Journal ArticleDOI
The Concise Guide to PHARMACOLOGY 2013/14: G Protein‐Coupled Receptors
Stephen P.H. Alexander,Helen E. Benson,Elena Faccenda,Adam J. Pawson,Joanna L. Sharman,Michael Spedding,John A. Peters,Anthony J. Harmar +7 more
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This article is published in British Journal of Pharmacology.The article was published on 2013-12-01. It has received 536 citations till now. The article focuses on the topics: G protein-coupled receptor & Receptor.read more
Citations
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Microglial M1/M2 polarization and metabolic states.
TL;DR: The polarization states of microglia and their relationship to mitochondrial metabolism are examined and a role of metabolic reprogramming in the regulation of the innate inflammatory response is suggested.
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Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor.
TL;DR: It is hypothesized that cannabidiol would inhibit cannabinoid agonist activity through negative allosteric modulation of CB1 receptors through positive allosterics modulation ofCB1 receptors.
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The contribution of astrocytes and microglia to traumatic brain injury
TL;DR: This review will focus on the roles of microglia and astrocytes following TBI, highlighting some of the key processes, pathways and mediators involved in this response.
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Movers and shakers: cell cytoskeleton in cancer metastasis
TL;DR: Improved understanding of how the cytoskeleton and its interacting partners influence tumour cell migration and metastasis has led to the development of novel therapeutics against aggressive and metastatic disease.
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Are cannabidiol and Δ9‐tetrahydrocannabivarin negative modulators of the endocannabinoid system? A systematic review
TL;DR: The evidence indicates that CBD and THCV are not rimonabant‐like in their action and thus appear very unlikely to produce unwanted CNS effects, illustrating how in vitro mechanistic studies do not always predict in vivo pharmacology and underlie the necessity of testing compounds in vivo before drawing any conclusion on their functional activity at a given target.
References
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Journal ArticleDOI
Ghrelin is a growth-hormone-releasing acylated peptide from stomach.
TL;DR: The occurrence of ghrelin in both rat and human indicates that GH release from the pituitary may be regulated not only by hypothalamic GHRH, but also by ghrelIn, a peptide specifically releases GH both in vivo and in vitro.
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Orexins and Orexin Receptors: A Family of Hypothalamic Neuropeptides and G Protein-Coupled Receptors that Regulate Feeding Behavior
Takeshi Sakurai,Akira Amemiya,Makoto Ishii,Ichiyo Matsuzaki,Richard M. Chemelli,Hirokazu Tanaka,S. Clay Williams,James A. Richardson,Gerald P. Kozlowski,Shelagh Wilson,Jonathan R.S. Arch,Robin E. Buckingham,Andrea C. Haynes,Steven A. Carr,Roland S. Annan,Dean E. McNulty,Wu Schyong Liu,Jonathan A. Terrett,Nabil Elshourbagy,Derk J. Bergsma,Masashi Yanagisawa +20 more
TL;DR: Two novel neuropeptides are identified, both derived from the same precursor by proteolytic processing, that bind and activate two closely related (previously) orphan G protein-coupled receptors in the hypothalamus of rats.
Journal Article
International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin).
Daniel Hoyer,David E. Clarke,John R. Fozard,Paul R. Hartig,Graeme R. Martin,Ewan J. Mylecharane,Pramod R. Saxena,Patrick P.A. Humphrey +7 more
TL;DR: It is evident that in the last decade or so, a vast amount of new information has become available concerning the various 5-HT receptor types and their characteristics, and it is important to rationalise in concert all of the available data from studies involving both operational approaches of the classical pharmacological type and those from molecular and cellular biology.
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High-Resolution Crystal Structure of an Engineered Human β2-Adrenergic G Protein–Coupled Receptor
Vadim Cherezov,Daniel M. Rosenbaum,Michael A. Hanson,Søren G. F. Rasmussen,Foon Sun Thian,Tong Sun Kobilka,Hee Jung Choi,Peter Kuhn,William I. Weis,Brian K. Kobilka,Raymond C. Stevens +10 more
TL;DR: Although the location of carazolol in the β2-adrenergic receptor is very similar to that of retinal in rhodopsin, structural differences in the ligand-binding site and other regions highlight the challenges in using rhodopin as a template model for this large receptor family.
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The G-Protein-Coupled Receptors in the Human Genome Form Five Main Families : Phylogenetic Analysis, Paralogon Groups, and Fingerprints
TL;DR: This study represents the first overall map of the GPCR sequences in a single mammalian genome and shows several common structural features indicating that the human GPCRs in the GRAFS families share a common ancestor.