1986 …2023

Research output per year

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Research Output

Distinct receptor activity-modifying protein domains differentially modulate interaction with calcitonin receptors

Udawela, M., Christopoulos, G., Tilakaratne, N., Christopoulos, A., Albiston, A. L. & Sexton, P. M., 2006, In : Molecular Pharmacology. 69, 6, p. 1984 - 1989 6 p.

Research output: Contribution to journalArticleResearchpeer-review

43 Citations (Scopus)

Divergent effects of strontium and calcium-sensing receptor positive allosteric modulators (calcimimetics) on human osteoclast activity

Diepenhorst, N. A., Leach, K., Keller, A. N., Rueda, P., Cook, A. E., Pierce, T. L., Nowell, C., Pastoureau, P., Sabatini, M., Summers, R. J., Charman, W. N., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Nov 2018, In : British Journal of Pharmacology. 175, 21, p. 4095-4108 14 p.

Research output: Contribution to journalArticleResearchpeer-review

5 Citations (Scopus)

Divergent structural requirements exist for calcitonin receptor binding specificity and adenylate cyclase activation

Houssami, S., Findlay, D. M., Brady, C. L., Martin, T. J., Epand, R. M., Moore, E. E., Murayama, E., Tamura, T., Orlowski, R. C. & Sexton, P. M., 1 Jan 1995, In : Molecular Pharmacology. 47, 4, p. 798-809 12 p.

Research output: Contribution to journalArticleResearchpeer-review

47 Citations (Scopus)

Dominant Negative G Proteins Enhance Formation and Purification of Agonist-GPCR-G Protein Complexes for Structure Determination

Liang, Y-L., Zhao, P., Draper-Joyce, C. J., Baltos, J-A., Glukhova, A., Truong, T. T., May, L. T., Christopoulos, A., Wootten, D., Sexton, P. & Furness, S., 2018, In : ACS Pharmacology and Translational Sciences. 1, 1, p. 12-20 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H3 receptor antagonists

Riddy, D. M., Cook, A. E., Shackleford, D. M., Pierce, T. L., Mocaer, E., Mannoury la Cour, C., Sors, A., Charman, W. N., Summers, R. J., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Jan 2019, In : Neuropharmacology. 144, p. 244-255 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
6 Citations (Scopus)

Effective GPCR screening using ERK 1/2: applying SureFire to detect ERK 1/2 phosphorylation

Osmond, R. W., Dyer, A. R., Sexton, P. M., Christopoulos, A. & Crouch, M. F., 2006, In : Genetic Engineering News. 26, 1, p. 27 - 28 2 p.

Research output: Contribution to journalArticleResearchpeer-review

Effects of conformational restriction of 2-amino-3-benzoylthiophenes on A1 adenosine receptor modulation

Aurelio, L., Valant, C., Flynn, B., Sexton, P., White, J., Christopoulos, A. & Scammells, P., 2010, In : Journal of Medicinal Chemistry. 53, p. 6550 - 6559 10 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

Effects of urea pretreatment on the binding properties of adenosine A 1 receptors

May, L. T., Sexton, P. M. & Christopoulos, A., 2005, In : British Journal of Pharmacology. 146, 8, p. 1119 - 1129 11 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

Electrophoretic mobility and glycosylation characteristics of heterogeneously expressed calcitonin receptors

Quiza, M., Dowton, M., Perry, K. J. & Sexton, P. M., 1 Jan 1997, In : Endocrinology. 138, 2, p. 530-539 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
16 Citations (Scopus)

Emerging paradigms in GPCR allostery: implications for drug discovery

Wootten, D. L., Christopoulos, A. & Sexton, P., 2013, In : Nature Reviews Drug Discovery. 12, 8, p. 630 - 644 15 p.

Research output: Contribution to journalArticleResearchpeer-review

242 Citations (Scopus)

Endogenous allosteric modulators of G protein-coupled receptors

Van Der Westhuizen, E. T., Valant, C., Sexton, P. & Christopoulos, A., 2015, In : Journal of Pharmacology and Experimental Therapeutics. 353, 2, p. 246 - 260 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
64 Citations (Scopus)

Engendering biased signalling from the calcium-sensing receptor for the pharmacotherapy of diverse disorders

Leach, K., Sexton, P., Christopoulos, A. & Conigrave, A., 2014, In : British Journal of Pharmacology. 171, 5, p. 1142 - 1155 14 p.

Research output: Contribution to journalArticleResearchpeer-review

27 Citations (Scopus)

Erratum: Differential activation and modulation of the glucagon-like peptide-1 receptor by small molecular ligands (Molecular Pharmacology (2013) 83 (822-834))

Wootten, D., Savage, E. E., Willard, F. S., Bueno, A. B., Sloop, K. W., Christopoulos, A. & Sexton, P. M., Jul 2013, In : Molecular Pharmacology. 84, 1, p. 170 1 p.

Research output: Contribution to journalComment / DebateOtherpeer-review

Evidence for a new subclass of calcitonin/ calcitonin gene-related peptide binding site in rat brain

Sexton, P. M., McKenzie, J. S. & Mendelsohn, F. A. O., 1 Jan 1988, In : Neurochemistry International. 12, 3, p. 323-335 13 p.

Research output: Contribution to journalArticleResearchpeer-review

83 Citations (Scopus)

Expression and activity of the calcitonin receptor family in a sample of primary human high-grade gliomas

Ostrovskaya, A., Hick, C., Hutchinson, D. S., Stringer, B. W., Wookey, P. J., Wootten, D., Sexton, P. M. & Furness, S. G. B., 18 Feb 2019, In : BMC Cancer. 19, 1, 12 p., 157.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
1 Citation (Scopus)

Extracellular loop 2 of the adenosine A1 receptor has a key role in orthosteric ligand affinity and agonist efficacy

Nguyen, A. T. N., Baltos, J-A., Thomas, T., Nguyen, T. D., Lopez Munoz, L., Gregory, K. J., White, P. J., Sexton, P. M., Christopoulos, A. & May, L. T., 1 Dec 2016, In : Molecular Pharmacology. 90, 6, p. 703-714 12 p.

Research output: Contribution to journalArticleResearchpeer-review

30 Citations (Scopus)

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
File
11 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

43 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

801 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
23 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

72 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 of the United States of America. 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

6 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

199 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 drug targets

Sexton, P. M. & Christopoulos, A., 2006, In : Current Pharmaceutical Design. 12, 14, p. 1681 - 1682 2 p.

Research output: Contribution to journalLetterOther

1 Citation (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

274 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)

G protein–coupled receptors targeting insulin resistance, obesity, and type 2 diabetes mellitus

Riddy, D. M., Delerive, P., Summers, R. J., Sexton, P. & Langmead, C. J., 1 Jan 2018, In : Pharmacological Reviews. 70, 1, p. 39-67 29 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

24 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)

Homology Modeling of GPCRs

Simms, J. W., Hall, N. E., Lam, P. HC., Christopoulos, A., Abagyan, R. & Sexton, P., 2009, Methods in Molecular Biology - G Protein-Coupled Receptors in Drug Delivery. Leifert, W. R. (ed.). 552 ed. USA: Humana Press, p. 97 - 113 17 p.

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

11 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

132 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

47 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

48 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

122 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
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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 & Metabolism. 16, 1, p. 26 - 33 8 p.

Research output: Contribution to journalArticleResearchpeer-review

77 Citations (Scopus)