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BJP Virtual Issues

The following virtual issues are available:

G-protein coupled receptors
Cannabinoids
Endothelium
Cancer

G-protein coupled receptors: Virtual Issue

This virtual issue brings together a collection of recent 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 recent BJP themed issue on GPCR. 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.

This web resource will be further supplemented in a few months time by a further GPCR Section containing reviews commissioned by guest editor Roger J. Summers.

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 A_2A-adenosine receptor: a GPCR with unique features?
J Zezula, M Freissmuth

Adenosine receptors and asthma in humans
C N Wilson

α1-AR

The α_1L-adrenoceptor is an alternative phenotype of the α_1A-adrenoceptor
C P Nelson

The α_1A-adrenoceptor gene is required for the α_1L-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

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

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 G_12/13-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

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 α_1L-adrenoceptor is an alternative phenotype of the α_1A-adrenoceptor
C P Nelson

The α_1A-adrenoceptor gene is required for the α_1L-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

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

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

Cannabinoids: Virtual Issue

In recent years, BJP has been at the forefront of cannabinoid publications, producing two highly successful Themed Issues on cannabinoids. We are planning a future Themed Issue on cannabinoids for publication in early 2010. For more information visit www.brjpharmacol.org.

In a special virtual issue, we have collated cannabinoid papers published in BJP over the last 12 months (back from June 2009) – see below. To access all cannabinoid papers published in BJP click here. If accessing this link for the first time, please also select ‘Go’ to activate the search.

Interaction between cannabinoid CB₁receptors and endogenous ATP in the control of spontaneous mechanical activity in mouse ileum
S Baldassano, MG Zizzo, R Serio, F Mulè

Potential anxiolytic- and antidepressant-like effects of salvinorin A, the main active ingredient of Salvia divinorum, in rodents
Daniela Braida, Valeria Capurro, Alessia Zani, Tiziana Rubino, Daniela Viganò, Daniela Parolaro, Mariaelvina Sala

Peripheral and central sites of action for the non-selective cannabinoid agonist WIN 55,212-2 in a rat model of post-operative pain
CZ Zhu, JP Mikusa, Y Fan, PR Hollingsworth, M Pai, P Chandran, AV Daza, BB Yao, MJ Dart, MD Meyer, MW Decker, GC Hsieh, P Honore

Peripheral endocannabinoid dysregulation in obesity: relation to intestinal motility and energy processing induced by food deprivation and re-feeding
Angelo A Izzo, Fabiana Piscitelli, Raffaele Capasso, Gabriella Aviello, Barbara Romano, Francesca Borrelli, Stefania Petrosino, Vincenzo Di Marzo

Positive allosteric modulation of the human cannabinoid (CB₁) receptor by RTI-371, a selective inhibitor of the dopamine transporter
Hernán A. Navarro, James L. Howard, Gerald T. Pollard, F. Ivy Carroll

The endocannabinoid system as a target for the treatment of motor dysfunction
Javier Fernández-Ruiz

Synthetic and plant-derived cannabinoid receptor antagonists show hypophagic properties in fasted and non-fasted mice
Gernot Riedel, Paola Fadda, Susan McKillop-Smith, Roger G Pertwee, Bettina Platt, Lianne Robinson

Inhibition of human recombinant T-type calcium channels by the endocannabinoid N-arachidonoyl dopamine
Hamish R Ross, Andrew J Gilmore, Mark Connor

Emerging strategies for exploiting cannabinoid receptor agonists as medicines
Roger G Pertwee

Acute hypertension reveals depressor and vasodilator effects of cannabinoids in conscious rats
W-S Vanessa Ho, Sheila M Gardiner

5-HT_1A receptors are involved in the cannabidiol-induced attenuation of behavioural and cardiovascular responses to acute restraint stress in rats
Leonardo B.M. Resstel, Rodrigo F. Tavares, Sabrina F.S. Lisboa, Sâmia R.L. Joca, Fernando M.A. Corrêa, Francisco S. Guimarães

Effect of Δ⁹-tetrahydrocannabinol, a cannabinoid receptor agonist, on the triggering of transient lower oesophageal sphincter relaxations in dogs and humans
H Beaumont, J Jensen, A Carlsson, M Ruth, A Lehmann, GE Boeckxstaens

Inhibition of fatty acid amide hydrolase produces PPAR-α-mediated analgesia in a rat model of inflammatory pain
D R Sagar, D A Kendall, V Chapman

Virodhamine relaxes the human pulmonary artery through the endothelial cannabinoid receptor and indirectly through a COX product
H Kozłowska, M Baranowska, E Schlicker, M Kozłowski, J Laudañski, B Malinowska

MDA7: a novel selective agonist for CB₂ receptors that prevents allodynia in rat neuropathic pain models
M Naguib, P Diaz, J J Xu, F Astruc-Diaz, S Craig, P Vivas-Mejia, D L Brown

Antinociceptive effects of tetrazole inhibitors of endocannabinoid inactivation: cannabinoid and non-cannabinoid receptor-mediated mechanisms
S Maione, E Morera, I Marabese, A Ligresti, L Luongo, G Ortar, V Di Marzo

Inhibitory effect of salvinorin A, from Salvia divinorum, on ileitis-induced hypermotility: cross-talk between κ-opioid and cannabinoid CB₁ receptors
R Capasso, F Borrelli, M G Cascio, G Aviello, K Huben, J K Zjawiony, P Marini, B Romano, V Di Marzo, F Capasso, A A Izzo

Modulation of the anti-nociceptive effects of 2-arachidonoyl glycerol by peripherally administered FAAH and MGL inhibitors in a neuropathic pain model
J Desroches, J Guindon, C Lambert, P Beaulieu

Inhibitory activity of the novel CB₂ receptor agonist, GW833972A, on guinea-pig and human sensory nerve function in the airways
M G Belvisi, H J Patel, V Freund-Michel, D J Hele, N Crispino, M A Birrell

Interactions between CB₁ receptors and TRPV1 channels mediated by 12-HPETE are cytotoxic to mesencephalic dopaminergic neurons
S R Kim, E Bok, Y C Chung, E S Chung, B K Jin

Inhibition of fatty acid amide hydrolase by kaempferol and related naturally occurring flavonoids
L Thors, M Belghiti, C J Fowler

Differential modulation of AP-1- and CRE-driven transcription by cannabinoid agonists emphasizes functional selectivity at the CB₁ receptor
B Bosier, E Hermans, D M Lambert

Cannabinoids reduce granuloma-associated angiogenesis in rats by controlling transcription and expression of mast cell protease-5
D De Filippis, A Russo, A D'Amico, G Esposito, P Concetta, M Cinelli, G Russo, T Iuvone

Effects of Δ⁹-tetrahydrocannabivarin on [³⁵S]GTPγS binding in mouse brain cerebellum and piriform cortex membranes
I Dennis, B J Whalley, G J Stephens

The cannabinoid receptor-1 antagonist rimonabant inhibits platelet activation and reduces pro-inflammatory chemokines and leukocytes in Zucker rats
A Schäfer, J Pfrang, J Neumüller, S Fiedler, G Ertl, J Bauersachs

Rimonabant in rats with a metabolic syndrome: good news after the depression
V Di Marzo, A Szallasi

The μ-opioid receptor agonist morphine, but not agonists at δ- or κ-opioid receptors, induces peripheral antinociception mediated by cannabinoid receptors
D da Fonseca Pacheco, A Klein, A de Castro Perez, C M da Fonseca Pacheco, J N de Francischi, I D G Duarte

Cannabidiol, extracted from Cannabis sativa, selectively inhibits inflammatory hypermotility in mice
R Capasso, F Borrelli, G Aviello, B Romano, C Scalisi, F Capasso, A A Izzo

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Free access to the two previous BJP cannabinoid Themed Issues – see below:

CB2 Receptors (January 2008)

Cannabinoid Pharmacology (November 2007)

Endothelium: Virtual Issue

We have collected below, reviews and research papers on the topic of the Endothelium that BJP and our sister journal BJCP have published in the past year, and that should help researchers and students to find the latest work in this field.

Many of these papers come from an endothelium themed section published to commemorate the work of Robert Furchgott who discovered endothelium-derived relaxant factor and who died on 12th May 2009. Furchgott was awarded the Nobel Prize for this work, which has led to an array of new therapeutic targets.

An “Appreciation” of Robert Furchgott can be found here – written by William Martin.

The themed section starts with an editorial, and contains three reviews on the pathophysiology of the endothelium and the drug targets that this presents, four research papers and three commentaries on research. These are all also included in the list below.

Reviews

Endothelial Function

Endothelium-dependent contractions in SHR: a tale of prostanoid TP and IP receptors
Michel Félétou, Tony J Verbeuren, Paul M Vanhoutte

Endothelial Pathophysiology

Role of nitroso radicals as drug targets in circulatory shock
Emanuela Esposito, Salvatore Cuzzocrea

Calcium-activated potassium channels and endothelial dysfunction: therapeutic options?
Michel Félétou

Endothelial Ca²⁺-activated K⁺ channels in normal and impaired EDHF–dilator responses – relevance to cardiovascular pathologies and drug discovery
Ivica Grgic, Brajesh P Kaistha, Joachim Hoyer, Ralf Köhler

Endothelium-dependent contractions and endothelial dysfunction in human hypertension
Daniele Versari, Elena Daghini, Agostino Virdis, Lorenzo Ghiadoni, Stefano Taddei

Research Papers with Commentaries

A role for nitroxyl (HNO) as an endothelium-derived relaxing and hyperpolarizing factor in resistance arteries
Karen L Andrews, Jennifer C Irvine, Marianne Tare, Jacqueline Apostolopoulos, Joanne L Favaloro, Chris R Triggle, Barbara K Kemp-Harper

Vascular K_ATP channels: dephosphorylation and deactivation
Paolo Tammaro

Ca²⁺/calcineurin regulation of cloned vascular K_ATP channels: crosstalk with the protein kinase A pathway
NN Orie, AM Thomas, BA Perrino, A Tinker, LH Clapp

Understanding organic nitrates – a vein hope?
Mark R Miller, Roger M Wadsworth

Different effects of ascorbate deprivation and classical vascular nitrate tolerance on aldehyde dehydrogenase-catalysed bioactivation of nitroglycerin
MV Wenzl, G Wölkart, H Stessel, M Beretta, K Schmidt, B Mayer

Research Papers

EDHF

Hypertension and the absence of EDHF-mediated responses favour endothelium-dependent contractions in renal arteries of the rat
F S Michel, G S Man, R Y K Man, P M Vanhoutte

Flow-induced enhancement of vasoconstriction and blockade of endothelium-derived hyperpolarizing factor (EDHF) by ascorbate in the rat mesentery
A Stirrat, S Nelli, F J Dowell, W Martin

Endothelial function

Enhanced antithrombotic effects of unfractionated heparin in rats after repeated oral doses and its relationship to endothelial heparin concentration
L M Hiebert, T Ping, S M Wice

Assessment of endothelial function: comparison of the pulse wave response to β₂-adrenoceptor stimulation with flow mediated dilatation
Curtis Rambaran, Benyu Jiang, James M. Ritter, Ajay Shah, Lalit Kalra, Philip J. Chowienczyk

Pharmacokinetic and pharmacodynamic properties of oral L-citrulline and L-arginine: impact on nitric oxide metabolism
Edzard Schwedhelm, Renke Maas, Ralf Freese, Donald Jung, Zoltan Lukacs, Alen Jambrecina, William Spickler, Friedrich Schulze, Rainer H. Böger

Lipoic acid supplementation and endothelial function
J-C Tardif, E Rhéaume

Effects of pre- vs. intra-dialysis folic acid on arterial wave reflections and endothelial function in patients with end-stage renal disease
Yuka Tochihara, Malcolm J. Whiting, Jeffrey A. Barbara, Arduino A. Mangoni

Transport of interleukin-1 across cerebromicrovascular endothelial cells
RA Skinner, RM Gibson, NJ Rothwell, E Pinteaux, JI Penny

Non-invasive measurement of the haemodynamic effects of inhaled salbutamol, intravenous L-arginine and sublingual nitroglycerin
Anna Tahvanainen, Miia Leskinen, Jenni Koskela, Erkki Ilveskoski, Juha Alanko, Mika Kähönen, Tiit Kööbi, Lauri Lehtimäki, Eeva Moilanen, Jukka Mustonen, Ilkka Pörsti

Endothelial Pathophysiology

Celecoxib modulates adhesion of HT29 colon cancer cells to vascular endothelial cells by inhibiting ICAM-1 and VCAM-1 expression
C Dianzani, L Brucato, M Gallicchio, A C Rosa, M Collino, R Fantozzi

Endothelium removal augments endothelium-independent vasodilatation in rat mesenteric vascular bed
Y Iwatani, K Kosugi, S Isobe-Oku, S Atagi, Y Kitamura, H Kawasaki

Effects of α-lipoic acid on endothelial function in aged diabetic and high-fat fed rats
C M Sena, E Nunes, T Louro, T Proença, R Fernandes, M R Boarder, R M Seiça

Raloxifene protects endothelial cell function against oxidative stress
C M Wong, L M Yung, F P Leung, S-Y Tsang, C L Au, Z-Y Chen, X Yao, C H K Cheng, C-W Lau, M Gollasch, Y Huang

Aldosterone induces endothelial dysfunction in resistance arteries from normotensive and hypertensive rats by increasing thromboxane A₂ and prostacyclin
F E Xavier, R Aras-López, I Arroyo-Villa, L del Campo, M Salaices, L V Rossoni, M Ferrer, G Balfagón

Increased endothelin-1 reactivity and endothelial dysfunction in carotid arteries from rats with hyperhomocysteinemia
CR de Andrade, PF Leite, AC Montezano, DA Casolari, A Yogi, RC Tostes, R Haddad, MN Eberlin, FRM Laurindo, HP de Souza, FMA Corrêa, AM de Oliveira

Inflammation

Ethyl pyruvate modulates acute inflammatory reactions in human endothelial cells in relation to the NF-κB pathway
A-S Johansson, K Johansson-Haque, S Okret, J Palmblad

Secretory PLA₂inhibitor indoxam suppresses LDL modification and associated inflammatory responses in TNF α-stimulated human endothelial cells
K Sonoki, M Iwase, N Sasaki, S Ohdo, S Higuchi, Y Takata, M Iida

Signalling / Drug targets

Contribution of the M₃ muscarinic receptors to the vasodilator response to acetylcholine in the human forearm vascular bed
Teresa M. Attinà, James J. Oliver, Lorenzo S. Malatino, David J. Webb

Short-term or long-term treatments with a phosphodiesterase-4 (PDE4) inhibitor result in opposing agonist-induced Ca²⁺ responses in endothelial cells
M Campos-Toimil, T Keravis, F Orallo, K Takeda, C Lugnier

Oxytocin stimulates migration and invasion in human endothelial cells
M G Cattaneo, B Chini, L M Vicentini

Endothelial α₁-adrenoceptors regulate neo-angiogenesis
M Ciccarelli, G Santulli, A Campanile, G Galasso, P Cervèro, G G Altobelli, V Cimini, L Pastore, F Piscione, B Trimarco, G Iaccarino

Activation of ET_Breceptors regulates the abundance of ET-1 mRNA in vascular endothelial cells
N Farhat, C C Matouk, A M Mamarbachi, P A Marsden, B G Allen, E Thorin

Smooth muscle α_1D-adrenoceptors mediate phenylephrine-induced vasoconstriction and increases in endothelial cell Ca²⁺ in hamster cremaster arterioles
W F Jackson, E M Boerman, E J Lange, S S Lundback, K D Cohen

H₂S-donating sildenafil (ACS6) inhibits superoxide formation and gp91^phox expression in arterial endothelial cells: role of protein kinases A and G
S Muzaffar, J Y Jeremy, A Sparatore, P Del Soldato, G D Angelini, N Shukla

Oleanolic acid induces relaxation and calcium-independent release of endothelium-derived nitric oxide
R Rodriguez-Rodriguez, E Stankevicius, M D Herrera, L Østergaard, M R Andersen, V Ruiz-Gutierrez, U Simonsen

Effects of chronic in vivo administration of nitroglycerine on ACh-induced endothelium-dependent relaxation in rabbit cerebral arteries
Y Watanabe, N Kusama, T Itoh

Resveratrol reduces endothelial progenitor cells senescence through augmentation of telomerase activity by Akt-dependent mechanisms
L Xia, X X Wang, X S Hu, X G Guo, Y P Shang, H J Chen, C L Zeng, F R Zhang, J Z Chen

Kaempferol stimulates large conductance Ca²⁺-activated K⁺ (BK_Ca) channels in human umbilical vein endothelial cells via a cAMP/PKA-dependent pathway
Y C Xu, G P H Leung, P Y D Wong, P M Vanhoutte, R Y K Man

Levosimendan induces NO production through p38 MAPK, ERK and Akt in porcine coronary endothelial cells: role for mitochondrial K_ATP channel
E Grossini, C Molinari, PP Caimmi, F Uberti, G Vacca

Myoendothelial coupling in the mesenteric arterial bed; segmental differences and interplay between nitric oxide and endothelin-1
RHP Hilgers, JGR De Mey

Protopanaxadiol and protopanaxatriol bind to glucocorticoid and oestrogen receptors in endothelial cells
Kar Wah Leung, Fung Ping Leung, Nai Ki Mak, Joyce Tombran-Tink, Yu Huang, Ricky NS Wong

Mechanisms of U46619-induced contraction of rat pulmonary arteries in the presence and absence of the endothelium
C McKenzie, A MacDonald, AM Shaw

Amiloride derivatives induce apoptosis by depleting ER Ca²⁺ stores in vascular endothelial cells
KS Park, D Poburko, CB Wollheim, N Demaurex

Cancer: Virtual Issue

This virtual issue brings together a collection of recent cancer papers and reviews that have been well-read and cited, demonstrating the range of our coverage: from characterisation of new drug targets to investigation of novel therapeutics and mechanistic studies of known drugs, using a wide range of in vitro and in vivo approaches.

Heparanase: a target for drug discovery in cancer and inflammation
E A McKenzie

A cellular and molecular investigation of the action of PMX464, a putative thioredoxin inhibitor, in normal and colorectal cancer cell lines
A Mukherjee, K Huber, H Evans, N Lakhani, S Martin

Telomerase and its potential for therapeutic intervention
P Phatak, A M Burger

Biomarker method validation in anticancer drug development
J Cummings, T H Ward, A Greystoke, M Ranson, C Dive

Inhibitors of histone deacetylase (HDAC) restore the p53 pathway in neuroblastoma cells
F Condorelli, I Gnemmi, A Vallario, A A Genazzani, P L Canonico

Celecoxib decreases expression of the adhesion molecules ICAM-1 and VCAM-1 in a colon cancer cell line (HT29)
M Gallicchio, A C Rosa, C Dianzani, L Brucato, E Benetti, M Collino, R Fantozzi

5-Aza-2'-deoxycytidine suppresses human renal carcinoma cell growth in a xenograft model via up-regulation of the connexin 32 gene
H Hagiwara, H Sato, Y Ohde, Y Takano, T Seki, T Ariga, N Hokaiwado, M Asamoto, T Shirai, Y Nagashima, T Yano

Tumour endoproteases: the cutting edge of cancer drug delivery?
J M Atkinson, C S Siller, J H Gill

Photodynamic activity of BAM-SiPc, an unsymmetrical bisamino silicon(IV) phthalocyanine, in tumour-bearing nude mice
S C H Leung, P-C Lo, D K P Ng, W-K Liu, K-P Fung, W-P Fong

Discovery and biological characterization of a novel series of androgen receptor modulators
C Zhou, G Wu, Y Feng, Q Li, H Su, D E Mais, Y Zhu, N Li, Y Deng, D Yang, M-W Wang

Cancer and the blood-brain barrier: 'Trojan horses' for courses? M Mazza, I F Uchegbu, A G Schätzlein

Alpha-2 adrenoceptor action on cell proliferation and mammary tumour growth in mice
A Bruzzone, C Pérez Piñero, L F Castillo, M G Sarappa, P Rojas, C Lanari, I A Lüthy

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