1986 …2023

Research output per year

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Research Output

Murine GPRC6A mediates cellular responses to L-amino acids, but not osteocalcin variants

Rueda, P., Harley, E., Lu, Y., Stewart, G. D., Fabb, S., Diepenhorst, N., Cremers, B., Rouillon, M-H., Wehrle, I., Geant, A., Lamarche, G., Leach, K., Charman, W. N., Christopoulos, A., Summers, R. J., Sexton, P. M. & Langmead, C. J., 1 Jan 2016, In : PLoS ONE. 11, 1, p. 1-19 19 p., e0146846.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
24 Citations (Scopus)

Muscarinic acetylcholine receptors: Novel opportunities for drug development

Kruse, A. C., Kobilka, B., Gautam, D., Sexton, P. M., Christopoulos, A. & Wess, J., 2014, In : Nature Reviews Drug Discovery. 13, 7, p. 549 - 560 12 p.

Research output: Contribution to journalArticleResearchpeer-review

173 Citations (Scopus)

Muscarinic M5 receptors modulate ethanol seeking in rats

Berizzi, A. E., Perry, C. J., Shackleford, D. M., Lindsley, C. W., Jones, C. K., Chen, N. A., Sexton, P. M., Christopoulos, A., Langmead, C. J. & Lawrence, A. J., 1 Jun 2018, In : Neuropsychopharmacology. 43, 7, p. 1510-1517 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
12 Citations (Scopus)

New insights into the function of M4 muscarinic acetylcholine receptors gained using a novel allosteric modulator and a DREADD (designer receptor exclusively activated by a designer drug)

Nawaratne, O. V., Leach, K., Suratman, S., Loiacono, R., Felder, C. C., Armbruster, B. N., Roth, B. L., Sexton, P. & Christopoulos, A., 2008, In : Molecular Pharmacology. 74, 4, p. 1119 - 1131 13 p.

Research output: Contribution to journalArticleResearchpeer-review

87 Citations (Scopus)

Novel allosteric modulators of G protein-coupled receptors

Gentry, P. R., Sexton, P. M. & Christopoulos, A., 2015, In : Journal of Biological Chemistry. 290, 32, p. 19478-19488 11 p.

Research output: Contribution to journalArticleResearchpeer-review

93 Citations (Scopus)

Novel irreversible agonists acting at the A1 adenosine receptor

Jorg, M., Glukhova, A., Abdul Ridha, A., Vecchio, E. A., Nguyen, A., Sexton, P., White, P., May, L., Christopoulos, A. & Scammells, P., 22 Dec 2016, In : Journal of Medicinal Chemistry. 59, 24, p. 11182-11194 13 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)

Novel receptor partners and function of receptor activity-modifying proteins

Christopoulos, A., Christopoulos, G., Morfis, M., Udawela, M., Laburthe, M., Couvineau, A., Kuwasako, K., Tilakaratne, N. & Sexton, P. M., 2003, In : Journal of Biological Chemistry. 278, 5, p. 3293 - 3297 5 p.

Research output: Contribution to journalArticleResearchpeer-review

224 Citations (Scopus)

O-GlcNAc Engineering of GPCR Peptide-Agonists Improves Their Stability and in Vivo Activity

Levine, P. M., Balana, A. T., Sturchler, E., Koole, C., Noda, H., Zarzycka, B., Daley, E. J., Truong, T., Katritch, V., Gardella, T. J., Wootten, D., Sexton, P. M., McDonald, P. & Pratt, M. R., 11 Sep 2019, In : Journal of the American Chemical Society. 141, 36, p. 14210-14219 10 p.

Research output: Contribution to journalArticleResearchpeer-review

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)

Orthosteric and allosteric modes of interaction of novel selective agonists of the M1 muscarinic acetylcholine receptor

Avlani, V. A., Langmead, C. J., Guida, E., Wood, M. D., Tehan, B. G., Herdon, H. J., Watson, J. M., Sexton, P. & Christopoulos, A., 2010, In : Molecular Pharmacology. 78, 1, p. 94 - 104 11 p.

Research output: Contribution to journalArticleResearchpeer-review

52 Citations (Scopus)

Overlapping distributions of receptors for atrial natriuretic peptide and angiotensin II visualized by in vitro autoradiography: Morphological basis of physiological antagonism

Mendelsohn, F. A. O., Allen, A. M., Chai, S. Y., Sexton, P. M. & Figdor, R., 1 Jan 1987, In : Canadian Journal of Physiology and Pharmacology. 65, 8, p. 1517-1521 5 p.

Research output: Contribution to journalArticleResearchpeer-review

60 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

30 Citations (Scopus)

Pattern of Intra-Family Hetero-Oligomerization Involving the G-Protein-Coupled Secretin Receptor

Harikumar, K. G., Morfis, M., Sexton, P. & Miller, L. J., 2008, In : Journal of Molecular Neuroscience. 36, 1-3, p. 279 - 285 7 p.

Research output: Contribution to journalArticleResearchpeer-review

42 Citations (Scopus)

Peptide-oligonucleotide hybrids in antisense therapy

Pierce, T. L., White, A. R., Tregear, G. W. & Sexton, P. M., 2005, In : Mini reviews in medicinal chemistry. 5, 1, p. 41 - 55 15 p.

Research output: Contribution to journalArticleResearchpeer-review

13 Citations (Scopus)

Pharmacological discrimination of calcitonin receptor: receptor activity-modifying protein complexes

Hay, D. L., Christopoulos, G., Christopoulos, A., Poyner, D. R. & Sexton, P. M., 2005, In : Molecular Pharmacology. 67, 5, p. 1655 - 1665 11 p.

Research output: Contribution to journalArticleResearchpeer-review

132 Citations (Scopus)

Pharmacology of 5HT2C receptor-mediated ERK1/2 phosphorylation: Agonist-specific activation pathways and the impact of RNA editing

Werry, T. D., Stewart, G. D., Crouch, M. F., Watts, A., Sexton, P. & Christopoulos, A., 2008, In : Biochemical Pharmacology. 76, 10, p. 1276 - 1287 12 p.

Research output: Contribution to journalArticleResearchpeer-review

15 Citations (Scopus)

Phase-plate cryo-EM structure of a biased agonistbound human GLP-1 receptor-Gs complex

Liang, Y. L., Khoshouei, M., Glukhova, A., Furness, S. G. B., Zhao, P., Clydesdale, L., Koole, C., Truong, T. T., Thal, D. M., Lei, S., Radjainia, M., Danev, R., Baumeister, W., Wang, M. W., Miller, L. J., Christopoulos, A., Sexton, P. M. & Wootten, D., 1 Mar 2018, In : Nature. 555, 7694, p. 121-125 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
99 Citations (Scopus)

Phase-plate cryo-EM structure of a class B GPCR-G-protein complex

Liang, Y-L., Khoshouei, M., Radjainia, M., Zhang, Y., Glukhova, A., Tarrasch, J., Thal, D., Furness, S. G. B., Christopoulos, G., Coudrat, T., Danev, R., Baumeister, W., Miller, L. J., Christopoulos, A., Kobilka, B., Wootten, D., Skiniotis, G. & Sexton, P., 1 Jun 2017, In : Nature. 546, 7656, p. 118-123 6 p.

Research output: Contribution to journalArticleResearchpeer-review

210 Citations (Scopus)

Photoaffinity scanning in the mapping of the peptide receptor interface of class II G protein-coupled receptors

Pham, V. I. & Sexton, P. M., 2004, In : Journal of Peptide Science. 10, 4, p. 179 - 203 25 p.

Research output: Contribution to journalArticleResearchpeer-review

19 Citations (Scopus)
101 Citations (Scopus)
1 Citation (Scopus)

Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation

Koole, C., Wootten, D., Simms, J., Valant, C., Miller, L. J., Christopoulos, A. & Sexton, P., 2011, In : Molecular Pharmacology. 80, 3, p. 486 - 497 12 p.

Research output: Contribution to journalArticleResearchpeer-review

52 Citations (Scopus)
9 Citations (Scopus)

Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor

Davey, A. E., Leach, K., Valant, C., Conigrave, A. D., Sexton, P. M. & Christopoulos, A., 2012, In : Endocrinology. 153, 3, p. 1232 - 1241 10 p.

Research output: Contribution to journalArticleResearchpeer-review

110 Citations (Scopus)
17 Citations (Scopus)

Prediction of loops in G protein-coupled receptor homology models: effect of imprecise surroundings and constraints

Arora, B., Coudrat, T., Wootten, D., Christopoulos, A., Noronha, S. B. & Sexton, P. M., 25 Apr 2016, In : Journal of Chemical Information and Modeling. 56, 4, p. 671-686 16 p.

Research output: Contribution to journalArticleResearchpeer-review

5 Citations (Scopus)

Preface

Sexton, P. M. & Christopoulos, A., 12 Jul 2004, In : Current Pharmaceutical Design. 10, 17, p. xxx 1 p.

Research output: Contribution to journalEditorialOtherpeer-review

80 Citations (Scopus)

Probing structural requirements of positive allosteric modulators of the M4 muscarinic receptor

Huynh, T., Valant, C., Crosby, I. T., Sexton, P., Christopoulos, A. & Capuano, B., 2013, In : Journal of Medicinal Chemistry. 56, 20, p. 8196 - 8200 5 p.

Research output: Contribution to journalArticleResearchpeer-review

13 Citations (Scopus)

Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor

Khajehali, E., Valant, C., Jörg, M., Tobin, A. B., Conn, P. J., Lindsley, C. W., Sexton, P. M., Scammells, P. J. & Christopoulos, A., 1 Aug 2018, In : Biochemical Pharmacology. 154, p. 243-254 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
4 Citations (Scopus)

Procalcitonin has bioactivity at calcitonin receptor family complexes: Potential mediator implications in sepsis

Sexton, P., Christopoulos, G., Christopoulos, A., Nylen, E. S., Snider Jr., R. H. & Becker, K. L., 2008, In : Critical Care Medicine. 36, 5, p. 1637 - 1640 4 p.

Research output: Contribution to journalArticleResearchpeer-review

34 Citations (Scopus)

Prolonged calcitonin receptor signaling by salmon, but not human calcitonin, reveals ligand bias

Andreassen, K. V., Hjuler, S. T., Furness, S. G. B., Sexton, P. M., Christopoulos, A., Nosjean, O., Karsdal, M. A. & Henriksen, K., 2014, In : PLoS ONE. 9, 3 (Art. No: e92042), p. 1 - 10 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
33 Citations (Scopus)

Purification of calcitonin-like peptides from rat brain and pituitary

Hilton, J. M., Mitchelhill, K. I., Pozvek, G., Dowton, M., Quiza, M. & Sexton, P. M., 1 Jan 1998, In : Endocrinology. 139, 3, p. 982-992 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
32 Citations (Scopus)

Quantification of adenosine A1 receptor biased agonism: Implications for drug discovery

Baltos, J-A., Gregory, K. J., White, P. J., Sexton, P. M., Christopoulos, A. & May, L. T., 1 Jan 2016, In : Biochemical Pharmacology. 99, p. 101-112 12 p.

Research output: Contribution to journalArticleResearchpeer-review

29 Citations (Scopus)

Quantification of allosteric interactions at G protein-coupled receptors using radioligand binding assays

Leach, K., Sexton, P. & Christopoulos, A., 2011, In : Current Protocols in Pharmacology. 1, Supp 52 (Unit 1.22), p. 1 - 41 41 p.

Research output: Contribution to journalArticleResearchpeer-review

11 Citations (Scopus)

Ramp

Hay, D. L., Sexton, P. M. & Poyner, D. R., 2012, Encyclopedia of Signaling Molecules. Choi, S. (ed.). New York NY USA: Springer, p. 1570-1574 5 p.

Research output: Chapter in Book/Report/Conference proceedingEncyclopaedia / Dictionary EntryOtherpeer-review

RAMPs: 5 years on, where to now?

Morfis, M., Christopoulos, A. & Sexton, P., 2003, In : Trends in Pharmacological Sciences. 24, 11, p. 596 - 601 6 p.

Research output: Contribution to journalArticleResearchpeer-review

82 Citations (Scopus)

RAMPs as drug targets

Sexton, P. M., Poyner, D. R., Simms, J., Christopoulos, A. & Hay, D. L., 2012, RAMPs. Spielman, W. S. & Parameswaran, N. (eds.). 1st ed. USA: Springer, p. 61 - 74 14 p.

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

10 Citations (Scopus)

Recent advances in our understanding of peptide hormone receptors and RAMPS

Sexton, P. M., 12 Nov 1999, In : Current Opinion in Drug Discovery and Development. 2, 5, p. 440-448 9 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

10 Citations (Scopus)

Recent advances in the determination of G protein-coupled receptor structures

Thal, D. M., Vuckovic, Z., Draper-Joyce, C. J., Liang, Y-L., Glukhova, A., Christopoulos, A. & Sexton, P. M., 1 Aug 2018, In : Current Opinion in Structural Biology. 51, p. 28-34 7 p.

Research output: Contribution to journalArticleResearchpeer-review

19 Citations (Scopus)

Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function

Koole, C. R., Pabreja, K., Savage, E. E., Wootten, D. L., Furness, S. G. B., Miller, L. J., Christopoulos, A. & Sexton, P., 2013, In : Biochemical Society Transactions. 41, 1, p. 172 - 179 8 p.

Research output: Contribution to journalArticleResearchpeer-review

45 Citations (Scopus)

Receptor activity modifying proteins

Sexton, P. M., Albiston, A., Morfis, M. & Tilakaratne, N., 28 Mar 2001, In : Cellular Signalling. 13, 2, p. 73-83 11 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

162 Citations (Scopus)

Receptor activity modifying proteins and their potential as drug targets

Wootten, D., Simms, J. W., Hay, D. L., Christopoulos, A. & Sexton, P., 2010, Progress in Molecular Biology and Translational Science. Lunn, C. A. (ed.). 1st ed. UK: Academic Press, p. 53 - 79 27 p.

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

7 Citations (Scopus)

Receptor activity-modifying proteins differentially modulate the G protein-coupling efficiency of amylin receptors

Morfis, M., Tilakaratne, N., Furness, S. G. B., Christopoulos, G., Werry, T. D., Christopoulos, A. & Sexton, P., 2008, In : Endocrinology. 149, 11, p. 5423 - 5431 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
79 Citations (Scopus)

Refinement of glucagon-like peptide 1 docking to its intact receptor using mid-region photolabile probes and molecular modeling

Miller, L. J., Chen, Q., Lam, P. C-H., Pinon, D. I., Sexton, P., Abagyan, R. & Dong, M., 2011, In : Journal of Biological Chemistry. 286, 18, p. 15895 - 15907 13 p.

Research output: Contribution to journalArticleResearchpeer-review

50 Citations (Scopus)
28 Citations (Scopus)

Regulation of serotonin 5-HT{2C} receptors by chronic ligand exposure

Devlin, M. G., Smith, N. J., Ryan, O. M., Guida, E., Sexton, P. M. & Christopoulos, A., 2004, In : European Journal of Pharmacology. 498, 1-3, p. 59 - 69 11 p.

Research output: Contribution to journalArticleResearchpeer-review

16 Citations (Scopus)

Relaxin receptors - new drug targets for multiple disease states

van der Westhuizen, E. T., Summers, R. J., Halls, M. L., Bathgate, R. & Sexton, P., 2007, In : Current Drug Targets. 8, 1, p. 91 - 104 14 p.

Research output: Contribution to journalArticleResearchpeer-review

21 Citations (Scopus)

Responses of GPCR135 to human gene 3 (H3) relaxin in CHO-K1 cells determined by microphysiometry

van der Westhuizen, E. T., Sexton, P. M., Bathgate, R. A. D. & Summers, R. J., 2005, Relaxin and Related Peptides: Fourth International Conference. Sherwood, O. D., Fields, P. A. & Steinetz, B. G. (eds.). New York USA: New York Academy of Sciences, Vol. 1041. p. 332 - 337 6 p.

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

28 Citations (Scopus)