1986 …2023

Research output per year

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Research Output

2015

Towards tissue-specific pharmacology: insights from the calcium-sensing receptor as a paradigm for GPCR (patho)physiological bias

Leach, K., Conigrave, A. D., Sexton, P. M. & Christopoulos, A., 2015, In : Trends in Pharmacological Sciences. 36, 4, p. 215-225 11 p.

Research output: Contribution to journalArticleResearchpeer-review

31 Citations (Scopus)
2014

Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking

Yeatman, H. R., Lane, J. R. D., Choy, K. H. C., Lambert, N., Sexton, P., Christopoulos, A. & Canals, M., 2014, In : Journal of Biological Chemistry. 289, 22, p. 15856 - 15866 11 p.

Research output: Contribution to journalArticleResearchpeer-review

18 Citations (Scopus)

A new mechanism of allostery in a G protein-coupled receptor dimer

Lane, J. R. D., Donthamsetti, P., Shonberg, J., Draper-Joyce, C. J., Dentry, S., Michino, M., Shi, L., Lopez Munoz, L., Scammells, P. J., Capuano, B., Sexton, P., Javitch, J. A. & Christopoulos, A., 2014, In : Nature Chemical Biology. 10, 9, p. 745 - 752 8 p.

Research output: Contribution to journalArticleResearchpeer-review

80 Citations (Scopus)

A nuclear transport inhibitor that modulates the unfolded protein response and provides in vivo protection against lethal dengue virus infection

Fraser, J. E., Watanabe, S., Wang, C., Chan, W. K. K., Maher, B., Lopez-Denman, A., Hick, C. A., Wagstaff, K. M., Mackenzie, J. M., Sexton, P. M., Vasudevan, S. G. & Jans, D. A., 2014, In : Journal of Infectious Diseases. 210, 11, p. 1780 - 1791 12 p.

Research output: Contribution to journalArticleResearchpeer-review

49 Citations (Scopus)

Development of a photoactivatable allosteric ligand for the M1 muscarinic acetylcholine receptor

Davie, B. J., Sexton, P., Capuano, B., Christopoulos, A. & Scammells, P. J., 2014, In : ACS Chemical Neuroscience. 5, 10, p. 902 - 907 6 p.

Research output: Contribution to journalArticleResearchpeer-review

8 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)

International union of basic and clinical pharmacology. XC. Multisite pharmacology: Recommendations for the nomenclature of receptor allosterism and allosteric ligands

Christopoulos, A., Changeux, J-P., Catterall, W. A., Fabbro, D., Burris, T. P., Cidlowski, J. A., Olsen, R. W., Peters, J. A., Neubig, R., Pin, J. P., Sexton, P., Kenakin, T. P., Ehlert, F. J., Spedding, M. & Langmead, C. J., 2014, In : Pharmacological Reviews. 66, 4, p. 918 - 947 30 p.

Research output: Contribution to journalArticleResearchpeer-review

116 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 : Journal of Biological Chemistry. 289, 48, p. 33701 - 33711 11 p.

Research output: Contribution to journalArticleResearchpeer-review

32 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 : Journal of Biological Chemistry. 289, 9, p. 6067 - 6079 13 p.

Research output: Contribution to journalArticleResearchpeer-review

39 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 : Journal of Biological Chemistry. 289, 34, p. 23817 - 23837 21 p.

Research output: Contribution to journalArticleResearchpeer-review

33 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

172 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
30 Citations (Scopus)
Open Access
58 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

18 Citations (Scopus)

The class B G-protein-coupled GLP-1 receptor: an important target for the treatment of type-2 diabetes mellitus

Miller, L. J., Sexton, P. M., Dong, M. & Harikumar, K. G., 2014, In : International Journal of Obesity. 4, p. S9-S13 5 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

2013

Activation and allosteric modulation of a muscarinic acetylcholine receptor

Kruse, A. C., Ring, A. M., Manglik, A., Hu, J., Hu, K., Eitel, K., Hubner, H., Pardon, E., Valant, C., Sexton, P., Christopoulos, A., Felder, C. C., Gmeiner, P., Steyaert, J., Weis, W., Garcia, K. C., Wess, J. & Kobilka, B., 2013, In : Nature. 504, 7478, p. 101 - 106 6 p.

Research output: Contribution to journalArticleResearchpeer-review

501 Citations (Scopus)

Allosteric modulation of a chemogenetically modified G protein-coupled receptor

Abdul Ridha, A., Lane, J. R. D., Sexton, P., Canals, M. & Christopoulos, A., 2013, In : Molecular Pharmacology. 83, 2, p. 521 - 530 10 p.

Research output: Contribution to journalArticleResearchpeer-review

16 Citations (Scopus)

A simple method to generate stable cell lines for the analysis of transient protein-protein interactions

Savage, E. E., Wootten, D. L., Christopoulos, A., Sexton, P. & Furness, S. G. B., 2013, In : BioTechniques. 54, 4, p. 217 - 221 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
10 Citations (Scopus)

Bridging the gap: bitopic ligands of G-protein-coupled receptors

Lane, J. R. D., Sexton, P. M. & Christopoulos, A., 2013, In : Trends in Pharmacological Sciences. 34, 1, p. 59 - 66 8 p.

Research output: Contribution to journalArticleResearchpeer-review

97 Citations (Scopus)

CGRP/adrenomedullin

Wootten, D. L., Tilakaratne, N., Christopoulos, A. & Sexton, P., 2013, Handbook of Biologically Active Peptides. Kastin, A. J. (ed.). Second Edition ed. San Diego CA USA: Elsevier, p. 744 - 751 8 p.

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

1 Citation (Scopus)

Differential activation and modulation of the glucagon-like peptide-1 receptor by small molecule ligands

Wootten, D. L., Savage, E. E., Willard, F. S., Bueno, A. B., Sloop, K. W., Christopoulos, A. & Sexton, P., 2013, In : Molecular Pharmacology. 83, 4, p. 822 - 834 13 p.

Research output: Contribution to journalArticleResearchpeer-review

53 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

237 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

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)

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

23 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 : Journal of Biological Chemistry. 288, 29, p. 21082 - 21095 14 p.

Research output: Contribution to journalArticleResearchpeer-review

11 Citations (Scopus)

Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformations

Wootten, D. L., Simms, J. W., Miller, L. J., Christopoulos, A. & Sexton, P., 2013, In : Proceedings of the National Academy of Sciences. 110, 13, p. 5211 - 5216 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
101 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)

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

44 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

258 Citations (Scopus)

Structural biology: meet the B family

Sexton, P. & Wootten, D. L., 2013, In : Nature. 499, 7459, p. 417 - 418 2 p.

Research output: Contribution to journalLetterOther

5 Citations (Scopus)
2012

Allosteric modulation of endogenous metabolites as an avenue for drug discovery

Wootten, D. L., Savage, E. E., Valant, C., May, L. T., Sloop, K. W., Ficorilli, J., Showalter, A. D., Willard, F. S., Christopoulos, A. & Sexton, P. M., 2012, In : Molecular Pharmacology. 82, 2, p. 281 - 290 10 p.

Research output: Contribution to journalArticleResearchpeer-review

50 Citations (Scopus)

A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation

Canals, M., Lane, J., Wen, A., Scammells, P., Sexton, P. & Christopoulos, A., 2012, In : Journal of Biological Chemistry. 287, 1, p. 650 - 659 10 p.

Research output: Contribution to journalArticleResearchpeer-review

84 Citations (Scopus)

Consequences of splice variation on secretin family G protein-coupled receptor function

Furness, S. G. B., Wootten, D. L., Christopoulos, A. & Sexton, P. M., 2012, In : British Journal of Pharmacology. 166, 1, p. 98 - 109 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
27 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. 109, 45, p. 18607 - 18612 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
41 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

47 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 : FASEB Journal. 26, 12, p. 5092 - 5105 14 p.

Research output: Contribution to journalArticleResearchpeer-review

23 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 : Journal of Biological Chemistry. 287, 22, p. 18618 - 18635 18 p.

Research output: Contribution to journalArticleResearchpeer-review

14 Citations (Scopus)
1 Citation (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

109 Citations (Scopus)
79 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 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)

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 : Journal of Biological Chemistry. 287, 6, p. 3659 - 3673 15 p.

Research output: Contribution to journalArticleResearchpeer-review

20 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 : Journal of Biological Chemistry. 287, 6, p. 3642 - 3658 17 p.

Research output: Contribution to journalArticleResearchpeer-review

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

31 Citations (Scopus)