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Keywords: G-protein-coupled receptor (GPCR)
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Articles
Using the fragment molecular orbital method to investigate agonist–orexin-2 receptor interactions
Open AccessAlexander Heifetz, Matteo Aldeghi, Ewa I. Chudyk, Dmitri G. Fedorov, Mike J. Bodkin, Philip C. Biggin
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2016) 44 (2): 574–581.
Published: 11 April 2016
...-based drug discovery (SBDD) process. Clearly, to begin SBDD, a structure is needed, and although there has been fantastic progress in solving G-protein-coupled receptor (GPCR) crystal structures, the process remains quite slow and is not currently feasible for every GPCR or GPCR–ligand complex...
Articles
GPCR–styrene maleic acid lipid particles (GPCR–SMALPs): their nature and potential
Available to PurchaseMark Wheatley, Jack Charlton, Mohammed Jamshad, Sarah J. Routledge, Sian Bailey, Penelope J. La-Borde, Maria T. Azam, Richard T. Logan, Roslyn M. Bill, Tim R. Dafforn, David R. Poyner
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2016) 44 (2): 619–623.
Published: 11 April 2016
...Mark Wheatley; Jack Charlton; Mohammed Jamshad; Sarah J. Routledge; Sian Bailey; Penelope J. La-Borde; Maria T. Azam; Richard T. Logan; Roslyn M. Bill; Tim R. Dafforn; David R. Poyner G-protein-coupled receptors (GPCRs) form the largest class of membrane proteins and are an important target...
Articles
Evidence for the heterotetrameric structure of the adenosine A 2A –dopamine D 2 receptor complex
Available to PurchaseVerònica Casadó-Anguera, Jordi Bonaventura, Estefanía Moreno, Gemma Navarro, Antoni Cortés, Sergi Ferré, Vicent Casadó
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2016) 44 (2): 595–600.
Published: 11 April 2016
...Verònica Casadó-Anguera; Jordi Bonaventura; Estefanía Moreno; Gemma Navarro; Antoni Cortés; Sergi Ferré; Vicent Casadó Heteromers of G-protein-coupled receptors (GPCRs) have emerged as potential novel targets for drug development. Accumulating evidence indicates that GPCRs can form homodimers...
Articles
Epac proteins: specific ligands and role in cardiac remodelling
Available to Purchase
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2014) 42 (2): 257–264.
Published: 20 March 2014
...-protein-coupled receptor (GPCR) heart failure phosphodiesterase cAMP is an ubiquitous second messenger that plays a critical role in a multitude of biological functions [ 1 ]. It is one of the most important second messengers in the heart, regulating many physiological processes, such as cardiac...
Articles
Arresting inflammation: contributions of plasma membrane and endosomal signalling to neuropeptide-driven inflammatory disease
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2013) 41 (1): 137–143.
Published: 29 January 2013
... targeting of cell-surface signalling. 1 To whom correspondence should be addressed (email [email protected] ). 20 11 2012 © The Authors Journal compilation © 2013 Biochemical Society 2013 arrestin endosome G-protein-coupled receptor (GPCR) neuropeptide protease...
Articles
G-Protein-Coupled Receptors: from Structural Insights to Functional Mechanisms
Available to Purchase
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2013) 41 (1): 135–136.
Published: 29 January 2013
...-arrestin crystal structure G-protein-coupled receptor (GPCR) modelling pharmacology What of the future? Arising from the meeting, we think that it is possible to see a number of important areas for future research in GPCR biology. The crystal structures are wonderfully revealing, but provide...
Articles
Palmitoylation of serotonin receptors
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2013) 41 (1): 89–94.
Published: 29 January 2013
...-hydroxytryptamine) receptors and its role in the regulation of receptor functions. 11 9 2012 © The Authors Journal compilation © 2013 Biochemical Society 2013 G-protein-coupled receptor (GPCR) palmitoylation serotonin (5-hydroxytryptamine) signal transduction Cellular as well...
Articles
Conserved activation pathways in G-protein-coupled receptors
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2012) 40 (2): 383–388.
Published: 21 March 2012
... ). 6 1 2012 © The Authors Journal compilation © 2012 Biochemical Society 2012 adenosine receptor adrenergic receptor G-protein-coupled receptor (GPCR) metarhodopsin-II retinal rhodopsin GPCRs (G-protein-coupled receptors) are a family of seven-transmembrane helix proteins...
Articles
Insights into the activation mechanism of the visual receptor rhodopsin
Available to Purchase
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2012) 40 (2): 389–393.
Published: 21 March 2012
... © The Authors Journal compilation © 2012 Biochemical Society 2012 G-protein-coupled receptor (GPCR) retinal chromophore rhodopsin solid-state NMR transmembrane helix vision Solid-state NMR spectroscopy has also provided several insights into the structure of Meta II [ 21 ]. Solid...
Articles
Crystallizing membrane proteins for structure–function studies using lipidic mesophases
Available to Purchase
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2011) 39 (3): 725–732.
Published: 20 May 2011
... crystallization G-protein-coupled receptor (GPCR) lipidic cubic phase macromolecular crystallography membrane protein structure mesophase robot structure–function analysis The 13 January 2011 issue of the journal Nature includes three papers reporting on the structure and function of medically...
Articles
Systems biochemistry approaches to vertebrate phototransduction: towards a molecular understanding of disease
Available to Purchase
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2010) 38 (5): 1275–1280.
Published: 24 September 2010
... G-protein-coupled receptor (GPCR) kinetic modelling Leber congenital amaurosis phototransduction rod systems biology The primary events in vertebrate vision are the biochemical steps in the phototransduction cascade in rods and cones, the retinal photoreceptor cells. This signal...
Articles
Solid-state NMR spectroscopy as a tool for drug design: from membrane-embedded targets to amyloid fibrils
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2007) 35 (5): 985–990.
Published: 25 October 2007
... 2007 Biochemical Society 2007 amyloid cross-polarization magic-angle spinning (CP-MAS) drug discovery G-protein-coupled receptor (GPCR) NMR solid-state NMR There are now numerous examples of how the search for new drug candidates has been hastened by structural information provided...
Articles
Intestinal glucose sensing and regulation of intestinal glucose absorption
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2007) 35 (5): 1191–1194.
Published: 25 October 2007
... Journal compilation © 2007 Biochemical Society 2007 enteroendocrine cell G-protein-coupled receptor (GPCR) gut hormone intestinal glucose sensing sodium/glucose co-transporter 1 (SGLT1) taste receptor In recent years, there has been remarkable progress made towards understanding...
Articles
Structural basis of natural ligand binding and activation of the Class II G-protein-coupled secretin receptor
Available to Purchase
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2007) 35 (4): 709–712.
Published: 20 July 2007
... Society 2007 G-protein-coupled receptor (GPCR) ligand binding mutagenesis photoaffinity labelling receptor activation secretin receptor Fluorescence techniques can provide complementary insights into the environment of indicators that can be situated at distinct sites throughout...
Articles
Monitoring interactions between G-protein-coupled receptors and β-arrestins
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2007) 35 (4): 764–766.
Published: 20 July 2007
... correspondence should be addressed (email [email protected] ). 23 4 2007 © The Authors Journal compilation © 2007 Biochemical Society 2007 β-arrestin bioluminescence resonance energy transfer (BRET) clathrin G-protein-coupled receptor (GPCR) live-cell imaging protein–protein...
Articles
Molecular mechanisms involved in vasoactive intestinal peptide receptor activation and regulation: current knowledge, similarities to and differences from the A family of G-protein-coupled receptors
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2007) 35 (4): 724–728.
Published: 20 July 2007
.... Mol. Pharmacol. 2006 69 363 373 34 Langer I. Gaspard N. Robberecht P. Br. J. Pharmacol. 2006 148 1051 1059 dimerization G-protein-coupled receptor (GPCR) internalization phosphorylation signalling vasoactive intestinal peptide/pituitary adenylate cyclase...
Articles
Computational studies of Family A and Family B GPCRs
Available to PurchaseS. Vohra, S.V. Chintapalli, C.J.R. Illingworth, P.J. Reeves, P.M. Mullineaux, H.S.X. Clark, M.K. Dean, G.J.G. Upton, C.A. Reynolds
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2007) 35 (4): 749–754.
Published: 20 July 2007
... ].) cold-spot alignment evolutionary trace G-protein-coupled receptor (GPCR) GCR1 Molecular Dynamics simulations receptor dimerization Family B G-protein coupled receptor (GPCRs), although less-well studied than Family A GPCRs, are interesting because their protein fold (in the N-terminus...
Includes: Supplementary data
Articles
Family Resemblances? Ligand Binding and Activation of Family A and B G-Protein-Coupled Receptors
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2007) 35 (4): 707–708.
Published: 20 July 2007
... articles. 1 To whom correspondence should be addressed (email [email protected] ). 11 5 2007 © The Authors Journal compilation © 2007 Biochemical Society 2007 drug design G-protein-coupled receptor (GPCR) ligand binding molecular modelling receptor activation...
Articles
Phenotypic classification of mutants: a tool for understanding ligand binding and activation of muscarinic acetylcholine receptors
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2007) 35 (4): 742–745.
Published: 20 July 2007
.... 1 To whom correspondence should be addressed (email [email protected] ). 23 3 2007 © The Authors Journal compilation © 2007 Biochemical Society 2007 acetylcholine alanine-scanning mutagenesis G-protein-coupled receptor (GPCR) muscarinic acetylcholine receptor (mAChR...
Articles
Unravelling the mechanisms underpinning chemokine receptor activation and blockade by small molecules: a fine line between agonism and antagonism?
Available to Purchase
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2007) 35 (4): 755–759.
Published: 20 July 2007
.... Acad. Sci. U.S.A. 1977 74 2256 1 To whom correspondence should be addressed (email [email protected] ) 2 4 2007 © The Authors Journal compilation © 2007 Biochemical Society 2007 allosteric modulator antagonist chemokine receptor G-protein-coupled receptor...
Articles
Peptide binding at the GLP-1 receptor
Available to PurchaseR. Mann, N. Nasr, D. Hadden, J. Sinfield, F. Abidi, S. Al-Sabah, R. López de Maturana, J. Treece-Birch, A. Willshaw, D. Donnelly
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2007) 35 (4): 713–716.
Published: 20 July 2007
... receptor. In order to better understand these differences, we have studied the interaction between combinations of full-length or truncated ligands with full-length or truncated receptors. exendin-4 (EX-4) glucagon-like peptide receptor 1 (GLP1-R) G-protein-coupled receptor (GPCR) peptide binding...
Articles
Mechanisms underlying agonist efficacy
Available to Purchase
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2007) 35 (4): 733–736.
Published: 20 July 2007
... that the very low agonist efficacy expressed by these drugs is important for their actions, and so systems that can define this efficacy are required. © The Authors Journal compilation © 2007 Biochemical Society 2007 agonist efficacy D 2 dopamine receptor G-protein-coupled receptor (GPCR) G...
Articles
Extracellular loops and ligand binding to a subfamily of Family A G-protein-coupled receptors
Available to PurchaseM. Wheatley, J. Simms, S.R. Hawtin, V.J. Wesley, D. Wootten, M. Conner, Z. Lawson, A.C. Conner, A. Baker, Y. Cashmore, R. Kendrick, R.A. Parslow
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2007) 35 (4): 717–720.
Published: 20 July 2007
... compilation © 2007 Biochemical Society 2007 agonist G-protein-coupled receptor (GPCR) peptide hormone receptor activation vasopressin GPCRs (G-protein-coupled receptors) are a large family of structurally related proteins which mediate their effects by coupling to G-proteins. Several hundred...
Articles
Agonist selectivity in the oxytocin/vasopressin receptor family: new insights and challenges
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2007) 35 (4): 737–741.
Published: 20 July 2007
... ] 0.45 [ 58 ] 1.54 [ 58 ] 0.29 [ 58 ] dDAVP 23.3 [ 54 ] 62.4 [ 54 ] 5.8 [ 54 ] 0.3 [ 54 ] 100 [ 54 ] 9.3 [ 32 ] © The Authors Journal compilation © 2007 Biochemical Society 2007 agonist selectivity bivalent ligand G-protein-coupled receptor (GPCR) oxytocin therapeutic...
Articles
G-protein-coupled receptor signalling through protein networks
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2007) 35 (1): 23–27.
Published: 22 January 2007
... Structure of the GPCR bovine rhodopsin with retinal bound The structure is shown both perpendicular and parallel to the membrane in which the protein is embedded. angiotensin receptor β-adrenoceptor G-protein G-protein-coupled receptor (GPCR) melatonin receptor protein network After...
Articles
Cannabinoids and PPARα signalling
Available to Purchase
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2006) 34 (6): 1095–1097.
Published: 25 October 2006
... The Biochemical Society 2006 cannabinoid receptor (CB receptor) central nervous system (CNS) G-protein-coupled receptor (GPCR) middle cerebral artery occlusion neuroprotection peroxisome-proliferator-activated receptor (PPAR) THC (Δ 9 -tetrahydrocannabinol) is the main psychoactive ingredient...
Articles
Developing chemokine mutants with improved proteoglycan affinity and knocked-out GPCR activity as anti-inflammatory recombinant drugs
Available to Purchase
Journal:
Biochemical Society Transactions
Biochem Soc Trans (2006) 34 (3): 435–437.
Published: 22 May 2006
... Society 2006 anti-inflammatory drug chemokine mutant glycomics glycosaminoglycan G-protein-coupled receptor (GPCR) protein engineering Chemokines induce cell migration and activation by binding to specific cell surface, seven-transmembrane-spanning GPCRs (G-protein-coupled receptors...
Articles
Compartmentation of G-protein-coupled receptors and their signalling components in lipid rafts and caveolae
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2005) 33 (5): 1131–1134.
Published: 26 October 2005
...P.A. Insel; B.P. Head; H.H. Patel; D.M. Roth; R.A. Bundey; J.S. Swaney G-protein-coupled receptors (GPCRs) and post-GPCR signalling components are expressed at low overall abundance in plasma membranes, yet they evoke rapid, high-fidelity responses. Considerable evidence suggests that GPCR...
Articles
Critical role of acylglycerol kinase in epidermal growth factor-induced mitogenesis of prostate cancer cells
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2005) 33 (6): 1362–1365.
Published: 26 October 2005
[email protected] ). 23 6 2005 © 2005 The Biochemical Society 2005 acylglycerol kinase epidermal growth factor (EGF) G-protein-coupled receptor (GPCR) lysophosphatidic acid (LPA) phosphatidic acid (PA) prostate cancer For over 50 years, the primary form of therapy for advanced...
Articles
Molecular mechanisms of GABA B receptor activation: new insights from the mechanism of action of CGP7930, a positive allosteric modulator
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2004) 32 (5): 871–872.
Published: 26 October 2004
... of GABA B receptor. 1 To whom correspondence should be addressed (email [email protected] ). 6 7 2004 © 2004 The Biochemical Society 2004 activation mechanism allostery dimerization γ-aminobutyric acid-B (GABA B ) receptor G-protein-coupled receptor (GPCR...
Articles
The third extracellular loop of G-protein-coupled receptors: more than just a linker between two important transmembrane helices
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2004) 32 (6): 1048–1050.
Published: 26 October 2004
... and that ECLs fulfil important functional roles within the GPCR architecture. In the present study, we examine the functional significance of ECL3, focusing primarily on Family A receptors. agonist binding G-protein-coupled receptor (GPCR) peptide hormone receptor activation © 2004...
Articles
Kinetics of G-protein-coupled receptor signalling and desensitization
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2004) 32 (6): 1029–1031.
Published: 26 October 2004
... it is possible that GRK phosphorylation of GPCRs depends on an additional conformational change in the receptor, which is not required for either G-protein activation or arrestin binding. © 2004 The Biochemical Society 2004 arrestin fluorescence resonance energy transfer (FRET) G-protein-coupled...
Articles
Evidence to support a spectrum of active states for the glucagon receptor
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2004) 32 (6): 1037–1039.
Published: 26 October 2004
.... Kobilka B.K. J. Biol. Chem. 2001 276 24433 24436 cAMP regulatory element (CRE)-luciferase glucagon G-protein-coupled receptor (GPCR) mutagenesis receptor activation ternary complex The extended ternary complex model for GPCR (G-protein-coupled receptor) activation suggests...
Articles
Phosphoinositide 3-kinase γ: kinase-dependent and -independent activities in cardiovascular function and disease
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2004) 32 (2): 383–386.
Published: 01 April 2004
..., these data suggested expression of PI3K not only in blood vessels but also in cardiac muscle. Evidence supporting this hypothesis included the finding Key words: -adrenergic receptor, contractility, G-protein-coupled receptor (GPCR), heart disease, hypertrophy, phosphoinositide 3-kinase (PI3K...
Articles
EGFR signal transactivation in cancer cells
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2003) 31 (6): 1203–1208.
Published: 01 December 2003
... receptor (EGFR) G-protein-coupled receptor (GPCR) transactivation Abbreviations used: ADAM, a d isintegrin a nd m etalloprotease; ET-1, endothelin-1; EGF, epidermal growth factor; EGFR, epidermal growth factor receptor; ERK, extracellular-signal-regulated kinase; GPCR, G-protein-coupled...
Articles
Exogenous and intracellularly generated sphingosine 1-phosphate can regulate cellular processes by divergent pathways
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Journal:
Biochemical Society Transactions
Biochem Soc Trans (2003) 31 (6): 1216–1219.
Published: 01 December 2003
... ). 679th Meeting of the Biochemical Society held at the University of Essex, Colchester, 2–4 July 2003 4 July 2003 © 2003 Biochemical Society 2003 cell growth and survival G-protein-coupled receptor (GPCR) sphingosine kinase sphingosine 1-phosphate (S1P) sphingosine 1-phosphate...