British Journal of Pharmacology

Cover image for Vol. 172 Issue 2

Editor-in-Chief: Professor J.C. (Ian) McGrath

Impact Factor: 4.99

ISI Journal Citation Reports © Ranking: 2013: 21/256 (Pharmacology & Pharmacy)

Online ISSN: 1476-5381

Associated Title(s): British Journal of Clinical Pharmacology

Virtual Issue: G-protein coupled receptors (Sep 2009)


Virtual Issue: G-protein coupled receptors
(content last updated May 2012)

BJP has had a regular focus on GPCRs since 2009, including the following themed issues and sections:

Novel cAMP Signalling Paradigms
Guest Editor: Martina Schmidt - Volume 166 Issue 2 (May 2012)

Secretin Family (Class B) G Protein-Coupled Receptors - from Molecular to Clinical Perspectives
Guest Editors: David R Poyner and Debbie L Hay - Volume 166 Issue 1 (May 2012)

Molecular Pharmacology of GPCRs
Guest Editor: Roger J Summers - Volume 165 Issue 6 (March 2012)

Molecular Pharmacology of G Protein-Coupled Receptors
Guest Editor: RJ Summers - Volume 159 Issue 5 (March 2010)

GPCR
Guest Editors: G Milligan and JC McGrath - Volume 158, Issue 1 (September 2009)


Virtual Issue: G-protein coupled receptors (September 2009)

This virtual issue brings together a collection of papers and reviews covering a range of G-protein coupled receptors, organised by receptor type. It also incorporates some of the papers published in a BJP themed issue on GPCR from September 2009. The themed issue presents a range of work across the GPCR field, illustrating the emerging depth of understanding of the molecular interactions within GPCR signalling, the range of physiological systems and therapeutic applications that are becoming engaged, and the value of translating knowledge gained at different levels of organisation into an understanding at the organismal level. All articles are available FREE.

                                               Receptor Type Sub-headings
 

        5-HT Adenosine              α1-AR
 α2-AR Amino Acid Sensing Family Annexin-A1
 β-AR Cannabinoid
 CXCR2 and CXCR3 GPR119
 Histamine Melatonin
 Neuromedin U & S NPY
 Opioid Prostanoid
 Agonism Dimerisation
 Signalling Pathology or Therapeutic Applications
 Cardiovascular Cancer
 Neuro Lung
 Receptor Theory  

 

5-HT Adenosine


Triggering neurotrophic factor actions through adenosine A2A receptor activation: implications for neuroprotection
Ana M Sebastião, Joaquim A Ribeiro

The A2A-adenosine receptor: a GPCR with unique features?
J Zezula, M Freissmuth

Adenosine receptors and asthma in humans
C N Wilson

α1-AR


The α1L-adrenoceptor is an alternative phenotype of the α1A-adrenoceptor
C P Nelson

The α1A-adrenoceptor gene is required for the α1L-adrenoceptor-mediated response in isolated preparations of the mouse prostate
K T Gray, J L Short, S Ventura

α2-AR Amino Acid Sensing Family


Molecular basis for amino acid sensing by family C G-protein-coupled receptors
P Wellendorph, H Bräuner-Osborne

Annexin-A1


Annexin-A1: a pivotal regulator of the innate and adaptive immune systems
F D'Acquisto, M Perretti, R J Flower

β-AR


The rush to adrenaline: drugs in sport acting on the β-adrenergic system
E Davis, R Loiacono, R J Summers

β1- and β2-Adrenoceptor polymorphisms and cardiovascular diseases
Kirsten Leineweber, Gerd Heusch

Deciphering the β-adrenergic response in human embryonic stem cell-derived-cardiac myocytes: closer to clinical use?
D Catalucci, M L Bang, G Condorelli

β1- and β2-adrenoceptor responses in cardiomyocytes derived from human embryonic stem cells: comparison with failing and non-failing adult human heart
M Brito-Martins, S E Harding, N N Ali

Atypical pharmacologies at β-adrenoceptors
R J Summers

Metabolic responses to BRL37344 and clenbuterol in soleus muscle and C2C12 cells via different atypical pharmacologies and β2-adrenoceptor mechanisms
R A Ngala, J O'Dowd, S J Wang, A Agarwal, C Stocker, M A Cawthorne, J R S Arch

Agonist efficacy and receptor desensitization: from partial truths to a fuller picture
Steven J Charlton

Agonist-specific patterns of β2-adrenoceptor responses in human airway cells during prolonged exposure
Caroline Düringer, Gunilla Grundström, Eylem Gürcan, Ian A Dainty, Mandy Lawson, Solange H Korn, Anders Jerre, Hanna Falk Håkansson, Elisabet Wieslander, Karin Fredriksson, Carl Magnus Sköld, Magnus Löfdahl, Claes-Göran Löfdahl, David J Nicholls, David S Silberstein

On the mechanism of the persistent action of salmeterol: what is the current position?
RA Coleman

Molecular mechanisms for the persistent bronchodilatory effect of the β2-adrenoceptor agonist salmeterol
A Szczuka, M Wennerberg, A Packeu, G Vauquelin

Stimulation of cardiac β-adrenoceptors targets connexin 43
Kerstin Boengler

The signal transduction cascade regulating the expression of the gap junction protein connexin43 by β-adrenoceptors
A Salameh, S Krautblatter, S Karl, K Blanke, D Rojas Gomez, S Dhein, D Pfeiffer, J Janousek

Cannabinoid


CB2 cannabinoid receptors: new vistas
K Mackie, R A Ross

CXCR2 and CXCR3


Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist?
A Mueller

Analysis of the pharmacokinetic/pharmacodynamic relationship of a small molecule CXCR3 antagonist, NBI-74330, using a murine CXCR3 internalization assay
L A Jopling, G F Watt, S Fisher, H Birch, S Coggon, M I Christie

GPR119


GPR119, a novel G protein-coupled receptor target for the treatment of type 2 diabetes and obesity
H A Overton, M C T Fyfe, C Reynet

Histamine


Molecular and biochemical pharmacology of the histamine H4 receptor
Rob Leurs, Paul L Chazot, Fiona C Shenton, Herman D Lim, Iwan JP de Esch

Melatonin


Melatonin receptors, heterodimerization, signal transduction and binding sites: what's new?
R Jockers, P Maurice, J A Boutin, P Delagrange

Neuromedin U & S


Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin S
JD Mitchell, JJ Maguire, AP Davenport

NPY


Neuropeptide Y Y2 receptor in health and disease
S L Parker, A Balasubramaniam

Opioid


Agonist-selective mechanisms of GPCR desensitization
E Kelly, C P Bailey, G Henderson

Shadows across μ-Star? Constitutively active μ-opioid receptors revisited
Mark Connor

Neutral antagonist activity of naltrexone and 6β-naltrexol in naïve and opioid-dependent C6 cells expressing a µ-opioid receptor
MF Divin, FA Bradbury, FI Carroll, JR Traynor

Role of protein kinase C in functional selectivity for desensitization at the µ-opioid receptor: from pharmacological curiosity to therapeutic potential
Susan L Ingram, John R Traynor

Involvement of PKCα and G-protein-coupled receptor kinase 2 in agonist-selective desensitization of µ-opioid receptors in mature brain neurons
CP Bailey, S Oldfield, J Llorente, CJ Caunt, AG Teschemacher, L Roberts, CA McArdle, FL Smith, WL Dewey, E Kelly, G Henderson

Prostanoid


Prostanoid receptor antagonists: development strategies and therapeutic applications
RL Jones, MA Giembycz, DF Woodward

Agonism


Agonist-selective mechanisms of GPCR desensitization
E Kelly, C P Bailey, G Henderson

Conformational changes in G-protein-coupled receptors—the quest for functionally selective conformations is open
C Hoffmann, A Zürn, M Bünemann, M J Lohse

Agonist binding, agonist affinity and agonist efficacy at G protein-coupled receptors
P G Strange

G-protein-coupled receptor heteromers or how neurons can display differently flavoured patterns in response to the same neurotransmitter
Rafael Franco

G protein-coupled receptor hetero-dimerization: contribution to pharmacology and function
Graeme Milligan

Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3
Graeme Milligan, Leigh A. Stoddart, Nicola J. Smith

Atypical pharmacologies at β-adrenoceptors
R J Summers

Metabolic responses to BRL37344 and clenbuterol in soleus muscle and C2C12 cells via different atypical pharmacologies and β2-adrenoceptor mechanisms
R A Ngala, J O'Dowd, S J Wang, A Agarwal, C Stocker, M A Cawthorne, J R S Arch

Agonist efficacy and receptor desensitization: from partial truths to a fuller picture
Steven J Charlton

Agonist-specific patterns of β2-adrenoceptor responses in human airway cells during prolonged exposure
Caroline Düringer, Gunilla Grundström, Eylem Gürcan, Ian A Dainty, Mandy Lawson, Solange H Korn, Anders Jerre, Hanna Falk Håkansson, Elisabet Wieslander, Karin Fredriksson, Carl Magnus Sköld, Magnus Löfdahl, Claes-Göran Löfdahl, David J Nicholls, David S Silberstein

On the mechanism of the persistent action of salmeterol: what is the current position?
RA Coleman

Molecular mechanisms for the persistent bronchodilatory effect of the β2-adrenoceptor agonist salmeterol
A Szczuka, M Wennerberg, A Packeu, G Vauquelin

Dimerisation


A day in the life of a G protein-coupled receptor: the contribution to function of G protein-coupled receptor dimerization
G Milligan

G protein-coupled receptor hetero-dimerization: contribution to pharmacology and function
Graeme Milligan

Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3
Graeme Milligan, Leigh A. Stoddart, Nicola J. Smith

G-protein-coupled receptor heteromers: function and ligand pharmacology
R Franco, V Casadó, A Cortés, J Mallol, F Ciruela, S Ferré, C Lluis, E I Canela

Melatonin receptors, heterodimerization, signal transduction and binding sites: what's new?
R Jockers, P Maurice, J A Boutin, P Delagrange

On the fitting of binding data when receptor dimerization is suspected
J Giraldo

Modelling the interdependence between the stoichiometry of receptor oligomerization and ligand binding for a coexisting dimer/tetramer receptor system
X Rovira, M Vivó, J Serra, D Roche, PG Strange, J Giraldo

Signalling


β-arrestins and heterotrimeric G-proteins: collaborators and competitors in signal transduction
K DeFea

G-protein-coupled receptor phosphorylation: where, when and by whom
A B Tobin

Kinetics of G-protein-coupled receptor signals in intact cells
M J Lohse, P Hein, C Hoffmann, V O Nikolaev, J-P Vilardaga, M Bünemann

Annexin-A1: a pivotal regulator of the innate and adaptive immune systems
F D'Acquisto, M Perretti, R J Flower

cAMP signal transduction in the heart: understanding spatial control for the development of novel therapeutic strategies
Manuela Zaccolo

EPAC proteins transduce diverse cellular actions of cAMP
Gillian Borland, Brian O Smith, Stephen J Yarwood

Role of G12 proteins in oncogenesis and metastasis
Juhi Juneja, Patrick J Casey

Regulation of RhoGEF proteins by G12/13-coupled receptors
Sandra Siehler

Role of protein kinase C in functional selectivity for desensitization at the µ-opioid receptor: from pharmacological curiosity to therapeutic potential
Susan L Ingram, John R Traynor

Involvement of PKCα and G-protein-coupled receptor kinase 2 in agonist-selective desensitization of µ-opioid receptors in mature brain neurons
CP Bailey, S Oldfield, J Llorente, CJ Caunt, AG Teschemacher, L Roberts, CA McArdle, FL Smith, WL Dewey, E Kelly, G Henderson

Pathology or Therapeutic Applications


Neuropeptide Y Y2 receptor in health and disease
S L Parker, A Balasubramaniam

GPR119, a novel G protein-coupled receptor target for the treatment of type 2 diabetes and obesity
H A Overton, M C T Fyfe, C Reynet

The rush to adrenaline: drugs in sport acting on the β-adrenergic system
E Davis, R Loiacono, R J Summers

Annexin-A1: a pivotal regulator of the innate and adaptive immune systems
F D'Acquisto, M Perretti, R J Flower

Adenosine receptors and asthma in humans
C N Wilson

β1- and β2-Adrenoceptor polymorphisms and cardiovascular diseases
Kirsten Leineweber, Gerd Heusch

Role of G12 proteins in oncogenesis and metastasis
Juhi Juneja, Patrick J Casey

Prostanoid receptor antagonists: development strategies and therapeutic applications
RL Jones, MA Giembycz, DF Woodward

Deciphering the β-adrenergic response in human embryonic stem cell-derived-cardiac myocytes: closer to clinical use?
D Catalucci, M L Bang, G Condorelli

β1- and β2-adrenoceptor responses in cardiomyocytes derived from human embryonic stem cells: comparison with failing and non-failing adult human heart
M Brito-Martins, S E Harding, N N Ali

The α1L-adrenoceptor is an alternative phenotype of the α1A-adrenoceptor
C P Nelson

The α1A-adrenoceptor gene is required for the α1L-adrenoceptor-mediated response in isolated preparations of the mouse prostate
K T Gray, J L Short, S Ventura

Cardiovascular


cAMP signal transduction in the heart: understanding spatial control for the development of novel therapeutic strategies
Manuela Zaccolo

Cancer


Role of G12 proteins in oncogenesis and metastasis
Juhi Juneja, Patrick J Casey

Neuro


G-protein-coupled receptor heteromers or how neurons can display differently flavoured patterns in response to the same neurotransmitter
Rafael Franco

Lung


Agonist efficacy and receptor desensitization: from partial truths to a fuller picture
Steven J Charlton

Agonist-specific patterns of β2-adrenoceptor responses in human airway cells during prolonged exposure
Caroline Düringer, Gunilla Grundström, Eylem Gürcan, Ian A Dainty, Mandy Lawson, Solange H Korn, Anders Jerre, Hanna Falk Håkansson, Elisabet Wieslander, Karin Fredriksson, Carl Magnus Sköld, Magnus Löfdahl, Claes-Göran Löfdahl, David J Nicholls, David S Silberstein

On the mechanism of the persistent action of salmeterol: what is the current position?
RA Coleman

Molecular mechanisms for the persistent bronchodilatory effect of the β2-adrenoceptor agonist salmeterol
A Szczuka, M Wennerberg, A Packeu, G Vauquelin

Receptor Theory


Orphan GPCR research
S Chung, T Funakoshi, O Civelli

On the fitting of binding data when receptor dimerization is suspected
J Giraldo

Modelling the interdependence between the stoichiometry of receptor oligomerization and ligand binding for a coexisting dimer/tetramer receptor system
X Rovira, M Vivó, J Serra, D Roche, PG Strange, J Giraldo

G-protein-coupled receptor heteromers or how neurons can display differently flavoured patterns in response to the same neurotransmitter
Rafael Franco

Shadows across μ-Star? Constitutively active μ-opioid receptors revisited
Mark Connor

Neutral antagonist activity of naltrexone and 6β-naltrexol in naïve and opioid-dependent C6 cells expressing a µ-opioid receptor
MF Divin, FA Bradbury, FI Carroll, JR Traynor

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