Research Output

2011

Status of GPCR modeling and docking as reflected by community-wide GPCR Dock 2010 assessment

Kufareva, I., Rueda, M., Katritch, V., Stevens, R. C., Abagyan, R., McRobb, F. M., Capuano, B., Crosby, I. T., Chalmers, D. K., Yuriev, E., Simms, J. W., Sexton, P., Wootten, D. L. & Hall, N. E., 2011, In : Structure. 19, 8, p. 1108 - 1126 19 p.

Research output: Contribution to journalArticleResearchpeer-review

229 Citations (Scopus)

Structure activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A)

van Veldhoven, J. P. D., Blad, C. C., Artsen, C. M., Klopman, C., Wolfram, D. R., Abdelkadir, M. J., Lane, J., Brussee, J. & IJzerman, A. P., 2011, In : Bioorganic and Medicinal Chemistry Letters. 21, 9, p. 2736 - 2739 4 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)

Structure-function analysis of amino acid 74 of human RAMP1 and RAMP3 and its role in peptide interactions with adrenomedullin and calcitonin gene-related peptide receptors

Qi, T., Ly, K., Poyner, D. R., Christopoulos, G., Sexton, P. & Hay, D. L., 2011, In : Peptides. 32, 5, p. 1060 - 1067 8 p.

Research output: Contribution to journalArticleResearchpeer-review

20 Citations (Scopus)

The role of placental homeobox genes in human fetal growth restriction

Murthi, P., Rajaraman, G., Brennecke, S. P. & Kalionis, B., 2011, In : Journal of Pregnancy. 2011, 11 p., 548171.

Research output: Contribution to journalReview ArticleResearchpeer-review

Open Access
8 Citations (Scopus)

The role of transmembrane domain 3 (Tmiii) in the actions of orthosteric, allosteric and atypical agonists of the M4 muscarinic acetylcholine receptor

Leach, K., Davey, A. E., Felder, C. C., Sexton, P. & Christopoulos, A., 2011, In : Molecular Pharmacology. 79, 5, p. 855 - 865 11 p.

Research output: Contribution to journalArticleResearchpeer-review

22 Citations (Scopus)

The Structure of the Adenosine Receptors: Implications for Drug Discovery

Lane, J. R., Jaakola, V-P. & IJzerman, A. P., 2011, Advances in Pharmacology: Pharmacology of Purine and Pyrimidine Receptors. Jacobson, K. A. & Linden, J. (eds.). Amsterdam The Netherlands: Elsevier, Vol. 61. p. 1-40 40 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

9 Citations (Scopus)

Transient receptor potential ankyrin 1 is expressed by inhibitory motoneurons of the mouse intestine

Poole, D., Pelayo, J-C., Cattaruzza, F., Kuo, Y., Gai, G., Chiu, J., Bron, R., Furness, J., Grady, E. & Bunnett, N., 2011, In : Gastroenterology. 141, p. 565 - 575 11 p.

Research output: Contribution to journalArticleResearchpeer-review

62 Citations (Scopus)

β1-adrenergic receptors increase UCP1 in human MADS brown adipocytes and rescue cold-acclimated β3-adrenergic receptor knockout mice via nonshivering thermogenesis

Mattsson, C. L., Csikasz, R. I., Chernogubova, E., Yamamoto, D. L., Hogberg, H. T., Amri, E-Z., Hutchinson, D. S. & Bengtsson, T., Dec 2011, In : American Journal of Physiology - Endocrinology and Metabolism. 301, 6, 11 p.

Research output: Contribution to journalArticleResearchpeer-review

39 Citations (Scopus)
2010

AKAP79/150 interacts with AC8 and regulates Ca2+-dependent cAMP synthesis in pancreatic and neuronal systems

Willoughby, D., Masada, N., Wachten, S., Pagano, M., Halls, M., Everett, K., Ciruela, A. & Cooper, D., 2010, In : The Journal of Biological Chemistry. 285, 26, p. 20328 - 20342 15 p.

Research output: Contribution to journalArticleResearchpeer-review

59 Citations (Scopus)

A novel chemogenomics analysis of G protein-coupled receptors (GPCRs) and their ligands: a potential strategy for receptor de-orphanization

Horst, E., Peironcely, J., IJzerman, A. P., Beukers, M., Lane, J., van Vlijmen, H., Emmerich, M., Okuno, Y. & Bender, A., 2010, In : BMC Bioinformatics. 11, 316, p. 1 - 12 12 p.

Research output: Contribution to journalArticleResearchpeer-review

41 Citations (Scopus)

A role for transient receptor potential vanilloid 4 in tonicity-induced neurogenic inflammation

Vergnolle, N., Cenac, N., Altier, C., Cellars, L., Chapman, K., Zamponi, G., Materazzi, S., Nassini, R., Liedtke, W., Cattaruzza, F., Grady, E., Geppetti, P. & Bunnett, N., 2010, In : British Journal of Pharmacology. 159, 5, p. 1161 - 1173 13 p.

Research output: Contribution to journalArticleResearchpeer-review

62 Citations (Scopus)

Characterization of [3H]LUF5834: a novel non-ribose high-affinity agonist radioligand for the adenosine A1 receptor

Lane, J., Klaasse, E., Lin, J., van Bruchem, J., Beukers, M. & IJzerman, A. P., 2010, In : Biochemical Pharmacology. 80, 8, p. 1180 - 1189 10 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

Discovery of a novel chemical class of mGlu5 allosteric ligands with distinct modes of pharmacology

Hammond, A., Rodriguez, A., Townsend, S., Niswender, C., Gregory, K., Lindsley, C. & Conn, P., 2010, In : ACS Chemical Neuroscience. 1, 10, p. 702 - 716 15 p.

Research output: Contribution to journalArticleResearchpeer-review

59 Citations (Scopus)

Effects of N-acetyl-cysteine treatment on glutathione depletion and a short-term spatial memory deficit in 2-cyclohexene-1-one-treated rats

Choy, K. H. C., Dean, O., Berk, M., Bush, A. I. & van den Buuse, M., Dec 2010, In : European Journal of Pharmacology. 649, 1-3, p. 224-228 5 p.

Research output: Contribution to journalArticleResearchpeer-review

48 Citations (Scopus)

Hybrid ortho/allosteric ligands for the adenosine A1 receptor

Narlawar, R., Lane, J., Doddareddy, M., Lin, J., Brussee, J. & IJzerman, A. P., 2010, In : Journal of Medicinal Chemistry. 53, 8, p. 3028 - 3037 10 p.

Research output: Contribution to journalArticleResearchpeer-review

64 Citations (Scopus)

Ligand binding and subtype selectivity of the human A2A adenosine receptor: Identification and characterization of essential amino acid residues

Jaakola, V-P., Lane, J., Lin, J., Katritch, V., IJzerman, A. P. & Stevens, R., 2010, In : The Journal of Biological Chemistry. 285, 17, p. 13032 - 13044 13 p.

Research output: Contribution to journalArticleResearchpeer-review

73 Citations (Scopus)

Measurement of ligand-G protein-coupled receptor interactions

Leach, K., Valant, C., Sexton, P. M. & Christopoulos, A., 25 Jan 2010, G Protein-Coupled Receptors: Essential Methods. Poyner, D. R. & Wheatley, M. (eds.). Chichester UK: Wiley-Blackwell, p. 1-29 29 p. (Proteins & Macromolecules).

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

2 Citations (Scopus)

Molecular pharmacology of G protein-coupled receptors: Editorial

Summers, R., 2010, In : British Journal of Pharmacology. 159, 5, p. 983 - 985 3 p.

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

Overview of receptor allosterism

Gregory, K., Sexton, P. & Christopoulos, A., Dec 2010, In : Current Protocols in Pharmacology. Chapter 1, Supp 51, p. 1.21-1 - 1.21-34 1 p.

Research output: Contribution to journalArticleResearchpeer-review

32 Citations (Scopus)

Pungent general anesthetics activate transient receptor potential-A1 to produce hyperalgesia and neurogenic bronchoconstriction

Eilers, H., Cattaruzza, F., Nassini, R., Materazzi, S., Andre, E., Chu, C., Cottrell, G., Schumacher, M., Geppetti, P. & Bunnett, N., 2010, In : Anesthesiology. 112, 6, p. 1452 - 1463 12 p.

Research output: Contribution to journalArticleResearchpeer-review

46 Citations (Scopus)

Second Messenger Assays for G Protein-Coupled Receptors: cAMP, Ca2+, Inositol Phosphates, ERK1/2

Gregory, K. J., Sexton, P. M., Christopoulos, A. & Hick, C. A., 25 Jan 2010, G Protein-Coupled Receptors: Essential Methods. Wiley-Blackwell, p. 31-52 22 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

1 Citation (Scopus)

Structure-based discovery of novel chemotypes for adenosine A2A receptor antagonists

Katritch, V., Jaakola, V-P., Lane, J., Lin, J., IJzerman, A. P., Yeager, M., Kufareva, I., Stevens, R. & Abagyan, R., 2010, In : Journal of Medicinal Chemistry. 53, 4, p. 1799 - 1809 11 p.

Research output: Contribution to journalArticleResearchpeer-review

198 Citations (Scopus)

Sub-picomolar relaxin signalling by a pre-assembled RXFP1, AKAP79, AC2, beta-arrestin 2, PDE4D3 complex

Halls, M. & Cooper, D., 2010, In : The EMBO Journal. 29, 16, p. 2772 - 2787 16 p.

Research output: Contribution to journalArticleResearchpeer-review

52 Citations (Scopus)

The Emergence of Allosteric Modulators for G Protein-Coupled Receptors

Gregory, K. J., Valant, C., Simms, J., Sexton, P. M. & Christopoulos, A., 15 Jul 2010, GPCR Molecular Pharmacology and Drug Targeting: Shifting Paradigms and New Directions. John Wiley & Sons, p. 61-87 27 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

4 Citations (Scopus)

The endocannabinoid 2-arachidonylglycerol is a negative allosteric modulator of the human A3 adenosine receptor

Lane, J., Beukers, M., Mulder-Krieger, T. & IJzerman, A. P., 2010, In : Biochemical Pharmacology. 79, 1, p. 48 - 56 9 p.

Research output: Contribution to journalArticleResearchpeer-review

29 Citations (Scopus)

Tissue functions mediated by beta3-adrenoceptors-Findings and challenges

Michel, M., Ochodnicky, P. & Summers, R., 2010, In : Naunyn-Schmiedeberg's Archives of Pharmacology. 382, 2, p. 103 - 108 6 p.

Research output: Contribution to journalArticleResearchpeer-review

27 Citations (Scopus)

Trafficking and signaling of G protein-coupled receptors in the nervous system: implications for disease and therapy

Bunnett, N. & Cottrell, G., 2010, In : CNS and Neurological Disorders - Drug Targets. 9, 5, p. 539 - 556 18 p.

Research output: Contribution to journalArticleResearchpeer-review

13 Citations (Scopus)

Transient receptor potential ankyrin-1 has a major role in mediating visceral pain in mice

Cattaruzza, F., Spreadbury, I., Miranda-Morales, M., Grady, E., Vanner, S. & Bunnett, N., 2010, In : American Journal of Physiology - Gastrointestinal and Liver Physiology. 298, p. 81 - 91 11 p.

Research output: Contribution to journalArticleResearchpeer-review

91 Citations (Scopus)

Transient receptor potential ion channels V4 and A1 contribute to pancreatitis pain in mice

Ceppa, E., Cattaruzza, F., Lyo, V., Amadesi, S., Pelayo, J-C., Poole, D., Vaksman, N., Liedtke, W., Cohen, D., Grady, E., Bunnett, N. & Kirkwood, K., 2010, In : American Journal of Physiology - Gastrointestinal and Liver Physiology. 299, p. 556 - 571 16 p.

Research output: Contribution to journalArticleResearchpeer-review

64 Citations (Scopus)

Understanding amylin Receptors

Just, R., Simms, J., Furness, S. G. B., Christopoulos, A. & Sexton, P. M., 2010, The Calcitonin Gene-related Peptide Family: Form, Function and Future Perspectives. Springer, p. 41-57 17 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

2 Citations (Scopus)
2009

B-type natriuretic peptide: Endogenous regulator of myocardial structure, biomarker and therapeutic target

Ritchie, R. H., Rosenkranz, A. C. & Kaye, D. M., 1 Sep 2009, In : Current Molecular Medicine. 9, 7, p. 814-825 12 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

26 Citations (Scopus)

Cannabinoid receptor type 1 protects against age- related osteoporosis by regulating osteoblast and adipocyte differentiation in marrow stromal cells

Idris, A., Sophocleous, A., Landao-Bassonga, E., Canals, M., Milligan, G., Baker, D., Hof, R. & Ralston, S., 2009, In : Cell Metabolism. 10, 2, p. 139 - 147 9 p.

Research output: Contribution to journalArticleResearchpeer-review

107 Citations (Scopus)

Cell surface delivery and structural re-organization by pharmacological chaperones of an oligomerization-defective alpha1b-adrenoceptor mutant demonstrates membrane targeting of GPCR oligomers

Canals, M., Lopez-Gimenez, J. & Milligan, G., 2009, In : Biochemical Journal. 417, 1, p. 161 - 172 12 p.

Research output: Contribution to journalArticleResearchpeer-review

31 Citations (Scopus)

Current and emerging trends in cell-based assays

Jordan, R., Bielefield-Sevigny, M., Christopoulos, A., Eglen, R. M., Mark, D. F., Pfleger, K., Valler, M. J. & Zaman, G. J. R., Dec 2009, In : Drug Discovery World. 11, 1, p. 66-78 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Effect of the calcimimetic R-568 [3-(2-chlorophenyl)-N-((1R)-1-(3- methoxyphenyl)ethyl)-1-propanamine] on correcting inactivating mutations in the human calcium-sensing receptor

Lu, J. Y. L., Yang, Y., Gnacadja, G., Christopoulos, A. & Reagan, J. D., 2009, In : Journal of Pharmacology and Experimental Therapeutics. 331, 3, p. 775 - 786 12 p.

Research output: Contribution to journalArticleResearchpeer-review

34 Citations (Scopus)

Endosomal deubiquitinating enzymes control ubiquitination and down-regulation of protease-activated receptor 2

Hasdemir, B., Murphy, J., Cottrell, G. & Bunnett, N., 2009, In : The Journal of Biological Chemistry. 284, 41, p. 28453 - 28466 14 p.

Research output: Contribution to journalArticleResearchpeer-review

67 Citations (Scopus)

Endosomal endothelin-converting enzyme-1: A regulator of beta-arrestin-dependent ERK signaling

Cottrell, G., Padilla, B., Amadesi, S., Poole, D., Murphy, J., Hardt, M., Roosterman, D., Steinhoff, M. & Bunnett, N., 2009, In : The Journal of Biological Chemistry. 284, 33, p. 22411 - 22425 15 p.

Research output: Contribution to journalArticleResearchpeer-review

50 Citations (Scopus)

Endosomes: A legitimate platform for the signaling train

Murphy, J., Padilla, B., Hasdemir, B., Cottrell, G. & Bunnett, N., 2009, In : Proceedings of the National Academy of Sciences of the United States of America. 106, 42, p. 17615 - 17622 8 p.

Research output: Contribution to journalArticleResearchpeer-review

243 Citations (Scopus)

Endothelin-converting enzyme 1 promotes re-sensitization of neurokinin 1 receptor-dependent neurogenic inflammation

Cattaruzza, F., Cottrell, G., Vaksman, N. & Bunnett, N., 2009, In : British Journal of Pharmacology. 156, 5, p. 730 - 739 10 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

Molecular basis of association of receptor activity-modifying protein 3 with the family B G protein-coupled secretin receptor

Harikumar, K. G., Simms, J., Christopoulos, G., Sexton, P. M. & Miller, L. J., 15 Dec 2009, In : Biochemistry. 48, 49, p. 11773-11785 13 p.

Research output: Contribution to journalArticleResearchpeer-review

39 Citations (Scopus)

Orthosteric/allosteric bitopic ligands going hybrid with GPCRs

Valant, C., Sexton, P. M. & Christopoulos, A., 1 Jun 2009, In : Molecular Interventions. 9, 3, p. 125-135 11 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

69 Citations (Scopus)

Protein kinase D isoforms are expressed in rat and mouse primary sensory neurons and are activated by agonists of protease-activated receptor 2

Amadesi, S., Grant, A., Cottrell, G., Vaksman, N., Poole, D., Rozengurt, E. & Bunnett, N., 2009, In : The Journal of Comparative Neurology. 516, 2, p. 141 - 156 16 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

Relaxin family peptides and receptors in mammalian brain

Ma, S., 2009, Annals of the New York Academy of Sciences.

Research output: Chapter in Book/Report/Conference proceedingConference PaperOtherpeer-review

Structure and activity in the relaxin family of peptides

Ma, S., 2009, Annals of the New York Academy of Sciences.

Research output: Chapter in Book/Report/Conference proceedingConference PaperOtherpeer-review

The pleiotropy of dioxin toxicity - Xenobiotic misappropriation of the aryl hydrocarbon receptor's alternative physiological roles

Furness, S. & Whelan, F., 2009, In : Pharmacology and Therapeutics. 124, 3, p. 336 - 353 18 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
49 Citations (Scopus)
2008

Antibodies that identify only the active conformation of Gi family G protein alpha subunits

Lane, J., Henderson, D., Powney, B., Wise, A., Rees, S., Daniels, D., Plumpton, C., Kinghorn, I. & Milligan, G., 2008, In : The FASEB Journal. 22, 6, p. 1924 - 1932 9 p.

Research output: Contribution to journalArticleResearchpeer-review

13 Citations (Scopus)

Attenuated disruption of prepulse inhibition by dopaminergic stimulation after maternal deprivation and adolescent corticosterone treatment in rats

Choy, K. H. C. & van den Buuse, M., 1 Jan 2008, In : European Neuropsychopharmacology. 18, 1, p. 1-13 13 p.

Research output: Contribution to journalArticleResearchpeer-review

33 Citations (Scopus)

Calcitonin receptor-like receptor (CLR), receptor activity-modifying protein 1 (RAMP1), and calcitonin gene-related peptide (CGRP) immunoreactivity in the rat trigeminovascular system:Differences between peripheral and central CGRP receptor distribut

Lennerz, J., Ruhle, V., Ceppa, E., Neuhuber, W., Bunnett, N., Grady, E. & Messlinger, K., 2008, In : The Journal of Comparative Neurology. 507, 3, p. 1277 - 1299 23 p.

Research output: Contribution to journalArticleResearchpeer-review

208 Citations (Scopus)