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Recent advances in the determination of G protein-coupled receptor structures.

Thal DM, Vuckovic Z, Draper-Joyce CJ, Liang YL, Glukhova A, Christopoulos A, Sexton PM.

Curr Opin Struct Biol. 2018 Mar 13;51:28-34. doi: 10.1016/ [Epub ahead of print] Review.


Muscarinic M5 receptors modulate ethanol seeking in rats.

Berizzi AE, Perry CJ, Shackleford DM, Lindsley CW, Jones CK, Chen NA, Sexton PM, Christopoulos A, Langmead CJ, Lawrence AJ.

Neuropsychopharmacology. 2018 Feb 5. doi: 10.1038/s41386-017-0007-3. [Epub ahead of print]


Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor-Gs complex.

Liang YL, Khoshouei M, Glukhova A, Furness SGB, Zhao P, Clydesdale L, Koole C, Truong TT, Thal DM, Lei S, Radjainia M, Danev R, Baumeister W, Wang MW, Miller LJ, Christopoulos A, Sexton PM, Wootten D.

Nature. 2018 Mar 1;555(7694):121-125. doi: 10.1038/nature25773. Epub 2018 Feb 21.


Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy.

Dal Maso E, Zhu Y, Pham V, Reynolds CA, Deganutti G, Hick CA, Yang D, Christopoulos A, Hay DL, Wang MW, Sexton PM, Furness SGB, Wootten D.

Biochem Pharmacol. 2018 Feb 16;150:214-244. doi: 10.1016/j.bcp.2018.02.005. [Epub ahead of print]


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

Korczynska M, Clark MJ, Valant C, Xu J, Moo EV, Albold S, Weiss DR, Torosyan H, Huang W, Kruse AC, Lyda BR, May LT, Baltos JA, Sexton PM, Kobilka BK, Christopoulos A, Shoichet BK, Sunahara RK.

Proc Natl Acad Sci U S A. 2018 Mar 6;115(10):E2419-E2428. doi: 10.1073/pnas.1718037115. Epub 2018 Feb 16.


To Bind or Not to Bind: Unravelling GPCR Polypharmacology.

Sexton PM, Christopoulos A.

Cell. 2018 Feb 8;172(4):636-638. doi: 10.1016/j.cell.2018.01.018.


Correspondence: Reply to 'Compound 17b and formyl peptide receptor biased agonism in relation to cardioprotective effects in ischaemia-reperfusion injury'.

Qin CX, May LT, Sexton PM, DeBono AJ, Baell JB, Christopoulos A, Ritchie RH.

Nat Commun. 2018 Feb 7;9(1):530. doi: 10.1038/s41467-017-02656-0. No abstract available.


Characterization of signalling and regulation of common calcitonin receptor splice variants and polymorphisms.

Dal Maso E, Just R, Hick C, Christopoulos A, Sexton PM, Wootten D, Furness SGB.

Biochem Pharmacol. 2018 Feb;148:111-129. doi: 10.1016/j.bcp.2017.12.016. Epub 2017 Dec 23.


G Protein-Coupled Receptors Targeting Insulin Resistance, Obesity, and Type 2 Diabetes Mellitus.

Riddy DM, Delerive P, Summers RJ, Sexton PM, Langmead CJ.

Pharmacol Rev. 2018 Jan;70(1):39-67. doi: 10.1124/pr.117.014373. Review.


Improving virtual screening of G protein-coupled receptors via ligand-directed modeling.

Coudrat T, Simms J, Christopoulos A, Wootten D, Sexton PM.

PLoS Comput Biol. 2017 Nov 13;13(11):e1005819. doi: 10.1371/journal.pcbi.1005819. eCollection 2017 Nov.


A kinetic view of GPCR allostery and biased agonism.

Lane JR, May LT, Parton RG, Sexton PM, Christopoulos A.

Nat Chem Biol. 2017 Aug 18;13(9):929-937. doi: 10.1038/nchembio.2431.


Coding GPCR-G protein specificity.

Furness SG, Sexton PM.

Cell Res. 2017 Oct;27(10):1193-1194. doi: 10.1038/cr.2017.92. Epub 2017 Jul 11.


Phase-plate cryo-EM structure of a class B GPCR-G-protein complex.

Liang YL, Khoshouei M, Radjainia M, Zhang Y, Glukhova A, Tarrasch J, Thal DM, Furness SGB, Christopoulos G, Coudrat T, Danev R, Baumeister W, Miller LJ, Christopoulos A, Kobilka BK, Wootten D, Skiniotis G, Sexton PM.

Nature. 2017 Jun 1;546(7656):118-123. doi: 10.1038/nature22327. Epub 2017 Apr 24.


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

Coudrat T, Christopoulos A, Sexton PM, Wootten D.

PLoS One. 2017 Apr 5;12(4):e0174719. doi: 10.1371/journal.pone.0174719. eCollection 2017.


Coexpressed Class B G Protein-Coupled Secretin and GLP-1 Receptors Self- and Cross-Associate: Impact on Pancreatic Islets.

Harikumar KG, Lau S, Sexton PM, Wootten D, Miller LJ.

Endocrinology. 2017 Jun 1;158(6):1685-1700. doi: 10.1210/en.2017-00023.


Characterization of signal bias at the GLP-1 receptor induced by backbone modification of GLP-1.

Hager MV, Clydesdale L, Gellman SH, Sexton PM, Wootten D.

Biochem Pharmacol. 2017 Jul 15;136:99-108. doi: 10.1016/j.bcp.2017.03.018. Epub 2017 Mar 29.


Genetically encoded photocross-linkers determine the biological binding site of exendin-4 peptide in the N-terminal domain of the intact human glucagon-like peptide-1 receptor (GLP-1R).

Koole C, Reynolds CA, Mobarec JC, Hick C, Sexton PM, Sakmar TP.

J Biol Chem. 2017 Apr 28;292(17):7131-7144. doi: 10.1074/jbc.M117.779496. Epub 2017 Mar 10.


Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity.

Glukhova A, Thal DM, Nguyen AT, Vecchio EA, Jörg M, Scammells PJ, May LT, Sexton PM, Christopoulos A.

Cell. 2017 Feb 23;168(5):867-877.e13. doi: 10.1016/j.cell.2017.01.042.


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

Qin CX, May LT, Li R, Cao N, Rosli S, Deo M, Alexander AE, Horlock D, Bourke JE, Yang YH, Stewart AG, Kaye DM, Du XJ, Sexton PM, Christopoulos A, Gao XM, Ritchie RH.

Nat Commun. 2017 Feb 7;8:14232. doi: 10.1038/ncomms14232.


What determines the magnitude of cellular response for activation of G protein-coupled receptors?

Furness SG, Wootten D, Sexton PM.

Cell Cycle. 2017 Mar 4;16(5):392-394. doi: 10.1080/15384101.2016.1271634. Epub 2017 Jan 5. No abstract available.


M1 muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss.

Bradley SJ, Bourgognon JM, Sanger HE, Verity N, Mogg AJ, White DJ, Butcher AJ, Moreno JA, Molloy C, Macedo-Hatch T, Edwards JM, Wess J, Pawlak R, Read DJ, Sexton PM, Broad LM, Steinert JR, Mallucci GR, Christopoulos A, Felder CC, Tobin AB.

J Clin Invest. 2017 Feb 1;127(2):487-499. doi: 10.1172/JCI87526. Epub 2016 Dec 19.


High throughput, quantitative analysis of human osteoclast differentiation and activity.

Diepenhorst NA, Nowell CJ, Rueda P, Henriksen K, Pierce T, Cook AE, Pastoureau P, Sabatini M, Charman WN, Christopoulos A, Summers RJ, Sexton PM, Langmead CJ.

Anal Biochem. 2017 Feb 15;519:51-56. doi: 10.1016/j.ab.2016.12.010. Epub 2016 Dec 14.


Novel Irreversible Agonists Acting at the A1 Adenosine Receptor.

Jörg M, Glukhova A, Abdul-Ridha A, Vecchio EA, Nguyen AT, Sexton PM, White PJ, May LT, Christopoulos A, Scammells PJ.

J Med Chem. 2016 Dec 22;59(24):11182-11194. doi: 10.1021/acs.jmedchem.6b01561. Epub 2016 Dec 13.


Monotreme glucagon-like peptide-1 in venom and gut: one gene - two very different functions.

Tsend-Ayush E, He C, Myers MA, Andrikopoulos S, Wong N, Sexton PM, Wootten D, Forbes BE, Grutzner F.

Sci Rep. 2016 Nov 29;6:37744. doi: 10.1038/srep37744.


Isoform-Specific Biased Agonism of Histamine H3 Receptor Agonists.

Riddy DM, Cook AE, Diepenhorst NA, Bosnyak S, Brady R, Mannoury la Cour C, Mocaer E, Summers RJ, Charman WN, Sexton PM, Christopoulos A, Langmead CJ.

Mol Pharmacol. 2017 Feb;91(2):87-99. doi: 10.1124/mol.116.106153. Epub 2016 Nov 18. Erratum in: Mol Pharmacol. 2017 Mar;91(3):263.


β-Arrestin-Biased Agonists of the GLP-1 Receptor from β-Amino Acid Residue Incorporation into GLP-1 Analogues.

Hager MV, Johnson LM, Wootten D, Sexton PM, Gellman SH.

J Am Chem Soc. 2016 Nov 16;138(45):14970-14979. Epub 2016 Nov 4.


Extracellular Loop 2 of the Adenosine A1 Receptor Has a Key Role in Orthosteric Ligand Affinity and Agonist Efficacy.

Nguyen AT, Baltos JA, Thomas T, Nguyen TD, Muñoz LL, Gregory KJ, White PJ, Sexton PM, Christopoulos A, May LT.

Mol Pharmacol. 2016 Dec;90(6):703-714. Epub 2016 Sep 28.


Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity.

Nguyen AT, Vecchio EA, Thomas T, Nguyen TD, Aurelio L, Scammells PJ, White PJ, Sexton PM, Gregory KJ, May LT, Christopoulos A.

Mol Pharmacol. 2016 Dec;90(6):715-725. Epub 2016 Sep 28.


Ligand-Dependent Modulation of G Protein Conformation Alters Drug Efficacy.

Furness SGB, Liang YL, Nowell CJ, Halls ML, Wookey PJ, Dal Maso E, Inoue A, Christopoulos A, Wootten D, Sexton PM.

Cell. 2016 Oct 20;167(3):739-749.e11. doi: 10.1016/j.cell.2016.09.021. Epub 2016 Oct 6.


Positive Allosteric Modulation of the Muscarinic M1 Receptor Improves Efficacy of Antipsychotics in Mouse Glutamatergic Deficit Models of Behavior.

Choy KH, Shackleford DM, Malone DT, Mistry SN, Patil RT, Scammells PJ, Langmead CJ, Pantelis C, Sexton PM, Lane JR, Christopoulos A.

J Pharmacol Exp Ther. 2016 Nov;359(2):354-365. Epub 2016 Sep 14.


Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes.

Graaf Cd, Donnelly D, Wootten D, Lau J, Sexton PM, Miller LJ, Ahn JM, Liao J, Fletcher MM, Yang D, Brown AJ, Zhou C, Deng J, Wang MW.

Pharmacol Rev. 2016 Oct;68(4):954-1013. doi: 10.1124/pr.115.011395. Review.


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

Miao Y, Goldfeld DA, Moo EV, Sexton PM, Christopoulos A, McCammon JA, Valant C.

Proc Natl Acad Sci U S A. 2016 Sep 20;113(38):E5675-84. doi: 10.1073/pnas.1612353113. Epub 2016 Sep 6.


Key interactions by conserved polar amino acids located at the transmembrane helical boundaries in Class B GPCRs modulate activation, effector specificity and biased signalling in the glucagon-like peptide-1 receptor.

Wootten D, Reynolds CA, Smith KJ, Mobarec JC, Furness SG, Miller LJ, Christopoulos A, Sexton PM.

Biochem Pharmacol. 2016 Oct 15;118:68-87. doi: 10.1016/j.bcp.2016.08.015. Epub 2016 Aug 26.


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

Gingell JJ, Simms J, Barwell J, Poyner DR, Watkins HA, Pioszak AA, Sexton PM, Hay DL.

Cell Discov. 2016 Jun 21;2:16020. doi: 10.1038/celldisc.2016.20. eCollection 2016.


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

J Gingell J, Simms J, Barwell J, Poyner DR, Watkins HA, Pioszak AA, Sexton PM, Hay DL.

Cell Discov. 2016 May 17;2:16012. doi: 10.1038/celldisc.2016.12. eCollection 2016. Erratum in: Cell Discov. 2016;2:16020.


Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators.

Berizzi AE, Gentry PR, Rueda P, Den Hoedt S, Sexton PM, Langmead CJ, Christopoulos A.

Mol Pharmacol. 2016 Oct;90(4):427-36. doi: 10.1124/mol.116.104182. Epub 2016 Jul 26.


The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism.

Wootten D, Reynolds CA, Smith KJ, Mobarec JC, Koole C, Savage EE, Pabreja K, Simms J, Sridhar R, Furness SGB, Liu M, Thompson PE, Miller LJ, Christopoulos A, Sexton PM.

Cell. 2016 Jun 16;165(7):1632-1643. doi: 10.1016/j.cell.2016.05.023.


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

Thompson GL, Lane JR, Coudrat T, Sexton PM, Christopoulos A, Canals M.

Biochem Pharmacol. 2016 Aug 1;113:70-87. doi: 10.1016/j.bcp.2016.05.014. Epub 2016 Jun 7.


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

Fletcher MM, Halls ML, Christopoulos A, Sexton PM, Wootten D.

Biochem Soc Trans. 2016 Apr 15;44(2):582-8. doi: 10.1042/BST20150244. Review.


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

Wootten D, Miller LJ, Koole C, Christopoulos A, Sexton PM.

Chem Rev. 2017 Jan 11;117(1):111-138. doi: 10.1021/acs.chemrev.6b00049. Epub 2016 Apr 4. Review.


Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor.

Leach K, Gregory KJ, Kufareva I, Khajehali E, Cook AE, Abagyan R, Conigrave AD, Sexton PM, Christopoulos A.

Cell Res. 2016 May;26(5):574-92. doi: 10.1038/cr.2016.36. Epub 2016 Mar 22.


Prediction of Loops in G Protein-Coupled Receptor Homology Models: Effect of Imprecise Surroundings and Constraints.

Arora B, Coudrat T, Wootten D, Christopoulos A, Noronha SB, Sexton PM.

J Chem Inf Model. 2016 Apr 25;56(4):671-86. doi: 10.1021/acs.jcim.5b00554. Epub 2016 Apr 1.


Crystal structures of the M1 and M4 muscarinic acetylcholine receptors.

Thal DM, Sun B, Feng D, Nawaratne V, Leach K, Felder CC, Bures MG, Evans DA, Weis WI, Bachhawat P, Kobilka TS, Sexton PM, Kobilka BK, Christopoulos A.

Nature. 2016 Mar 17;531(7594):335-40. doi: 10.1038/nature17188. Epub 2016 Mar 9.


The role of kinetic context in apparent biased agonism at GPCRs.

Klein Herenbrink C, Sykes DA, Donthamsetti P, Canals M, Coudrat T, Shonberg J, Scammells PJ, Capuano B, Sexton PM, Charlton SJ, Javitch JA, Christopoulos A, Lane JR.

Nat Commun. 2016 Feb 24;7:10842. doi: 10.1038/ncomms10842.


Murine GPRC6A Mediates Cellular Responses to L-Amino Acids, but Not Osteocalcin Variants.

Rueda P, Harley E, Lu Y, Stewart GD, Fabb S, Diepenhorst N, Cremers B, Rouillon MH, Wehrle I, Geant A, Lamarche G, Leach K, Charman WN, Christopoulos A, Summers RJ, Sexton PM, Langmead CJ.

PLoS One. 2016 Jan 19;11(1):e0146846. doi: 10.1371/journal.pone.0146846. eCollection 2016.


Use of Cysteine Trapping to Map Spatial Approximations between Residues Contributing to the Helix N-capping Motif of Secretin and Distinct Residues within Each of the Extracellular Loops of Its Receptor.

Dong M, Lam PC, Orry A, Sexton PM, Christopoulos A, Abagyan R, Miller LJ.

J Biol Chem. 2016 Mar 4;291(10):5172-84. doi: 10.1074/jbc.M115.706010. Epub 2016 Jan 6.


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 Structures.

Wootten D, Reynolds CA, Koole C, Smith KJ, Mobarec JC, Simms J, Quon T, Coudrat T, Furness SG, Miller LJ, Christopoulos A, Sexton PM.

Mol Pharmacol. 2016 Mar;89(3):335-47. doi: 10.1124/mol.115.101246. Epub 2015 Dec 23.


Molecular Mechanism of Action of Triazolobenzodiazepinone Agonists of the Type 1 Cholecystokinin Receptor. Possible Cooperativity across the Receptor Homodimeric Complex.

Desai AJ, Lam PC, Orry A, Abagyan R, Christopoulos A, Sexton PM, Miller LJ.

J Med Chem. 2015 Dec 24;58(24):9562-77. doi: 10.1021/acs.jmedchem.5b01110. Epub 2015 Dec 10.


4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.

Mistry SN, Jörg M, Lim H, Vinh NB, Sexton PM, Capuano B, Christopoulos A, Lane JR, Scammells PJ.

J Med Chem. 2016 Jan 14;59(1):388-409. doi: 10.1021/acs.jmedchem.5b01562. Epub 2015 Dec 31.


Quantification of adenosine A(1) receptor biased agonism: Implications for drug discovery.

Baltos JA, Gregory KJ, White PJ, Sexton PM, Christopoulos A, May LT.

Biochem Pharmacol. 2016 Jan 1;99:101-12. doi: 10.1016/j.bcp.2015.11.013. Epub 2015 Nov 12.


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