1986 …2023

Research output per year

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Research Output

2012

Stimulus bias provides evidence for conformational constraints in the structure of a G protein-coupled receptor

Gregory, K. J., Sexton, P. M., Tobin, A. B. & Christopoulos, A., 2012, In : Journal of Biological Chemistry. 287, 44, p. 37066 - 37077 12 p.

Research output: Contribution to journalArticleResearchpeer-review

23 Citations (Scopus)

Structure-function studies of muscarinic acetylcholine receptors

Leach, K., Simms, J., Sexton, P. M. & Christopoulos, A., 2012, Muscarinic Receptors - Handbook of Experimental Pharmacology 208. Fryer, A. D., Christopoulos, A. & Nathanson, N. M. (eds.). 1st ed. USA: Springer, p. 29 - 48 20 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Other

13 Citations (Scopus)

Synthesis and characterization of novel 2-amino-3-benzoylthiophene derivatives as biased allosteric agonists and modulators of the adenosine A1 receptor

Valant, C., Aurelio, L., Devine, S. M., Ashton, T. D., White, J. M., Sexton, P. M., Christopoulos, A. & Scammells, P. J., 2012, In : Journal of Medicinal Chemistry. 55, 5, p. 2367 - 2375 9 p.

Research output: Contribution to journalArticleResearchpeer-review

36 Citations (Scopus)

The best of both worlds? Bitopic orthosteric/allosteric ligands of G protein - coupled receptors

Valant, C., Lane, J., Sexton, P. & Christopoulos, A., 2012, In : Annual Review of Pharmacology and Toxicology. 53, p. 153 - 178 26 p.

Research output: Contribution to journalArticleResearchpeer-review

114 Citations (Scopus)
2011

Allosteric modulation of G protein-coupled receptors: A pharmacological perspective

Keov, P., Sexton, P. & Christopoulos, A., 2011, In : Neuropharmacology. 60, 1, p. 24 - 35 12 p.

Research output: Contribution to journalArticleResearchpeer-review

201 Citations (Scopus)

Allostery in GPCRs: 'MWC' revisited

Canals, M., Sexton, P. & Christopoulos, A., 2011, In : Trends in Biochemical Sciences. 36, 12, p. 663 - 672 10 p.

Research output: Contribution to journalArticleResearchpeer-review

48 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)

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

45 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 : Journal of Biological Chemistry. 286, 27, p. 23888 - 23899 12 p.

Research output: Contribution to journalArticleResearchpeer-review

22 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

52 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)

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)

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

226 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

19 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)
2010

Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: Implications for drug screening

Koole, C., Wootten, D., Simms, J., Valant, C., Sridhar, R., Woodman, O., Miller, L. J., Summers, R., Christopoulos, A. & Sexton, P. M., 2010, In : Molecular Pharmacology. 78, 3, p. 456 - 465 10 p.

Research output: Contribution to journalArticleResearchpeer-review

135 Citations (Scopus)

Delineating the mode of action of adenosine A1 receptor allosteric modulators

Valant, C., Aurelio, L., Urmaliya, V., White, P., Scammells, P., Sexton, P. & Christopoulos, A., 2010, In : Molecular Pharmacology. 78, 3, p. 444 - 455 12 p.

Research output: Contribution to journalArticleResearchpeer-review

34 Citations (Scopus)

Detection of novel functional selectivity at M3 muscarinic acetylcholine receptors using a Saccharomyces cerevisiae platform

Stewart, G. D., Sexton, P. & Christopoulos, A., 2010, In : ACS Chemical Biology. 5, 4, p. 365 - 375 11 p.

Research output: Contribution to journalArticleResearchpeer-review

21 Citations (Scopus)

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)

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)

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)

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)

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 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

119 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)

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

29 Citations (Scopus)
17 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)

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)

Secretin occupies a single protomer of the homodimeric secretin receptor complex: insights from photoaffinity labeling studies using dual sites of covalent attachment

Dong, M., Lam, P. C-H., Pinon, D. I., Orry, A., Sexton, P., Abagyan, R. & Miller, L. J., 2010, In : Journal of Biological Chemistry. 285, 13, p. 9919 - 9931 13 p.

Research output: Contribution to journalArticleResearchpeer-review

19 Citations (Scopus)
52 Citations (Scopus)

The effect of social isolation on rat brain expression of genes associated with endocannabinoid signaling

Robinson, S. A., Loiacono, R., Christopoulos, A., Sexton, P. & Malone, D. T., 2010, In : Brain Research. 1343, p. 153 - 167 15 p.

Research output: Contribution to journalArticleResearchpeer-review

38 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)

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

1 Citation (Scopus)
2009

3- and 6-substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists

Aurelio, L., Valant, C., Figler, H., Flynn, B. L., Linden, J., Sexton, P., Christopoulos, A. & Scammells, P. J., 2009, In : Bioorganic & Medicinal Chemistry. 17, 20, p. 7353 - 7361 9 p.

Research output: Contribution to journalArticleResearchpeer-review

27 Citations (Scopus)
92 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)

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)

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)

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

37 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)
2008

2-Aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists

Ferguson, G. N., Valant, C., Horne, H. J., Figler, H., Flynn, B. L., Linden, J., Chalmers, D. K., Sexton, P., Christopoulos, A. & Scammells, P. J., 2008, In : Journal of Medicinal Chemistry. 51, 19, p. 6165 - 6172 8 p.

Research output: Contribution to journalArticleResearchpeer-review

38 Citations (Scopus)
132 Citations (Scopus)

Benzodiazepine ligands can act as allosteric modulators of the Type 1 cholecystokinin receptor

Gao, F., Sexton, P., Christopoulos, A. & Miller, L. J., 2008, In : Bioorganic and Medicinal Chemistry Letters. 18, 5, p. 4401 - 4404 4 p.

Research output: Contribution to journalArticleResearchpeer-review

16 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)

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

86 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

41 Citations (Scopus)