1986 …2020

Research output per year

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Research Output

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Article

M1 muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss

Bradley, S. J., Bourgognon, J. M., Sanger, H. E., Verity, N., Mogg, A. J., White, D. J., Butcher, A. J., Moreno, J. A., Molloy, C., Macedo-Hatch, T., Edwards, J. M., Wess, J., Pawlak, R., Read, D. J., Sexton, P. M., Broad, L. M., Steinert, J. R., Mallucci, G. R., Christopoulos, A., Felder, C. C. & 1 others, Tobin, A. B., 1 Feb 2017, In : Journal of Clinical Investigation. 127, 2, p. 487-499 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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28 Citations (Scopus)

Mapping spatial approximations between the amino terminus of secretin and each of the extracellular loops of its receptor using cysteine trapping

Dong, M., Xu, X., Ball, A. M., Makhoul, J. A., Lam, P. CH., Pinon, D. I., Orry, A., Sexton, P. M., Abagyan, R. & Miller, L. J., 2012, In : The FASEB Journal. 26, 12, p. 5092 - 5105 14 p.

Research output: Contribution to journalArticleResearchpeer-review

25 Citations (Scopus)

Mechanisms of ERK1/2 regulation by seven-transmembrane-domain receptors

Werry, T. D., Christopoulos, A. & Sexton, P. M., 2006, In : Current Pharmaceutical Design. 12, 14, p. 1683 - 1702 20 p.

Research output: Contribution to journalArticleResearchpeer-review

34 Citations (Scopus)

Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor

Abdul Ridha, A., Lane, J. R. D., Mistry, S. N., Lopez Munoz, L., Sexton, P., Scammells, P. J., Christopoulos, A. & Canals, M., 2014, In : The Journal of Biological Chemistry. 289, 48, p. 33701 - 33711 11 p.

Research output: Contribution to journalArticleResearchpeer-review

35 Citations (Scopus)

Minireview: Signal bias, allosterism, and polymorphic variation at the GLP-1R: implications for drug discovery

Koole, C. R., Savage, E. E., Christopoulos, A., Miller, L. J., Sexton, P. & Wootten, D. L., 2013, In : Molecular Endocrinology. 27, 8, p. 1234 - 1244 11 p.

Research output: Contribution to journalArticleResearchpeer-review

25 Citations (Scopus)

Modulating receptor function through RAMPs: can they represent drug targets in themselves?

Sexton, P. M., Poyner, D. R., Simms, J. W., Christopoulos, A. & Hay, D. L., 2009, In : Drug Discovery Today. 14, 7-8, p. 413 - 419 7 p.

Research output: Contribution to journalArticleResearchpeer-review

53 Citations (Scopus)

Modulation of the glucagon-like peptide-1 receptor signaling by naturally occurring and synthetic flavonoids

Wootten, D., Simms, J., Koole, C., Woodman, O., Summers, R., Christopoulos, A. & Sexton, P., 2011, In : Journal of Pharmacology and Experimental Therapeutics. 336, 2, p. 540 - 550 11 p.

Research output: Contribution to journalArticleResearchpeer-review

49 Citations (Scopus)

Molecular approximations between residues 21 and 23 of secretin and its receptor: Development of a model for peptide docking with the amino terminus of the secretin receptor

Dong, M., Lam, P. C-H., Gao, F., Hosohata, K., Pinon, D. I., Sexton, P., Abagyan, R. & Miller, L. J., 2007, In : Molecular Pharmacology. 72, 2, p. 280 - 290 11 p.

Research output: Contribution to journalArticleResearchpeer-review

30 Citations (Scopus)

Molecular basis for benzodiazepine agonist action at the type 1 cholecystokinin receptor

Harikumar, K. G., Cawston, E. E., Lam, P. C. H., Patil, A., Orry, A., Henke, B., Abagyan, R., Christopoulos, A., Sexton, P. & Miller, L. J., 2013, In : The Journal of Biological Chemistry. 288, 29, p. 21082 - 21095 14 p.

Research output: Contribution to journalArticleResearchpeer-review

11 Citations (Scopus)

Molecular basis for binding and subtype selectivity of 1,4-benzodiazepine antagonist ligands of the cholecystokinin receptor

Cawston, E. E., Lam, P. C. H., Harikumar, K. G., Dong, M., Ball, A. M., Augustine, M. L., Akgun, E., Portoghese, P. S., Orry, A., Abagyan, R., Sexton, P. M. & Miller, L., 2012, In : The Journal of Biological Chemistry. 287, 22, p. 18618 - 18635 18 p.

Research output: Contribution to journalArticleResearchpeer-review

15 Citations (Scopus)

Molecular Basis for Hormone Recognition and Activation of Corticotropin-Releasing Factor Receptors

Ma, S., Shen, Q., Zhao, L. H., Mao, C., Zhou, X. E., Shen, D. D., de Waal, P. W., Bi, P., Li, C., Jiang, Y., Wang, M. W., Sexton, P. M., Wootten, D., Melcher, K., Zhang, Y. & Xu, H. E., 6 Feb 2020, In : Molecular Cell. 77, 3, p. 669-680.e4 16 p.

Research output: Contribution to journalArticleResearchpeer-review

7 Citations (Scopus)

Molecular Basis of Action of a Small-Molecule Positive Allosteric Modulator Agonist at the Type 1 Cholecystokinin Holoreceptor

Desai, A. J., Mechin, I., Nagarajan, K., Valant, C., Wootten, D., Lam, P. C. H., Orry, A., Abagyan, R., Nair, A., Sexton, P. M., Christopoulos, A. & Miller, L. J., 1 Mar 2019, In : Molecular Pharmacology. 95, 3, p. 245-259 15 p.

Research output: Contribution to journalArticleResearchpeer-review

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)

Molecular basis of secretin docking to its intact receptor using multiple photolabile probes distributed throughout the

Dong, M., Lam, P., Pinon, D., Orry, A., Sexton, P., Abagyan, R. & Miller, L. J., 2011, In : The Journal of Biological Chemistry. 286, 27, p. 23888 - 23899 12 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor

Abdul Ridha, A., Lopez, L., Keov, P., Thal, D., Mistry, S. N., Sexton, P., Lane, J. R. D., Canals, M. & Christopoulos, A., 2014, In : The Journal of Biological Chemistry. 289, 9, p. 6067 - 6079 13 p.

Research output: Contribution to journalArticleResearchpeer-review

40 Citations (Scopus)

Molecular mechanism of action of triazolobenzodiazepinone agonists of the type 1 cholecystokinin receptor. Possible cooperativity across the receptor homodimeric complex

Desai, A. J., Lam, P. C. H., Orry, A., Abagyan, R., Christopoulos, A., Sexton, P. & Miller, L. J., 2015, In : Journal of Medicinal Chemistry. 58, 24, p. 9562-9577 16 p.

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties

Leach, K., Loiacono, R. E., Felder, C. C., McKinzie, D. L., Mogg, A., Shaw, D. B., Sexton, P. M. & Christopoulos, A., 2010, In : Neuropsychopharmacology. 35, 4, p. 855 - 869 15 p.

Research output: Contribution to journalArticleResearchpeer-review

120 Citations (Scopus)

Molecular mechanisms of action of M5 muscarinic acetylcholine receptor allosteric modulators

Berizzi, A. E., Gentry, P. R., Rueda, P., Hoedt, S. D., Sexton, P. M., Langmead, C. J. & Christopoulos, A., 1 Oct 2016, In : Molecular Pharmacology. 90, 4, p. 427-436 10 p.

Research output: Contribution to journalArticleResearchpeer-review

12 Citations (Scopus)

Molecular mechanisms of bitopic ligand engagement with the M1 muscarinic acetylcholine receptor

Keov, P., Lopez, L., Devine, S., Valant, C., Lane, J. R. D., Scammells, P. J., Sexton, P. & Christopoulos, A., 2014, In : The Journal of Biological Chemistry. 289, 34, p. 23817 - 23837 21 p.

Research output: Contribution to journalArticleResearchpeer-review

33 Citations (Scopus)

Molecular pharmacology of the calcitonin receptor

Purdue, B. W., Tilakaratne, N. & Sexton, P., 2002, In : Receptors and Channels. 8, 3 & 4, p. 243 - 255 13 p.

Research output: Contribution to journalArticleResearchpeer-review

84 Citations (Scopus)

Monotreme glucagon-like peptide-1 in venom and gut: one gene - two very different functions

Tsend-Ayush, E., He, C., Myers, M. A., Andrikopoulos, S., Wong, N., Sexton, P. M., Wootten, D., Forbes, B. E. & Grutzner, F., 29 Nov 2016, In : Scientific Reports. 6, 12 p., 37744.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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5 Citations (Scopus)

Mouse receptor-activity-modifying proteins 1, -2 and -3: Amino acid sequence, expression and function

Husmann, K., Sexton, P. M., Fischer, J. A. & Born, W., 25 Apr 2000, In : Molecular and Cellular Endocrinology. 162, 1-2, p. 35-43 9 p.

Research output: Contribution to journalArticleResearchpeer-review

71 Citations (Scopus)

Multiple amylin receptors arise from receptor activity-modifying protein interaction with the calcitonin receptor gene product

Christopoulos, G., Perry, K. J., Morfis, M., Tilakaratne, N., Gao, Y., Fraser, N. J., Main, M. J., Foord, S. M. & Sexton, P. M., 1 Jan 1999, In : Molecular Pharmacology. 56, 1, p. 235-242 8 p.

Research output: Contribution to journalArticleResearchpeer-review

375 Citations (Scopus)

Multiple ramp domains are required for generation of amylin receptor phenotype from the calcitonin receptor gene product.

Zumpe, E. T., Tilakaratne, N., Fraser, NJ., Christopoulos, G., Foord, S. M. & Sexton, P., 7 Jan 2000, In : Biochemical and Biophysical Research Communications. 267, 1, p. 368-372

Research output: Contribution to journalArticleResearchpeer-review

61 Citations (Scopus)

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
27 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

184 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
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13 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 : The Journal of Biological Chemistry. 290, 32, p. 19478-19488 11 p.

Research output: Contribution to journalArticleResearchpeer-review

96 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

9 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 : The Journal of Biological Chemistry. 278, 5, p. 3293 - 3297 5 p.

Research output: Contribution to journalArticleResearchpeer-review

228 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

2 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

32 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 characterization of mono-, dual- and tri-peptidic agonists at GIP and GLP-1 receptors

Yuliantie, E., Darbalaei, S., Dai, A., Zhao, P., Yang, D., Sexton, P. M., Wang, M-W. & Wootten, D., Jul 2020, In : Biochemical Pharmacology. 177, 13 p., 114001.

Research output: Contribution to journalArticleResearchpeer-review

2 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

140 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
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120 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

242 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)
110 Citations (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

53 Citations (Scopus)
Open Access
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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

114 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)
83 Citations (Scopus)