1986 …2020

Research output per year

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Research Output

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Article

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
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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

36 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
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36 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

30 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

13 Citations (Scopus)

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

83 Citations (Scopus)

Rational development of a high-affinity secretin receptor antagonist

Dong, M., Harikumar, K. G., Raval, S. R., Milburn, J. E., Clark, C., Alcala-Torano, R., Mobarec, J. C., Reynolds, C. A., Ghirlanda, G., Christopoulos, A., Wootten, D., Sexton, P. M. & Miller, L. J., Jul 2020, In : Biochemical Pharmacology. 177, 13 p., 113929.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (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

24 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

46 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
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87 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 : The 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

22 Citations (Scopus)

Reversible calcitonin binding to solubilized sheep brain binding sites

Sexton, P. M., Schneider, H. G., D'Santos, C. S., Mendelsohn, F. A. O., Kemp, B. E., Moseley, J. M., Martin, T. J. & Findlay, D. M., 1 Jan 1991, In : Biochemical Journal. 273, 1, p. 179-184 6 p.

Research output: Contribution to journalArticleResearchpeer-review

14 Citations (Scopus)

REVIEW: Receptor activity modifying proteins

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

Research output: Contribution to journalArticleResearchpeer-review

RNA editing of the serotonin 5HT2C receptor and its effects on cell signalling, pharmacology and brain function

Werry, T. D., Loiacono, R., Sexton, P. & Christopoulos, A., 2008, In : Pharmacology and Therapeutics. 119, 1, p. 7 - 23 17 p.

Research output: Contribution to journalArticleResearchpeer-review

115 Citations (Scopus)

Role of the second extracellular loop of the adenosine A1 receptor on allosteric modulator binding, signaling, and cooperativity

Nguyen, A. T. N., Vecchio, E. A., Thomas, T., Nguyen, T. D., Aurelio, L., Scammells, P. J., White, P. J., Sexton, P. M., Gregory, K. J., May, L. T. & Christopoulos, A., 1 Dec 2016, In : Molecular Pharmacology. 90, 6, p. 715-725 11 p.

Research output: Contribution to journalArticleResearchpeer-review

25 Citations (Scopus)

Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) differentially regulates orthosteric but not allosteric agonist binding and function

Koole, C. R., Wootten, D. L., Simms, J., Savage, E. E., Miller, L. J., Christopoulos, A. & Sexton, P. M., 2012, In : The Journal of Biological Chemistry. 287, 6, p. 3659 - 3673 15 p.

Research output: Contribution to journalArticleResearchpeer-review

22 Citations (Scopus)

Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) has a critical role in GLP-1 peptide binding and receptor activation

Koole, C. R., Wootten, D. L., Simms, J. W., Miller, L. J., Christopoulos, A. & Sexton, P., 2012, In : The Journal of Biological Chemistry. 287, 6, p. 3642 - 3658 17 p.

Research output: Contribution to journalArticleResearchpeer-review

64 Citations (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 : The Journal of Biological Chemistry. 285, 13, p. 9919 - 9931 13 p.

Research output: Contribution to journalArticleResearchpeer-review

19 Citations (Scopus)
58 Citations (Scopus)

Small molecule allosteric modulation of the glucagon-like Peptide-1 receptor enhances the insulinotropic effect of oxyntomodulin

Willard, F. S., Wootten, D. L., Showalter, A. D., Savage, E. E., Ficorilli, J., Farb, T. B., Bokvist, K., Alsina-Fernandez, J., Furness, S. GB., Christopoulos, A., Sexton, P. M. & Sloop, K. W., 2012, In : Molecular Pharmacology. 82, 6, p. 1066 - 1073 8 p.

Research output: Contribution to journalArticleResearchpeer-review

37 Citations (Scopus)

Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice

Qin, C. X., May, L. T., Li, R., Cao, N., Rosli, S., Deo, M., Alexander, A. E., Horlock, D., Bourke, J. E., Yang, Y. H., Stewart, A. G., Kaye, D. M., Du, X. J., Sexton, P. M., Christopoulos, A., Gao, X. M. & Ritchie, R. H., 7 Feb 2017, In : Nature Communications. 8, 13 p., 14232.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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36 Citations (Scopus)

Spatial approximation between secretin residue five and the third extracellular loop of its receptor provides new insight into the molecular basis of natural agonist binding

Dong, M., Lam, P. C-H., Pinon, D. I., Sexton, P., Abagyan, R. & Miller, L. J., 2008, In : Molecular Pharmacology. 74, 2, p. 413 - 422 10 p.

Research output: Contribution to journalArticleResearchpeer-review

31 Citations (Scopus)

Spatial proximity between a photolabile residue in position 19 of salmon calcitonin and the amino terminus of the human calcitonin receptor

Pham, V., Wade, J. D., Purdue, B. W. & Sexton, P. M., 2004, In : The Journal of Biological Chemistry. 279, 8, p. 6720 - 6729 10 p.

Research output: Contribution to journalArticleResearchpeer-review

33 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

229 Citations (Scopus)

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 : The Journal of Biological Chemistry. 287, 44, p. 37066 - 37077 12 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

Structural and functional insights into the juxtamembranous amino-terminal tail and extracellular loop regions of class B GPCRs

Dong, M., Koole, C. R., Wootten, D. L., Sexton, P. & Miller, L. J., 2014, In : British Journal of Pharmacology. 171, 5, p. 1085 - 1101 17 p.

Research output: Contribution to journalArticleResearchpeer-review

20 Citations (Scopus)

Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs

Dror, R., Green, H. F., Valant, C., Borhani, D. W., Valcourt, J. R., Pan, A. C., Arlow, D. H., Canals, M., Lane, J. R. D., Rahmani, R. S., Baell, J. B., Sexton, P., Christopoulos, A. & Shaw, D. E., 2013, In : Nature. 503, 7475, p. 295 - 299 5 p.

Research output: Contribution to journalArticleResearchpeer-review

265 Citations (Scopus)

Structural basis of Gs and Gi recognition by the human glucagon receptor

Qiao, A., Han, S., Li, X., Li, Z., Zhao, P., Dai, A., Chang, R., Tai, L., Tan, Q., Chu, X., Ma, L., Thorsen, T. S., Reedtz-Runge, S., Yang, D., Wang, M-W., Sexton, P. M., Wootten, D., Sun, F., Zhao, Q. & Wu, B., 20 Mar 2020, In : Science. 367, 6484, p. 1346-1352 7 p.

Research output: Contribution to journalArticleResearchpeer-review

6 Citations (Scopus)
52 Citations (Scopus)

Structural features embedded in G protein-coupled receptor co-crystal structures are key to their success in virtual screening

Coudrat, T., Christopoulos, A., Sexton, P. M. & Wootten, D., 1 Apr 2017, In : PLoS ONE. 12, 4, 29 p., e0174719.

Research output: Contribution to journalArticleResearchpeer-review

File
3 Citations (Scopus)

Structure/function relationships of calcitonin analogues as agonists, antagonists, or inverse agonists in a constitutively activated receptor cell system

Pozvek, G., Hilton, J. M., Quiza, M., Houssami, S. & Sexton, P. M., 1 Jan 1997, In : Molecular Pharmacology. 51, 4, p. 658-665 8 p.

Research output: Contribution to journalArticleResearchpeer-review

33 Citations (Scopus)

Structure-Activity Relationships of Pan-Gαq/11 Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators

Berizzi, A. E., Bender, A. M., Lindsley, C. W., Conn, P. J., Sexton, P. M., Langmead, C. J. & Christopoulos, A., 18 Jul 2018, In : ACS Chemical Neuroscience. 9, 7, p. 1818-1828 11 p.

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

Structure-based discovery of selective positive allosteric modulators of antagonists for the M2 muscarinic acetylcholine receptor

Korczynska, M., Clark, M. J., Valant, C., Xu, J., Moo, E. V., Albold, S., Weiss, D. R., Torosyan, H., Huang, W., Kruse, A. C., Lyda, B. R., May, L. T., Baltos, J. A., Sexton, P. M., Kobilka, B. K., Christopoulos, A., Shoichet, B. K. & Sunahara, R. K., 6 Mar 2018, In : Proceedings of the National Academy of Sciences of the United States of America. 115, 10, p. E2419-E2428 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
21 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

20 Citations (Scopus)

Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors

May, L. T., Avlani, V. A., Langmead, C. J., Herdon, H. J., Wood, M. D., Sexton, P. & Christopoulos, A., 2007, In : Molecular Pharmacology. 72, 2, p. 463 - 476 14 p.

Research output: Contribution to journalArticleResearchpeer-review

95 Citations (Scopus)

Structure of the adenosine A1 receptor reveals the basis for subtype selectivity

Glukhova, A., Thal, D. M., Nguyen, A. T., Vecchio, L., Jorg, M., Scammells, P. J., May, L. T., Sexton, P. M. & Christopoulos, A., 23 Feb 2017, In : Cell. 168, 5, p. 867-877.e13

Research output: Contribution to journalArticleResearchpeer-review

108 Citations (Scopus)

Structure of the adenosine-bound human adenosine A1 receptor-Gi complex

Draper-Joyce, C. J., Khoshouei, M., Thal, D. M., Liang, Y. L., Nguyen, A. T. N., Furness, S. G. B., Venugopal, H., Baltos, J. A., Plitzko, J. M., Danev, R., Baumeister, W., May, L. T., Wootten, D., Sexton, P. M., Glukhova, A. & Christopoulos, A., 20 Jun 2018, In : Nature. 558, 7711, p. 559-565 7 p.

Research output: Contribution to journalArticleResearchpeer-review

108 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

38 Citations (Scopus)

Synthesis and pharmacological evaluation of M4 muscarinic receptor positive allosteric modulators derived from VU10004

Huynh, T., Valant, C., Crosby, I. T., Sexton, P., Christopoulos, A. & Capuano, B., 2015, In : ACS Chemical Neuroscience. 6, 6, p. 838 - 844 7 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

Systematic analysis of factors influencing observations of biased agonism at the mu-opioid receptor

Thompson, G. L., Lane, J. R., Coudrat, T., Sexton, P. M., Christopoulos, A. & Canals, M., 1 Aug 2016, In : Biochemical Pharmacology. 113, p. 70-87 18 p.

Research output: Contribution to journalArticleResearchpeer-review

34 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

118 Citations (Scopus)

The complexity of signalling mediated by the glucagon-like peptide-1 receptor

Fletcher, M. M., Halls, M. L., Christopoulos, A., Sexton, P. M. & Wootten, D., 15 Apr 2016, In : Biochemical Society Transactions. 44, 2, p. 582-588 7 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)