type 2 diabetic patients treated with exendin-4. This review we will focus on the effects resulting from GLP-1 receptor activation in islets of Langerhans

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Section: Glp-1r In the Pancreasmentioning

confidence: 99%

Section: Glp-1r In the Pancreasmentioning

confidence: 99%

Mechanisms of action of glucagon-like peptide 1 in the pancreas

Doyle

Egan

2007

Pharmacology & Therapeutics

557

448

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“…Metabotropic glutamate receptors are the prototypic members of Class 3 (now Class C) GPCR (Alexander et al 2015;Foord et al 2005), sharing little amino acid similarity with rhodopsin-like receptors or the secretin family. Alternative splicing produces several variants of mGlu 1 and mGlu 5 with long (mGlu 1a , mGlu 5a-b ) or short (mGlu 1b-d , mGlu 5d ) carboxyl terminals with differences in cellular localization, and Gprotein signaling efficacy and desensitization (Grandes et al 1994;Malherbe et al 2002;Mary et al 1998).…”

Section: Structure Of Mglu Receptorsmentioning

confidence: 99%

“…This group of receptors, comprising mGlu 1 and mGlu 5 , share sequence homology, coupling through protein Gα q/11, pharmacology, and post-synaptic localization that distinguish them from the other six mGlu isoforms found in the mammalian genome (Cartmell and Schoepp 2000;Foord et al 2005;Nakanishi 1992). Our focus is on short-term changes in membrane current that directly result from Group I mGlu receptor activation and the subsequent mobilization of second messenger systems.…”

Section: Introductionmentioning

confidence: 99%

Control of neuronal excitability by Group I metabotropic glutamate receptors

Amb

Jds

et al. 2017

Biophys Rev

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Metabotropic glutamate (mGlu) receptors couple through G proteins to regulate a large number of cell functions. Eight mGlu receptor isoforms have been cloned and classified into three Groups based on sequence, signal transduction mechanisms and pharmacology. This review will focus on Group I mGlu receptors, comprising the isoforms mGlu 1 and mGlu 5 . Activation of these receptors initiates both G protein-dependent and -independent signal transduction pathways. The G-protein-dependent pathway involves mainly Gα q , which can activate PLCβ, leading initially to the formation of IP 3 and diacylglycerol. IP 3 can release Ca 2+ from cellular stores resulting in activation of Ca 2+ -dependent ion channels. Intracellular Ca 2+ , together with diacylglycerol, activates PKC, which has many protein targets, including ion channels. Thus, activation of the G-protein-dependent pathway affects cellular excitability though several different effectors. In parallel, G protein-independent pathways lead to activation of non-selective cationic currents and metabotropic synaptic currents and potentials. Here, we provide a survey of the membrane transport proteins responsible for these electrical effects of Group I metabotropic glutamate receptors.

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“…Overview: Melanocortin receptors (provisional nomenclature, see Foord et al, 2005) Rank order of potency (Chagnon et al, 1997;Farooqi and O'Rahilly, 2008). (2-[1-{tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl}-5-chlorophenyl] 2,3,4-tetrahydroisoquinolinium-3-ylcarbonyl (Browning et al, 2000) Melatonin, 2-iodo-melatonin, S20098, GR196429, LY156735 and TAK375 (Kato et al, 2005) are nonselective agonists for MT1 and MT2 receptors.…”

Section: Melanocortinmentioning

confidence: 99%

Ligand-gated Ion Channels

Encyclopedic Reference of Molecular Pharmacology

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International Union of Pharmacology. XLVI. G Protein-Coupled Receptor List

Cited by 460 publications

References 18 publications

Mechanisms of action of glucagon-like peptide 1 in the pancreas

Mechanisms of action of glucagon-like peptide 1 in the pancreas

Control of neuronal excitability by Group I metabotropic glutamate receptors

Ligand-gated Ion Channels

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