1986 …2023

Research output per year

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Research Output

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Article

Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy

Dal Maso, E., Zhu, Y., Pham, V., Reynolds, C. A., Deganutti, G., Hick, C. A., Yang, D., Christopoulos, A., Hay, D. L., Wang, M. W., Sexton, P. M., Furness, S. G. B. & Wootten, D., 1 Apr 2018, In : Biochemical Pharmacology. 150, p. 214-244 31 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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10 Citations (Scopus)

Fluorescence resonance energy transfer analysis of secretin docking to its receptor: Mapping distances between residues distributed throughout the ligand pharmacophore and distinct receptor residues

Harikumar, K. G., Lam, P. C-H., Dong, M., Sexton, P., Abagyan, R. & Miller, L. J., 2007, In : Journal of Biological Chemistry. 282, 45, p. 32834 - 32843 10 p.

Research output: Contribution to journalArticleResearchpeer-review

25 Citations (Scopus)

Functional importance of a structurally distinct homodimeric complex of the family B G protein-coupled secretin receptor

Gao, F., Harikumar, K. G., Dong, M., Lam, P. C-H., Sexton, P. M., Christopoulos, A., Bordner, A., Abagyan, R. & Miller, L. J., 2009, In : Molecular Pharmacology. 76, 2, p. 264 - 274 11 p.

Research output: Contribution to journalArticleResearchpeer-review

42 Citations (Scopus)

Functionally different isoforms of the human calcitonin receptor result from alternative splicing of the gene transcript

Moore, E. E., Kuestner, R. E., Stroop, S. D., Grant, F. J., Matthewes, S. L., Brady, C. L., Sexton, P. M. & Findlay, D. M., 1 Aug 1995, In : Molecular Endocrinology. 9, 8, p. 959-968 10 p.

Research output: Contribution to journalArticleResearchpeer-review

94 Citations (Scopus)

Functional selectivity and classical concepts of quantitative pharmacology

Urban, J. D., Clarke, W. P., von Zastrow, M., Nichols, D. E., Kobilka, B., Weinstein, H., Javitch, J. A., Roth, B. L., Christopoulos, A., Sexton, P. M., Miller, K. J., Spedding, M. & Mailman, R. B., 2007, In : Journal of Pharmacology and Experimental Therapeutics. 320, 1, p. 1 - 13 13 p.

Research output: Contribution to journalArticleResearchpeer-review

796 Citations (Scopus)

Function of the rat calcitonin receptors, C1a and C1b, expressed in Xenopus oocytes

Matsumoto, M., Kaibara, M., Uezono, Y., Izumi, F., Sumikawa, K., Sexton, P. M. & Taniyama, K., 26 Jan 1998, In : Biochemical and Biophysical Research Communications. 242, 3, p. 484-491 8 p.

Research output: Contribution to journalArticleResearchpeer-review

7 Citations (Scopus)

Genetically encoded photocross-linkers determine the biological binding site of exendin-4 peptide in the N-terminal domain of the intact human glucagon-like peptide-1 receptor (GLP-1R)

Koole, C., Reynolds, C. A., Mobarec, J. C., Hick, C., Sexton, P. M. & Sakmar, T. P., 28 Apr 2017, In : Journal of Biological Chemistry. 292, 17, p. 7131-7144 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
22 Citations (Scopus)

Glucagon-like peptide-1 and its class B G protein-coupled receptors: a long march to therapeutic successes

de Graaf, C., Donnelly, D., Wootten, D., Lau, J., Sexton, P. M., Miller, L. J., Ahn, J-M., Liao, J., Fletcher, M. M., Yang, D., Brown, A. J. H., Zhou, C., Deng, J. & Wang, M-W., 1 Oct 2016, In : Pharmacological Reviews. 68, 4, p. 954-1013 60 p.

Research output: Contribution to journalArticleResearchpeer-review

65 Citations (Scopus)

Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery

Harikumar, K. G., Wootten, D. L., Pinon, D. I., Koole, C. R., Ball, A. M., Furness, S. GB., Graham, B., Dong, M., Christopoulos, A., Miller, L. J. & Sexton, P. M., 2012, In : Proceedings of the National Academy of Sciences. 109, 45, p. 18607 - 18612 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
41 Citations (Scopus)

Glucagon-like peptide-1 receptor internalisation controls spatiotemporal signalling mediated by biased agonists

Fletcher, M. M., Halls, M. L., Zhao, P., Clydesdale, L., Christopoulos, A., Sexton, P. M. & Wootten, D., 1 Oct 2018, In : Biochemical Pharmacology. 156, p. 406-419 14 p.

Research output: Contribution to journalArticleResearchpeer-review

5 Citations (Scopus)

GPCR modulation by RAMPs

Hay, D. L., Poyner, D. R. & Sexton, P. M., 2006, In : Pharmacology and Therapeutics. 109, 1-2, p. 173 - 197 25 p.

Research output: Contribution to journalArticleResearchpeer-review

197 Citations (Scopus)

GPCR structure, function, drug discovery and crystallography: report from Academia-Industry International Conference (UK Royal Society) Chicheley Hall, 1-2 September 2014

Heifetz, A., Schertler, G. F. X., Seifert, R., Tate, C. G., Sexton, P. M., Gurevich, V. V., Fourmy, D., Cherezov, V., Marshall, F., Storer, R. I., Moraes, I., Tikhonova, I., Tautermann, C., Hunt, P., Ceska, T., Hodgson, S., Bodkin, M., Singh, S., Law, R. & Biggin, P., 22 Aug 2015, In : Naunyn-Schmiedeberg's Archives of Pharmacology. 388, 8, p. 883-903 21 p., 1111.

Research output: Contribution to journalArticleOther

Open Access
24 Citations (Scopus)

G-protein-coupled receptor allosterism: the promise and the problem(s)

Christopoulos, A., May, L. T., Avlani, V. A. & Sexton, P. M., 2004, In : Biochemical Society Transactions. 32, Pt 5, p. 873 - 877 5 p.

Research output: Contribution to journalArticleOther

41 Citations (Scopus)

G-protein-coupled receptor Mas is a physiological antagonist of the angiotensin II type 1 receptor

Kostenis, E., Milligan, G., Christopoulos, A., Sanchez-Ferrer, C. F., Heringer-Walther, S., Sexton, P. M., Gembardt, F., Kellett, E., Martini, L., Vanderheyden, P., Schultheiss, H-P. & Walther, T., 2005, In : Circulation. 111, p. 1806 - 1813 8 p.

Research output: Contribution to journalArticleResearchpeer-review

273 Citations (Scopus)

G-Protein-coupled receptor-protein interactions: basis for new concepts on receptor structure and function

Tilakaratne, N. & Sexton, P. M., 2005, In : Clinical and Experimental Pharmacology and Physiology. 32, 11, p. 979 - 987 9 p.

Research output: Contribution to journalArticleResearchpeer-review

29 Citations (Scopus)

H2 relaxin is a biased ligand relative to H3 relaxin at the relaxin family peptide receptor 3 (RXFP3) [S]

van der Westhuizen, E. T., Christopoulos, A., Sexton, P., Wade, J. & Summers, R., 2010, In : Molecular Pharmacology. 77, 5, p. 759 - 772 14 p.

Research output: Contribution to journalArticleResearchpeer-review

23 Citations (Scopus)

Hematological defects in the oc/oc mouse, a model of infantile malignant osteopetrosis

Blin-Wakkach, C., Blin-Wakkach, A., Sexton, P., Rochet, N. & Carle, G. F., 2004, In : Leukemia. 18, 9, p. 1505 - 1511 7 p.

Research output: Contribution to journalArticleResearchpeer-review

44 Citations (Scopus)

Heterogeneity in ligand recognition of calcitonin receptors

Houssami, S., Findlay, D. M., Hilton, J. M., O'Keeffe, L. M., Martin, T. J. & Sexton, P. M., 1 Jan 1994, In : Endocrine. 2, 2, p. 127-134 8 p.

Research output: Contribution to journalArticleResearchpeer-review

15 Citations (Scopus)

Heterogeneity of the calcitonin receptor: Functional aspects in osteoclasts and other sites

Martin, T. J., Findlay, D. M., Houssami, S., Ikegame, M., Rakopoulos, M., Moseley, J. M. & Sexton, P. M., 1 Jan 1995, In : Journal of Nutrition. 125, 7 SUPPL., p. 2009S-2014S

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

High throughput, quantitative analysis of human osteoclast differentiation and activity

Diepenhorst, N., Nowell, C., Rueda, P., Henriksen, K., Pierce, T., Cook, A., Pastoureau, P., Sabatini, M., Charman, W., Christopoulos, A., Summers, R., Sexton, P. & Langmead, C., 15 Feb 2017, In : Analytical Biochemistry. 519, p. 51-56 6 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Homologous regulation of the rat C1a calcitonin receptor (CTR) in nonosteoclastic cells is independent of CTR messenger ribonucleic acid changes and cyclic adenosine 3',5'-monophosphate-dependent protein kinase activation

Findlay, D. M., Houssami, S., Christopoulos, G. & Sexton, P. M., 1 Jan 1996, In : Endocrinology. 137, 11, p. 4576-4585 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
10 Citations (Scopus)

Identification of brain isoforms of the rat calcitonin receptor

Sexton, P. M., Houssami, S., Hilton, J. M., O'Keeffe, L. M., Center, R. J., Gillespie, M. T., Darcy, P. & Findlay, D. M., 1 Jan 1993, In : Molecular Endocrinology. 7, 6, p. 815-821 7 p.

Research output: Contribution to journalArticleResearchpeer-review

131 Citations (Scopus)

Identification of key components in the irreversibility of salmon calcitonin binding to calcitonin receptors

Hilton, J. M., Dowton, M., Houssami, S. & Sexton, P. M., 1 Jan 2000, In : Journal of Endocrinology. 166, 1, p. 213-226 14 p.

Research output: Contribution to journalArticleResearchpeer-review

45 Citations (Scopus)

Identification of molecular phenotypes and biased signaling induced by naturally occurring mutations of the human calcium-sensing receptor

Leach, K., Wen, C., Davey, A. E., Sexton, P. M., Conigrave, A. D. & Christopoulos, A., 2012, In : Endocrinology. 153, 9, p. 4304 - 4316 13 p.

Research output: Contribution to journalArticleResearchpeer-review

47 Citations (Scopus)

Identification of N-terminal receptor activity-modifying protein residues important for calcitonin gene-related peptide, adrenomedullin, and amylin receptor function

Qi, T., Christopoulos, G., Bailey, R. J., Christopoulos, A., Sexton, P. & Hay, D. L., 2008, In : Molecular Pharmacology. 74, 4, p. 1059 - 1071 13 p.

Research output: Contribution to journalArticleResearchpeer-review

53 Citations (Scopus)

Identification of orthosteric and allosteric site mutations in M 2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias

Gregory, K. J., Hall, N., Tobin, A., Sexton, P. & Christopoulos, A., 2010, In : Journal of Biological Chemistry. 285, 10, p. 7459 - 7474 16 p.

Research output: Contribution to journalArticleResearchpeer-review

121 Citations (Scopus)

Impact of clinically relevant mutations on the pharmacoregulation and signaling bias of the calcium-sensing receptor by positive and negative allosteric modulators

Leach, K., Wen, C., Cook, A. E., Sexton, P., Conigrave, A. & Christopoulos, A., 2013, In : Endocrinology. 154, 3, p. 1105 - 1116 12 p.

Research output: Contribution to journalArticleResearchpeer-review

52 Citations (Scopus)

Impact of species variability and "probe-dependence" on the detection and in vivo validation of allosteric modulation at the M(4) muscarinic acetylcholine receptor

Suratman, N. S., Leach, K., Sexton, P., Felder, C. C., Loiacono, R. & Christopoulos, A., 2011, In : British Journal of Pharmacology. 162, 7, p. 1659 - 1670 12 p.

Research output: Contribution to journalArticleResearchpeer-review

44 Citations (Scopus)

Importance of lipid-exposed residues in transmembrane segment four for family B calcitonin receptor homo-dimerization

Harikumar, K. G., Ball, A. M., Sexton, P. & Miller, L. J., 2010, In : Regulatory Peptides. 164, 2-3, p. 113 - 119 7 p.

Research output: Contribution to journalArticleResearchpeer-review

22 Citations (Scopus)

Improving virtual screening of G protein-coupled receptors via ligand-directed modeling

Coudrat, T., Simms, J., Christopoulos, A., Wootten, D. & Sexton, P. M., 1 Nov 2017, In : PLoS Computational Biology. 13, 11, 40 p., e1005819.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
5 Citations (Scopus)

'Ins and outs' of seven-transmembrane receptor signalling to ERK

Werry, T. D., Sexton, P. M. & Christopoulos, A., 2005, In : Trends in Endocrinology and Metabolism. 16, 1, p. 26 - 33 8 p.

Research output: Contribution to journalArticleResearchpeer-review

77 Citations (Scopus)

Insights into interactions between the alpha-helical region of the salmon calcitonin antagonists and the human calcitonin receptor using photoaffinity labeling

Pham, V., Dong, M., Wade, J. D., Miller, L. J., Morton, C. J., Ng, H., Parker, M. W. & Sexton, P. M., 2005, In : Journal of Biological Chemistry. 280, 31, p. 28610 - 28622 13 p.

Research output: Contribution to journalArticleResearchpeer-review

25 Citations (Scopus)

Interaction studies of multiple binding sites on M4 muscarinic acetylcholine receptors

Lanzafame, A. A., Sexton, P. M. & Christopoulos, A., 2006, In : Molecular Pharmacology. 70, 2, p. 736 - 746 11 p.

Research output: Contribution to journalArticleResearchpeer-review

25 Citations (Scopus)

International union of basic and clinical pharmacology. XC. Multisite pharmacology: Recommendations for the nomenclature of receptor allosterism and allosteric ligands

Christopoulos, A., Changeux, J-P., Catterall, W. A., Fabbro, D., Burris, T. P., Cidlowski, J. A., Olsen, R. W., Peters, J. A., Neubig, R., Pin, J. P., Sexton, P., Kenakin, T. P., Ehlert, F. J., Spedding, M. & Langmead, C. J., 2014, In : Pharmacological Reviews. 66, 4, p. 918 - 947 30 p.

Research output: Contribution to journalArticleResearchpeer-review

116 Citations (Scopus)

International Union of Pharmacology. XXXII. The mammalian calcitonin gene-related peptides, adrenomedullin, amylin, and calcitonin receptors

Poyner, D. R., Sexton, P. M., Marshall, I., Smith, D. M., Quirion, R., Born, W., Muff, R., Fischer, J. A. & Foord, S. M., 2002, In : Pharmacological Reviews. 54, 2, p. 233 - 246 14 p.

Research output: Contribution to journalArticleResearchpeer-review

594 Citations (Scopus)

In vitro autoradiographic localization of amylin binding sites in rat brain

Sexton, P. M., Paxinos, G., Kenney, M. A., Wookey, P. J. & Beaumont, K., 1 Jan 1994, In : Neuroscience. 62, 2, p. 553-567 15 p.

Research output: Contribution to journalArticleResearchpeer-review

212 Citations (Scopus)

In vitro autoradiographic localization of ANP receptors in rat kidney and adrenal gland

Chai, S. Y., Sexton, P. M., Allen, A. M., Figdor, R. & Mendelsohn, F. A., 26 Nov 1986, In : American Journal of Physiology - Renal Fluid and Electrolyte Physiology. 250, 4

Research output: Contribution to journalArticleResearchpeer-review

63 Citations (Scopus)

In vitro autoradiographic localization of calcitonin and amylin binding sites in monkey brain

Paxinos, G., Chai, S. Y., Christopoulos, G., Huang, X-F., Toga, A. W., Wang, H. Q. & Sexton, P. M., 2004, In : Journal of Chemical Neuroanatomy. 27, 4, p. 217 - 236 20 p.

Research output: Contribution to journalArticleResearchpeer-review

42 Citations (Scopus)

In vitro autoradiographic localization of calcitonin binding sites in human medulla oblongata

Sexton, P. M., Paxinos, G., Huang, XF. F. & Mendelsohn, F. A. O., 1 Jan 1994, In : Journal of Comparative Neurology. 341, 4, p. 449-463 15 p.

Research output: Contribution to journalArticleResearchpeer-review

13 Citations (Scopus)

In vitro autoradiographic localization of the calcitonin receptor isoforms, C1a and C1b, in rat brain

Hilton, J. M., Chai, S. Y. & Sexton, P. M., 1 Jan 1995, In : Neuroscience. 69, 4, p. 1223-1237 15 p.

Research output: Contribution to journalArticleResearchpeer-review

43 Citations (Scopus)

Involvement of the sigma1 (sigma1) receptor in the anti-amnesic, but not antidepressant-like, effects of the aminotetrahydrofuran derivative ANAVEX1-41

Espallergues, J., Lapalud, P., Christopoulos, A., Avlani, V. A., Sexton, P., Vamvakides, A. & Maurice, T., 2007, In : British Journal of Pharmacology. 152, 2, p. 267 - 279 13 p.

Research output: Contribution to journalArticleResearchpeer-review

21 Citations (Scopus)

Isoforms of the rat calcitonin receptor: Consequences for ligand binding and signal transduction

Houssami, S., Findlay, D. M., Brady, C. L., Myers, D. L., Martin, T. J. & Sexton, P. M., 1 Jan 1994, In : Endocrinology. 135, 1, p. 183-190 8 p.

Research output: Contribution to journalArticleResearchpeer-review

86 Citations (Scopus)

Isoform-specific biased agonism of histamine H3 receptor agonists

Riddy, D. M., Cook, A. E., Diepenhorst, N. A., Bosnyak, S., Brady, R., La Cour, C. M., Mocaer, E., Summers, R. J., Charman, W. N., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Feb 2017, In : Molecular Pharmacology. 91, 2, p. 87-99 13 p.

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)
19 Citations (Scopus)

Ligand-dependent modulation of G protein conformation alters drug efficacy

Furness, S. G. B., Liang, Y-L., Nowell, C. J., Halls, M. L., Wookey, P. J., Dal Maso, E., Inoue, A., Christopoulos, A., Wootten, D. & Sexton, P. M., 20 Oct 2016, In : Cell. 167, 3, p. 739-749 11 p.

Research output: Contribution to journalArticleResearchpeer-review

51 Citations (Scopus)

Lipopolysaccharide supports survival and fusion of preosteoclasts independent of TNF-, IL-1 and RANKL

Suda, K., Woo, J-T., Takami, M., Sexton, P. M. & Nagai, K., 2002, In : Journal of Cellular Physiology. 190, p. 101 - 108 8 p.

Research output: Contribution to journalArticleResearchpeer-review

91 Citations (Scopus)

Localization and characterizarion of renal calcitonin receptors by in vitro autoradiography

Sexton, P. M., Adam, W. R., Moseley, J. M., Martin, T. J. & Mendelsohn, F. A. O., 1 Jan 1987, In : Kidney International. 32, 6, p. 862-868 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
44 Citations (Scopus)

Localization and Regulation of Renal Receptors for Angiotensin II and Atrial Natriuretic Peptide

Sexton, P. M., Zhuo, J. & Mendelsohn, F. A. O., 1 Jan 1992, In : Tohoku Journal of Experimental Medicine. 166, 1, p. 41-56 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
9 Citations (Scopus)

Localization of binding sites for calcitonin gene-related peptide in rat brain by in vitro autoradiography

Sexton, P. M., McKenzie, J. S., Mason, R. T., moseley, J. M., Martin, T. J. & Mendelsohn, F. A. O., 1 Jan 1986, In : Neuroscience. 19, 4, p. 1235-1245 11 p.

Research output: Contribution to journalArticleResearchpeer-review

98 Citations (Scopus)