The Concise Guide to PHARMACOLOGY 2013/14: G Protein‐Coupled Receptors

Alexander, Stephen P.H.; Benson, Helen E.; Faccenda, Elena; Pawson, Adam J.; Sharman, Joanna L.; Spedding, Michael; Peters, John A.; Harmar, Anthony J.

doi:10.1111/bph.12445

Cited by 555 publications

(352 citation statements)

References 1,600 publications

(861 reference statements)

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“…Previous experiments, as those reported in [22] and [27], have shown that the maximum lag is to be found in the range [1,160]. Following [27], and the rationale that a large maximum lag implies high data dimensionality and the problems that come with it (curse of dimensionality), we searched for L in the range of 1 to 30.…”

Section: Resultsmentioning

confidence: 99%

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The influence of alignment-free sequence representations on the semi-supervised classification of class C G protein-coupled receptors

Cruz-Barbosa

Vellido

Giraldo

2014

Med Biol Eng Comput

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G protein-coupled receptors (GPCRs) are integral cell membrane proteins of relevance for pharmacology. The tertiary structure of the transmembrane domain, a gate to the study of protein functionality, is unknown for almost all members of class C GPCRs, which are the target of the current study. As a result, their investigation must often rely on alignments of their amino acid sequences. Sequence alignment entails the risk of missing relevant information. Various approaches have attempted to circumvent this risk through alignment-free transformations of the sequences on the basis of different amino acid physicochemical properties. In this paper, we use several of these alignment-free methods, as well as a basic amino acid composition representation, to transform the available sequences. Novel semi-supervised statistical machine learning methods are then used to discriminate the different class C GPCRs types from the transformed data. This approach is relevant due to the existence of orphan proteins to which type labels should be assigned in a process of deorphanization or reverse pharmacology. The reported experiments show that the proposed techniques provide accurate classification even in settings of extreme class-label scarcity and that fair accuracy can be achieved even with very simple transformation strategies that ignore the sequence ordering.

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Section: Resultsmentioning

confidence: 99%

“…In this section, we simulate a process of deorphanization of some sequences which are known to belong to the class C GPCR family [30,1] but for whom the corresponding natural ligand is unknown. For this, we developed a novel inductive version of the naturally transductive SS-GTM model.…”

Section: Deorphanization Experiments Using An Inductive Version Of Ss-gtmmentioning

confidence: 99%

The influence of alignment-free sequence representations on the semi-supervised classification of class C G protein-coupled receptors

Cruz-Barbosa

Vellido

Giraldo

2014

Med Biol Eng Comput

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“…This nomenclature complies with the British Journal of Pharmacology's guidelines (Alexander et al, 2013). In the past decade, GPBA has been shown to mediate many of the nongenomic actions of BAs on thermogenesis, insulin secretion and glucose homeostasis, inflammation, digestive functions and sensory transduction.…”

Section: Introductionmentioning

confidence: 99%

GPBA: a GPCR for bile acids and an emerging therapeutic target for disorders of digestion and sensation

Lieu¹,

Jayaweera²,

Bunnett³

2014

British J Pharmacology

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Bile acids (BAs) are digestive secretions that are necessary for the emulsification and absorption of dietary fats. Given the episodic nature of BA secretion and intestinal re-absorption, the circulating and tissue levels of BAs, like those of the gut hormones, fluctuate in fasting and fed states, and BA levels and forms are markedly affected by disease. BAs exert widespread hormonal-like effects by activating receptors in the nucleus and at the plasma membrane. The nuclear steroid receptors mediate the genomic actions of BAs on BA, glucose and lipid homeostasis. GPBA (TGR5) is a G-protein coupled plasma membrane receptor for BAs that mediates many of the rapid, non-genomic actions of BAs. GPBA has been implicated in the control of glucose homeostasis, inflammation and liver functions. Recent observations have revealed an unexpected role for GPBA in the nervous system. GPBA is expressed by enteric neurons and enterochromaffin cells that control peristalsis, and GPBA mediates the prokinetic actions of BAs in the colon that have been known for millennia. GPBA is also present on primary spinal afferent and spinal neurons that are necessary for sensory transduction. BA-induced activation of GPBA in the sensory nervous system promotes scratching behaviours and analgesia, which may contribute to the pruritus and painless jaundice that are observed in some patients with chronic cholestatic disease, where circulating BA concentrations are markedly increased. Thus, GPBA has emerged as an intriguing target for diverse metabolic, inflammatory, digestive and sensory disorders, where agonists and antagonists may be of value. LINKED ARTICLESThis article is part of a themed section on Molecular Pharmacology of GPCRs. To view the other articles in this section visit http://dx.doi. org/10.1111/bph.2014.171.issue-5 Abbreviations ADAM, A disintegrin and metalloproteinase domain-containing protein; ASBT, apical sodium-dependent BA transporter; BA, bile acid; CA, cholic acid; CDCA, chenodeoxycholic acid; CGRP, calcitonin gene-related peptide; D2, type 2 iodothyronine deodinase; DCA, deoxycholic acid; GLP-1, glucagon-like peptide 1; GPBA, bile acid receptor; KATP, ATP-dependent potassium channels; LCA, lithocholic acid; OA, oleanolic acid; TDCA, taurodeoxycholic acid; TLCA, taurolithocholic acid; UDCA, ursodeoxycholic acid IntroductionBile acids (BAs), a major component of bile, are digestive secretions that are necessary for the emulsification and absorption of dietary fats. Remarkably, BAs are also signalling molecules. The levels of BAs fluctuate in the circulation under physiological conditions and during disease states, rather like the circulating levels of gut hormones, and BAs can regulate cells throughout the body by activating specific BA receptors in the nucleus and at the plasma membrane. These receptors mediate the effects of BAs on diverse physiological processes, ranging from the control of glucose homeostasis to peristaltic contractions of the digestive tract, and have been implicated in disorders as diverse as obes...

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“…The existence of other G-protein cannabinoid receptors has also been suggested. These proposed receptors (also called putative or nonclassical cannabinoid receptors) include GPR18, GPR55 and GPR119 that have structural similarity to CB 1 and CB 2 (Alexander et al 2013;Zubrzycki et al 2014). …”

Section: The Endocannabinoid System and Classification Of Cannabinoidsmentioning

confidence: 99%

The use of cannabinoids in animals and therapeutic implications for veterinary medicine: a review

Landa¹,

Šulcová²,

Gbelec³

2016

Vet. Med. - Czech

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Cannabinoids/medical marijuana and their possible therapeutic use have received increased attention in human medicine during the last years. This increased attention is also an issue for veterinarians because particularly companion animal owners now show an increased interest in the use of these compounds in veterinary medicine. This review sets out to comprehensively summarise well known facts concerning properties of cannabinoids, their mechanisms of action, role of cannabinoid receptors and their classification. It outlines the main pharmacological effects of cannabinoids in laboratory rodents and it also discusses examples of possible beneficial use in other animal species (ferrets, cats, dogs, monkeys) that have been reported in the scientific literature. Finally, the article deals with the prospective use of cannabinoids in veterinary medicine. We have not intended to review the topic of cannabinoids in an exhaustive manner; rather, our aim was to provide both the scientific community and clinical veterinarians with a brief, concise and understandable overview of the use of cannabinoids in veterinary medicine.

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The Concise Guide to PHARMACOLOGY 2013/14: G Protein‐Coupled Receptors

Cited by 555 publications

References 1,600 publications

The influence of alignment-free sequence representations on the semi-supervised classification of class C G protein-coupled receptors

The influence of alignment-free sequence representations on the semi-supervised classification of class C G protein-coupled receptors

GPBA: a GPCR for bile acids and an emerging therapeutic target for disorders of digestion and sensation

The use of cannabinoids in animals and therapeutic implications for veterinary medicine: a review

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