1986 …2023

Research output per year

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Research Output

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)

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)

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

22 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

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
397 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. 113, 38, p. E5675-E5684 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
40 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

501 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
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2 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

27 Citations (Scopus)

A kinetic view of GPCR allostery and biased agonism

Lane, J. R., May, L. T., Parton, R. G., Sexton, P. M. & Christopoulos, A., 18 Aug 2017, In : Nature Chemical Biology. 13, 9, p. 929-937 9 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Open Access
File
50 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

251 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

135 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

50 Citations (Scopus)

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

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

Research output: Contribution to journalReview ArticleResearchpeer-review

72 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

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

Research output: Contribution to journalArticleResearchpeer-review

18 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

77 Citations (Scopus)
92 Citations (Scopus)

Allostery and Biased Agonism at Class B G Protein-Coupled Receptors

Wootten, D., Miller, L. J., Koole, C., Christopoulos, A. & Sexton, P. M., 11 Jan 2017, In : Chemical Reviews. 117, 1, p. 111-138 28 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

37 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)

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)

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

25 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

127 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

65 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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24 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

49 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)
3 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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3 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

69 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

44 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
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41 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

56 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
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9 Citations (Scopus)