1986 …2020

Research output per year

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Research Output

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Article

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

39 Citations (Scopus)

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

28 Citations (Scopus)

4-phenylpyridin-2-one derivatives: a novel class of positive allosteric modulator of the M1 muscarinic acetylcholine receptor

Mistry, S. N., Jorg, M., Lim, H., Vinh, N. B., Sexton, P. M., Capuano, B., Christopoulos, A., Lane, J. R. & Scammells, P. J., 14 Jan 2016, In : Journal of Medicinal Chemistry. 59, 1, p. 388-409 22 p.

Research output: Contribution to journalArticleResearchpeer-review

23 Citations (Scopus)

6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity

Jorg, M. T., van der Westhuizen, E. T., Khajehali, E., Burger, W. A. C., White, J., Choy, K. H. C., Tobin, A. B., Sexton, P. M., Valant, C., Capuano, B., Christopoulos, A. & Scammells, P. J., 20 Mar 2019, In : ACS Chemical Neuroscience. 10, 3, p. 1099-1114 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Abundant calcitonin receptors in isolated rat osteoclasts. Biochemical and autoradiographic characterization

Nicholson, G. C., Moseley, J. M., Sexton, P. M., Mendelsohn, F. A. & Martin, T. J., 1 Jan 1986, In : Journal of Clinical Investigation. 78, 2, p. 355-360 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
401 Citations (Scopus)

Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor

Miao, Y., Goldfeld, D. A., Moo, E. V., Sexton, P. M., Christopoulos, A., McCammon, J. A. & Valant, C., 20 Sep 2016, In : Proceedings of the National Academy of Sciences of the United States of America. 113, 38, p. E5675-E5684 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
45 Citations (Scopus)

A critical role for the short intracellular C terminus in receptor activity-modifying protein function

Udawela, M., Christopoulos, G., Morfis, M., Christopoulos, A., Ye, S., Tilakaratne, N. & Sexton, P. M., 2006, In : Molecular Pharmacology. 70, 5, p. 1750 - 1760 11 p.

Research output: Contribution to journalArticleResearchpeer-review

31 Citations (Scopus)

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

520 Citations (Scopus)

Activation of the GLP-1 receptor by a non-peptidic agonist

Zhao, P., Liang, Y. L., Belousoff, M. J., Deganutti, G., Fletcher, M. M., Willard, F. S., Bell, M. G., Christe, M. E., Sloop, K. W., Inoue, A., Truong, T. T., Clydesdale, L., Furness, S. G. B., Christopoulos, A., Wang, M. W., Miller, L. J., Reynolds, C. A., Danev, R., Sexton, P. M. & Wootten, D., 8 Jan 2020, In : Nature. 577, 7790, p. 432-436 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
9 Citations (Scopus)

A hydrogen-bonded polar network in the core of the glucagon-like peptide-1 receptor is a fulcrum for biased agonism: lessons from class B crystal structuress

Wootten, D., Reynolds, C. A., Koole, C., Smith, K. J., Mobarec, J. C., Simms, J., Quon, T., Coudrat, T., Furness, S. G. B., Miller, L. J., Christopoulos, A. & Sexton, P. M., 1 Mar 2016, In : Molecular Pharmacology. 89, 3, p. 335-347 13 p.

Research output: Contribution to journalArticleResearchpeer-review

29 Citations (Scopus)

Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology

Leach, K., Sexton, P. & Christopoulos, A., 2007, In : Trends in Pharmacological Sciences. 28, 8, p. 382 - 389 8 p.

Research output: Contribution to journalArticleResearchpeer-review

258 Citations (Scopus)

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

137 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)

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

52 Citations (Scopus)

Allosteric modulation of G protein-coupled receptors

May, L. T., Avlani, V. A., Sexton, P. & Christopoulos, A., 2004, In : Current Pharmaceutical Design. 10, 17, p. 2003 - 2013 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Allosteric modulation of G protein-coupled receptors

May, L. T., Leach, K., Sexton, P. M. & Christopoulos, A., 2007, In : Annual Review of Pharmacology and Toxicology. 47, p. 1 - 51 51 p.

Research output: Contribution to journalArticleResearchpeer-review

502 Citations (Scopus)

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

205 Citations (Scopus)

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 : The Journal of Biological Chemistry. 289, 22, p. 15856 - 15866 11 p.

Research output: Contribution to journalArticleResearchpeer-review

19 Citations (Scopus)

Allosteric modulation of muscarinic acetylcholine receptors

Gregory, K. J., Sexton, P. & Christopoulos, A., 2007, In : Current Neuropharmacology. 5, 3, p. 157 - 167 11 p.

Research output: Contribution to journalArticleResearchpeer-review

78 Citations (Scopus)
94 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

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 : The Journal of Biological Chemistry. 287, 1, p. 650 - 659 10 p.

Research output: Contribution to journalArticleResearchpeer-review

87 Citations (Scopus)

Amylin and calcitonin gene-related peptide in the rat kidney: functional and autoradiographic studies.

Haynes, J. M., Wookey, P. J., Tikellis, C., Du, H-C., Sexton, P. & Cooper, M. E., 1994, In : Canadian Journal of Physiology and Pharmacology. 72, p. 566

Research output: Contribution to journalArticleResearchpeer-review

Amylin binding in rat renal cortex, stimulation of adenylyl cyclase, and activation of plasma renin

Wookey, P. J., Tikellis, C., He-Cheng, D. U., Qin, H. F., Sexton, P. M. & Cooper, M. E., 1996, In : American Journal of Physiology. 270, 2 PART 2

Research output: Contribution to journalArticleResearchpeer-review

61 Citations (Scopus)

Amylin is an agonist of the renal porcine calcitonin receptor

Sextont, P. M., Houssami, S., Brady, C. L., Myers, D. E. & Findlays, D. M., 1 Jan 1994, In : Endocrinology. 134, 5, p. 2103-2107 5 p.

Research output: Contribution to journalArticleResearchpeer-review

26 Citations (Scopus)

Amylin receptor phenotypes derived from human calcitonin receptor/RAMP coexpression exhibit pharmacological differences dependent on receptor isoform and host cell environment.

Tilakaratne, N., Christopoulos, G., Zumpe, E. T., Foord, S. M. & Sexton, P. M., Jul 2000, In : Journal of Pharmacology and Experimental Therapeutics. 294, 1, p. 61-72 12 p.

Research output: Contribution to journalArticleResearchpeer-review

131 Citations (Scopus)

Amylin receptors: Molecular composition and pharmacology

Hay, D. L., Christopoulos, G., Christopoulos, A. & Sexton, P., 2004, In : Biochemical Society Transactions. 32, Pt 5, p. 865 - 867 3 p.

Research output: Contribution to journalArticleOther

67 Citations (Scopus)

An allosteric role for receptor activity-modifying proteins in defining GPCR pharmacology

Gingell, J. J., Simms, J., Barwell, J., Poyner, D., Watkins, H. A., Pioszak, A. A., Sexton, P. M. & Hay, D., 17 May 2016, In : Cell Discovery. 2, 14 p., 16012.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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25 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)

Angiotensin II receptors and angiotensin converting enzyme in the medulla oblongata

Allen, A. M., Chai, S. Y., Sexton, P. M., Lewis, S. J., Verberne, A. J. M., Jarrott, B., Louis, W. J., Clevers, J., McKinley, M. J., Paxinos, G. & Mendelsohn, F. A. O., 1 Jan 1987, In : Hypertension. 9, 6, Part 2, p. III-198-III-205 8 p.

Research output: Contribution to journalArticleResearchpeer-review

50 Citations (Scopus)

Angiotensin ii receptors in the kidney: localization and physiological significance

Yamada, H., Sexton, P. M., Yeen Chai, S., Adam, W. R. & Mendelsohn, F. A. O., 1 Jan 1990, In : American Journal of Hypertension. 3, 3, p. 250-255 6 p.

Research output: Contribution to journalArticleResearchpeer-review

34 Citations (Scopus)
132 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

51 Citations (Scopus)

Application of photoaffinity crosslinking in determining the interaction between calcitonin and its receptor

Pham, V., Wade, J. D. & Sexton, P. M., 1 Nov 2003, In : Letters in Peptide Science. 10, 5-6, p. 447-453 7 p.

Research output: Contribution to journalArticleResearchpeer-review

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
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10 Citations (Scopus)
4 Citations (Scopus)

A structure-activity relationship study of the positive allosteric modulator LY2033298 at the M4 muscarinic acetylcholine receptor

Szabo, M., Huynh, T., Valant, C., Lane, J. R., Sexton, P. M., Christopoulos, A. & Capuano, B., 2015, In : MedChemComm. 6, 11, p. 1998-2003 6 p.

Research output: Contribution to journalArticleResearchpeer-review

5 Citations (Scopus)

Automatic local resolution-based sharpening of cryo-EM maps

Ramírez-Aportela, E., Vilas, J. L., Glukhova, A., Melero, R., Conesa, P., Martínez, M., Maluenda, D., Mota, J., Jiménez, A., Vargas, J., Marabini, R., Sexton, P. M., Carazo, J. M. & Sorzano, C. O. S., 1 Feb 2020, In : Bioinformatics. 36, 3, p. 765-772 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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6 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)

Biased agonism and biased allosteric modulation at the CB1 cannabinoid receptors

Khajehali, E., Malone, D. T., Glass, M., Sexton, P., Christopoulos, A. & Leach, K., 2015, In : Molecular Pharmacology. 88, 2, p. 368-379 12 p.

Research output: Contribution to journalArticleResearchpeer-review

74 Citations (Scopus)

Biased agonism of endogenous opioid peptides at the μ-opioid receptor

Thompson, G. L., Lane, J. R. D., Coudrat, T., Sexton, P., Christopoulos, A. & Canals, M., 2015, In : Molecular Pharmacology. 88, 2, p. 335-346 12 p.

Research output: Contribution to journalArticleResearchpeer-review

51 Citations (Scopus)

Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics

Cook, A. E., Mistry, S. N., Gregory, K. J., Furness, S. G. B., Sexton, P., Scammells, P. J., Conigrave, A., Christopoulos, A. & Leach, K., 2015, In : British Journal of Pharmacology. 172, 1, p. 185 - 200 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
44 Citations (Scopus)

Biased M1-muscarinic-receptor-mutant mice inform the design of next-generation drugs

Bradley, S. J., Molloy, C., Valuskova, P., Dwomoh, L., Scarpa, M., Rossi, M., Finlayson, L., Svensson, K. A., Chernet, E., Barth, V. N., Gherbi, K., Sykes, D. A., Wilson, C. A., Mistry, R., Sexton, P. M., Christopoulos, A., Mogg, A. J., Rosethorne, E. M., Sakata, S., John Challiss, R. A. & 2 others, Broad, L. M. & Tobin, A. B., 20 Feb 2020, In : Nature Chemical Biology. 16, 3, p. 240-249 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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1 Citation (Scopus)

Biologically active salmon calcitonin-like peptide is present in rat brain

Sexton, P. M. & Hilton, J. M., 20 Nov 1992, In : Brain Research. 596, 1-2, p. 279-284 6 p.

Research output: Contribution to journalArticleResearchpeer-review

58 Citations (Scopus)

Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes S

Bradley, S. J., Molloy, C., Bundgaard, C., Mogg, A. J., Thompson, K. J., Dwomoh, L., Sanger, H. E., Crabtree, M. D., Brooke, S. M., Sexton, P. M., Felder, C. C., Christopoulos, A., Broad, L. M., Tobin, A. B. & Langmead, C. J., 1 Jun 2018, In : Molecular Pharmacology. 93, 6, p. 645-656 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
9 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

101 Citations (Scopus)

Calcitonin

Sexton, P. M., Findlay, D. M. & Martin, T. J., 3 Nov 1999, In : Current Medicinal Chemistry. 6, 11, p. 1067-1093 27 p.

Research output: Contribution to journalArticleResearchpeer-review

162 Citations (Scopus)

Calcitonin

Findlay, D. M. & Sexton, P. M., 2004, In : Growth Factors. 22, 4, p. 217 - 224 8 p.

Research output: Contribution to journalArticleResearchpeer-review