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Differential regulation of β2-adrenoceptor and adenosine A2B receptor signalling by GRK and arrestin proteins in arterial smooth muscle.

Nash CA, Nelson CP, Mistry R, Moeller-Olsen C, Christofidou E, Challiss RAJ, Willets JM.

Cell Signal. 2018 Nov;51:86-98. doi: 10.1016/j.cellsig.2018.07.013. Epub 2018 Jul 31.


Small-Molecule G Protein-Coupled Receptor Kinase Inhibitors Attenuate G Protein-Coupled Receptor Kinase 2-Mediated Desensitization of Vasoconstrictor-Induced Arterial Contractions.

Rainbow RD, Brennan S, Jackson R, Beech AJ, Bengreed A, Waldschmidt HV, Tesmer JJG, Challiss RAJ, Willets JM.

Mol Pharmacol. 2018 Sep;94(3):1079-1091. doi: 10.1124/mol.118.112524. Epub 2018 Jul 6.


Ligand-Specific Signaling Profiles and Resensitization Mechanisms of the Neuromedin U2 Receptor.

Alhosaini K, Bahattab O, Qassam H, Challiss RAJ, Willars GB.

Mol Pharmacol. 2018 Jul;94(1):674-688. doi: 10.1124/mol.117.111070. Epub 2018 May 3.


Nitric oxide-mediated posttranslational modifications control neurotransmitter release by modulating complexin farnesylation and enhancing its clamping ability.

Robinson SW, Bourgognon JM, Spiers JG, Breda C, Campesan S, Butcher A, Mallucci GR, Dinsdale D, Morone N, Mistry R, Smith TM, Guerra-Martin M, Challiss RAJ, Giorgini F, Steinert JR.

PLoS Biol. 2018 Apr 9;16(4):e2003611. doi: 10.1371/journal.pbio.2003611. eCollection 2018 Apr.


HMGB1 is upregulated in the airways in asthma and potentiates airway smooth muscle contraction via TLR4.

Di Candia L, Gomez E, Venereau E, Chachi L, Kaur D, Bianchi ME, Challiss RAJ, Brightling CE, Saunders RM.

J Allergy Clin Immunol. 2017 Aug;140(2):584-587.e8. doi: 10.1016/j.jaci.2016.11.049. Epub 2017 Mar 1. No abstract available.


An Antibody Biosensor Establishes the Activation of the M1 Muscarinic Acetylcholine Receptor during Learning and Memory.

Butcher AJ, Bradley SJ, Prihandoko R, Brooke SM, Mogg A, Bourgognon JM, Macedo-Hatch T, Edwards JM, Bottrill AR, Challiss RA, Broad LM, Felder CC, Tobin AB.

J Biol Chem. 2016 Apr 22;291(17):8862-75. doi: 10.1074/jbc.M115.681726. Epub 2016 Jan 29.


Distinct and complementary roles for α and β isoenzymes of PKC in mediating vasoconstrictor responses to acutely elevated glucose.

Jackson R, Brennan S, Fielding P, Sims MW, Challiss RA, Adlam D, Squire IB, Rainbow RD.

Br J Pharmacol. 2016 Mar;173(5):870-87. doi: 10.1111/bph.13399. Epub 2016 Feb 8.


Biosynthetic infochemical communication.

Olsson SB, Challiss RA, Cole M, Gardeniers JG, Gardner JW, Guerrero A, Hansson BS, Pearce TC.

Bioinspir Biomim. 2015 Jul 9;10(4):043001. doi: 10.1088/1748-3190/10/4/043001. Review.


British Pharmacological Society, 5th Focused Meeting on Cell Signalling: Matters arising ….

Willars GB, Tobin AB, Challiss RA.

Br J Pharmacol. 2015 Jul;172(13):3194-5. doi: 10.1111/bph.13171. No abstract available.


Defining the roles of arrestin2 and arrestin3 in vasoconstrictor receptor desensitization in hypertension.

Willets JM, Nash CA, Rainbow RD, Nelson CP, Challiss RA.

Am J Physiol Cell Physiol. 2015 Aug 1;309(3):C179-89. doi: 10.1152/ajpcell.00079.2015. Epub 2015 May 13.


No evidence for altered intracellular calcium-handling in airway smooth muscle cells from human subjects with asthma.

Sweeney D, Hollins F, Gomez E, Mistry R, Saunders R, Challiss RA, Brightling CE.

BMC Pulm Med. 2015 Feb 13;15:12. doi: 10.1186/s12890-015-0009-z.


Steady-state modulation of voltage-gated K+ channels in rat arterial smooth muscle by cyclic AMP-dependent protein kinase and protein phosphatase 2B.

Brignell JL, Perry MD, Nelson CP, Willets JM, Challiss RA, Davies NW.

PLoS One. 2015 Mar 20;10(3):e0121285. doi: 10.1371/journal.pone.0121285. eCollection 2015.


[Ca2+]i oscillations in ASM: relationship with persistent airflow obstruction in asthma.

Sweeney D, Hollins F, Gomez E, Saunders R, Challiss RA, Brightling CE.

Respirology. 2014 Jul;19(5):763-6. doi: 10.1111/resp.12318. Epub 2014 May 22.


Long-term channel block is required to inhibit cellular transformation by human ether-à-go-go-related gene (hERG1) potassium channels.

Pier DM, Shehatou GS, Giblett S, Pullar CE, Trezise DJ, Pritchard CA, Challiss RA, Mitcheson JS.

Mol Pharmacol. 2014 Aug;86(2):211-21. doi: 10.1124/mol.113.091439. Epub 2014 May 15.


Novel structural and functional insights into M3 muscarinic receptor dimer/oligomer formation.

Hu J, Hu K, Liu T, Stern MK, Mistry R, Challiss RA, Costanzi S, Wess J.

J Biol Chem. 2013 Nov 29;288(48):34777-90. doi: 10.1074/jbc.M113.503714. Epub 2013 Oct 16.


Nitric oxide synthesis and cGMP production is important for neurite growth and synapse remodeling after axotomy.

Cooke RM, Mistry R, Challiss RA, Straub VA.

J Neurosci. 2013 Mar 27;33(13):5626-37. doi: 10.1523/JNEUROSCI.3659-12.2013.


G protein-coupled receptor signalling in astrocytes in health and disease: a focus on metabotropic glutamate receptors.

Bradley SJ, Challiss RA.

Biochem Pharmacol. 2012 Aug 1;84(3):249-59. doi: 10.1016/j.bcp.2012.04.009. Epub 2012 Apr 15. Review.


FRET-based detection of M1 muscarinic acetylcholine receptor activation by orthosteric and allosteric agonists.

Markovic D, Holdich J, Al-Sabah S, Mistry R, Krasel C, Mahaut-Smith MP, Challiss RA.

PLoS One. 2012;7(1):e29946. doi: 10.1371/journal.pone.0029946. Epub 2012 Jan 17.


Arrestins 2 and 3 differentially regulate ETA and P2Y2 receptor-mediated cell signaling and migration in arterial smooth muscle.

Morris GE, Nelson CP, Brighton PJ, Standen NB, Challiss RA, Willets JM.

Am J Physiol Cell Physiol. 2012 Mar 1;302(5):C723-34. doi: 10.1152/ajpcell.00202.2011.. Epub 2011 Dec 7.


Increased nicotinamide adenine dinucleotide phosphate oxidase 4 expression mediates intrinsic airway smooth muscle hypercontractility in asthma.

Sutcliffe A, Hollins F, Gomez E, Saunders R, Doe C, Cooke M, Challiss RA, Brightling CE.

Am J Respir Crit Care Med. 2012 Feb 1;185(3):267-74. doi: 10.1164/rccm.201107-1281OC. Epub 2011 Nov 22.


Structural aspects of M₃ muscarinic acetylcholine receptor dimer formation and activation.

Hu J, Thor D, Zhou Y, Liu T, Wang Y, McMillin SM, Mistry R, Challiss RA, Costanzi S, Wess J.

FASEB J. 2012 Feb;26(2):604-16. doi: 10.1096/fj.11-191510. Epub 2011 Oct 26.


A model for Ca2+ oscillations stimulated by the type 5 metabotropic glutamate receptor: an unusual mechanism based on repetitive, reversible phosphorylation of the receptor.

Dupont G, Lokenye EF, Challiss RA.

Biochimie. 2011 Dec;93(12):2132-8. doi: 10.1016/j.biochi.2011.09.010. Epub 2011 Sep 17.


Receptors: GPCR-G protein preassembly?

Challiss RA, Wess J.

Nat Chem Biol. 2011 Sep 19;7(10):657-8. doi: 10.1038/nchembio.665. No abstract available.


The use of translocating fluorescent biosensors for real-time monitoring of GPCR-mediated signaling events.

Nelson CP, Challiss RA.

Methods Mol Biol. 2011;746:329-43. doi: 10.1007/978-1-61779-126-0_18.


[³⁵S]GTPγS binding as an index of total G-protein and Gα-subtype-specific activation by GPCRs.

Mistry R, Dowling MR, Challiss RA.

Methods Mol Biol. 2011;746:263-75. doi: 10.1007/978-1-61779-126-0_14.


Principal role of adenylyl cyclase 6 in K⁺ channel regulation and vasodilator signalling in vascular smooth muscle cells.

Nelson CP, Rainbow RD, Brignell JL, Perry MD, Willets JM, Davies NW, Standen NB, Challiss RA.

Cardiovasc Res. 2011 Sep 1;91(4):694-702. doi: 10.1093/cvr/cvr137. Epub 2011 May 23.


Clustered coding variants in the glutamate receptor complexes of individuals with schizophrenia and bipolar disorder.

Frank RA, McRae AF, Pocklington AJ, van de Lagemaat LN, Navarro P, Croning MD, Komiyama NH, Bradley SJ, Challiss RA, Armstrong JD, Finn RD, Malloy MP, MacLean AW, Harris SE, Starr JM, Bhaskar SS, Howard EK, Hunt SE, Coffey AJ, Ranganath V, Deloukas P, Rogers J, Muir WJ, Deary IJ, Blackwood DH, Visscher PM, Grant SG.

PLoS One. 2011 Apr 29;6(4):e19011. doi: 10.1371/journal.pone.0019011.


Defining protein kinase/phosphatase isoenzymic regulation of mGlu₅ receptor-stimulated phospholipase C and Ca²⁺ responses in astrocytes.

Bradley SJ, Challiss RA.

Br J Pharmacol. 2011 Sep;164(2b):755-71. doi: 10.1111/j.1476-5381.2011.01421.x.


Early failure of N-methyl-D-aspartate receptors and deficient spine formation induced by reduction of regulatory heme in neurons.

Chernova T, Steinert JR, Richards P, Mistry R, Challiss RA, Jukes-Jones R, Cain K, Smith AG, Forsythe ID.

Mol Pharmacol. 2011 May;79(5):844-54. doi: 10.1124/mol.110.069831. Epub 2011 Feb 15.


Quantitative analysis reveals multiple mechanisms of allosteric modulation of the mGlu5 receptor in rat astroglia.

Bradley SJ, Langmead CJ, Watson JM, Challiss RA.

Mol Pharmacol. 2011 May;79(5):874-85. doi: 10.1124/mol.110.068882. Epub 2011 Feb 14.


Arrestins differentially regulate histamine- and oxytocin-evoked phospholipase C and mitogen-activated protein kinase signalling in myometrial cells.

Brighton PJ, Rana S, Challiss RJ, Konje JC, Willets JM.

Br J Pharmacol. 2011 Apr;162(7):1603-17. doi: 10.1111/j.1476-5381.2010.01173.x.


G protein-coupled receptor kinase 2 and arrestin2 regulate arterial smooth muscle P2Y-purinoceptor signalling.

Morris GE, Nelson CP, Everitt D, Brighton PJ, Standen NB, Challiss RA, Willets JM.

Cardiovasc Res. 2011 Jan 1;89(1):193-203. doi: 10.1093/cvr/cvq249. Epub 2010 Aug 12.


Contrasting effects of allosteric and orthosteric agonists on m1 muscarinic acetylcholine receptor internalization and down-regulation.

Thomas RL, Langmead CJ, Wood MD, Challiss RA.

J Pharmacol Exp Ther. 2009 Dec;331(3):1086-95. doi: 10.1124/jpet.109.160242. Epub 2009 Sep 18.


Endothelin signalling in arterial smooth muscle is tightly regulated by G protein-coupled receptor kinase 2.

Morris GE, Nelson CP, Standen NB, Challiss RA, Willets JM.

Cardiovasc Res. 2010 Feb 1;85(3):424-33. doi: 10.1093/cvr/cvp310. Epub 2009 Sep 11.


Effects of positive allosteric modulators on single-cell oscillatory Ca2+ signaling initiated by the type 5 metabotropic glutamate receptor.

Bradley SJ, Watson JM, Challiss RA.

Mol Pharmacol. 2009 Dec;76(6):1302-13. doi: 10.1124/mol.109.059170. Epub 2009 Sep 8.


Alternative splicing of G protein-coupled receptors: physiology and pathophysiology.

Markovic D, Challiss RA.

Cell Mol Life Sci. 2009 Oct;66(20):3337-52. doi: 10.1007/s00018-009-0093-4. Epub 2009 Jul 23. Review.


Characterization of anandamide-stimulated cannabinoid receptor signaling in human ULTR myometrial smooth muscle cells.

Brighton PJ, McDonald J, Taylor AH, Challiss RA, Lambert DG, Konje JC, Willets JM.

Mol Endocrinol. 2009 Sep;23(9):1415-27. doi: 10.1210/me.2009-0097. Epub 2009 May 28.


Regulation of oxytocin receptor responsiveness by G protein-coupled receptor kinase 6 in human myometrial smooth muscle.

Willets JM, Brighton PJ, Mistry R, Morris GE, Konje JC, Challiss RA.

Mol Endocrinol. 2009 Aug;23(8):1272-80. doi: 10.1210/me.2009-0047. Epub 2009 May 7.


Altered M(1) muscarinic acetylcholine receptor (CHRM1)-Galpha(q/11) coupling in a schizophrenia endophenotype.

Salah-Uddin H, Scarr E, Pavey G, Harris K, Hagan JJ, Dean B, Challiss RA, Watson JM.

Neuropsychopharmacology. 2009 Aug;34(9):2156-66. doi: 10.1038/npp.2009.41. Epub 2009 Apr 29.


Nitric oxide is a volume transmitter regulating postsynaptic excitability at a glutamatergic synapse.

Steinert JR, Kopp-Scheinpflug C, Baker C, Challiss RA, Mistry R, Haustein MD, Griffin SJ, Tong H, Graham BP, Forsythe ID.

Neuron. 2008 Nov 26;60(4):642-56. doi: 10.1016/j.neuron.2008.08.025.


Visualizing the temporal effects of vasoconstrictors on PKC translocation and Ca2+ signaling in single resistance arterial smooth muscle cells.

Nelson CP, Willets JM, Davies NW, Challiss RA, Standen NB.

Am J Physiol Cell Physiol. 2008 Dec;295(6):C1590-601. doi: 10.1152/ajpcell.00365.2008. Epub 2008 Oct 1.


G protein coupling and signaling pathway activation by m1 muscarinic acetylcholine receptor orthosteric and allosteric agonists.

Thomas RL, Mistry R, Langmead CJ, Wood MD, Challiss RA.

J Pharmacol Exp Ther. 2008 Nov;327(2):365-74. doi: 10.1124/jpet.108.141788. Epub 2008 Jul 29.


Selective regulation of H1 histamine receptor signaling by G protein-coupled receptor kinase 2 in uterine smooth muscle cells.

Willets JM, Taylor AH, Shaw H, Konje JC, Challiss RA.

Mol Endocrinol. 2008 Aug;22(8):1893-907. doi: 10.1210/me.2007-0463. Epub 2008 May 29.


Pharmacological assessment of m1 muscarinic acetylcholine receptor-gq/11 protein coupling in membranes prepared from postmortem human brain tissue.

Salah-Uddin H, Thomas DR, Davies CH, Hagan JJ, Wood MD, Watson JM, Challiss RA.

J Pharmacol Exp Ther. 2008 Jun;325(3):869-74. doi: 10.1124/jpet.108.137968. Epub 2008 Mar 5.


Regulation of cyclic AMP response-element binding-protein (CREB) by Gq/11-protein-coupled receptors in human SH-SY5Y neuroblastoma cells.

Rosethorne EM, Nahorski SR, Challiss RA.

Biochem Pharmacol. 2008 Feb 15;75(4):942-55. Epub 2007 Oct 22.


Compartmentalized signalling in neurons.

Pedarzani P, Cockcroft S, Challiss RA.

J Physiol. 2007 Oct 15;584(2):371-2. doi: 10.1113/jphysiol.2007.144766. No abstract available.


The regulation of M1 muscarinic acetylcholine receptor desensitization by synaptic activity in cultured hippocampal neurons.

Willets JM, Nelson CP, Nahorski SR, Challiss RA.

J Neurochem. 2007 Dec;103(6):2268-80. Epub 2007 Oct 1.


"Phenotypic" pharmacology: the influence of cellular environment on G protein-coupled receptor antagonist and inverse agonist pharmacology.

Nelson CP, Challiss RA.

Biochem Pharmacol. 2007 Mar 15;73(6):737-51. Epub 2006 Sep 12. Review.


Modulation of Gq-protein-coupled inositol trisphosphate and Ca2+ signaling by the membrane potential.

Billups D, Billups B, Challiss RA, Nahorski SR.

J Neurosci. 2006 Sep 27;26(39):9983-95.

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