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Molecular basis of action of a small molecule positive allosteric modulator (PAM)-agonist at the type 1 cholecystokinin holoreceptor.

Desai AJ, Mechin I, Nagarajan K, Valant C, Wootten D, Lam PCH, Orry A, Abagyan R, Nair A, Sexton PM, Christopoulos A, Miller LJ.

Mol Pharmacol. 2018 Dec 27. pii: mol.118.114082. doi: 10.1124/mol.118.114082. [Epub ahead of print]


Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor.

Liang YL, Khoshouei M, Deganutti G, Glukhova A, Koole C, Peat TS, Radjainia M, Plitzko JM, Baumeister W, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Wootten D, Sexton PM.

Nature. 2018 Sep;561(7724):492-497. doi: 10.1038/s41586-018-0535-y. Epub 2018 Sep 12.


Glucagon-like peptide-1 receptor internalisation controls spatiotemporal signalling mediated by biased agonists.

Fletcher MM, Halls ML, Zhao P, Clydesdale L, Christopoulos A, Sexton PM, Wootten D.

Biochem Pharmacol. 2018 Oct;156:406-419. doi: 10.1016/j.bcp.2018.09.003. Epub 2018 Sep 7.


Differential engagement of polar networks in the glucagon-like peptide 1 receptor by endogenous variants of the glucagon-like peptide 1.

Furness SGB, Christopoulos A, Sexton PM, Wootten D.

Biochem Pharmacol. 2018 Oct;156:223-240. doi: 10.1016/j.bcp.2018.08.033. Epub 2018 Aug 25.


Mechanisms of signalling and biased agonism in G protein-coupled receptors.

Wootten D, Christopoulos A, Marti-Solano M, Babu MM, Sexton PM.

Nat Rev Mol Cell Biol. 2018 Oct;19(10):638-653. doi: 10.1038/s41580-018-0049-3. Review.


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

Draper-Joyce CJ, Khoshouei M, Thal DM, Liang YL, Nguyen ATN, Furness SGB, Venugopal H, Baltos JA, Plitzko JM, Danev R, Baumeister W, May LT, Wootten D, Sexton PM, Glukhova A, Christopoulos A.

Nature. 2018 Jun;558(7711):559-563. doi: 10.1038/s41586-018-0236-6. Epub 2018 Jun 20.


Two distinct domains of the glucagon-like peptide-1 receptor control peptide-mediated biased agonism.

Lei S, Clydesdale L, Dai A, Cai X, Feng Y, Yang D, Liang YL, Koole C, Zhao P, Coudrat T, Christopoulos A, Wang MW, Wootten D, Sexton PM.

J Biol Chem. 2018 Jun 15;293(24):9370-9387. doi: 10.1074/jbc.RA118.003278. Epub 2018 May 1.


Vascular and molecular pharmacology of the metabolically stable CGRP analogue, SAX.

Sheykhzade M, Abdolalizadeh B, Koole C, Pickering DS, Dreisig K, Johansson SE, Abboud BK, Dreier R, Berg JO, Jeppesen JL, Sexton PM, Edvinsson L, Wootten D, Sams A.

Eur J Pharmacol. 2018 Jun 15;829:85-92. doi: 10.1016/j.ejphar.2018.04.007. Epub 2018 Apr 10.


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 Apr;150:214-244. doi: 10.1016/j.bcp.2018.02.005. Epub 2018 Feb 16.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


Differential impact of amino acid substitutions on critical residues of the human glucagon-like peptide-1 receptor involved in peptide activity and small-molecule allostery.

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

J Pharmacol Exp Ther. 2015 Apr;353(1):52-63. doi: 10.1124/jpet.114.220913. Epub 2015 Jan 28.


Emerging paradigms in GPCR allostery: implications for drug discovery.

Wootten D, Christopoulos A, Sexton PM.

Nat Rev Drug Discov. 2013 Aug;12(8):630-44. doi: 10.1038/nrd4052. Review.


Molecular mechanisms underlying physiological and receptor pleiotropic effects mediated by GLP-1R activation.

Pabreja K, Mohd MA, Koole C, Wootten D, Furness SG.

Br J Pharmacol. 2014 Mar;171(5):1114-28. doi: 10.1111/bph.12313. Review.


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

Dong M, Koole C, Wootten D, Sexton PM, Miller LJ.

Br J Pharmacol. 2014 Mar;171(5):1085-101. doi: 10.1111/bph.12293. Review.


Minireview: Signal bias, allosterism, and polymorphic variation at the GLP-1R: implications for drug discovery.

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

Mol Endocrinol. 2013 Aug;27(8):1234-44. doi: 10.1210/me.2013-1116. Epub 2013 Jul 17. Review.


Structural biology: meet the B family.

Sexton PM, Wootten D.

Nature. 2013 Jul 25;499(7459):417-8. doi: 10.1038/nature12413. Epub 2013 Jul 17. No abstract available.


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

Savage EE, Wootten D, Christopoulos A, Sexton PM, Furness SG.

Biotechniques. 2013 Apr;54(4):217-21. doi: 10.2144/000114013.


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

Wootten D, Simms J, Miller LJ, Christopoulos A, Sexton PM.

Proc Natl Acad Sci U S A. 2013 Mar 26;110(13):5211-6. doi: 10.1073/pnas.1221585110. Epub 2013 Mar 11.


Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function.

Koole C, Pabreja K, Savage EE, Wootten D, Furness SG, Miller LJ, Christopoulos A, Sexton PM.

Biochem Soc Trans. 2013 Feb 1;41(1):172-9. doi: 10.1042/BST20120236. Review.


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

Wootten D, Savage EE, Willard FS, Bueno AB, Sloop KW, Christopoulos A, Sexton PM.

Mol Pharmacol. 2013 Apr;83(4):822-34. doi: 10.1124/mol.112.084525. Epub 2013 Jan 24. Erratum in: Mol Pharmacol. 2013 Jul;84(1):170.


Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery.

Harikumar KG, Wootten D, Pinon DI, Koole C, Ball AM, Furness SG, Graham B, Dong M, Christopoulos A, Miller LJ, Sexton PM.

Proc Natl Acad Sci U S A. 2012 Nov 6;109(45):18607-12. doi: 10.1073/pnas.1205227109. Epub 2012 Oct 22.


Receptor activity modifying proteins (RAMPs) interact with the VPAC2 receptor and CRF1 receptors and modulate their function.

Wootten D, Lindmark H, Kadmiel M, Willcockson H, Caron KM, Barwell J, Drmota T, Poyner DR.

Br J Pharmacol. 2013 Feb;168(4):822-34. doi: 10.1111/j.1476-5381.2012.02202.x.


Receptor activity-modifying protein-dependent impairment of calcitonin receptor splice variant Δ(1-47)hCT((a)) function.

Qi T, Dong M, Watkins HA, Wootten D, Miller LJ, Hay DL.

Br J Pharmacol. 2013 Feb;168(3):644-57. doi: 10.1111/j.1476-5381.2012.02197.x.


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

Willard FS, Wootten D, Showalter AD, Savage EE, Ficorilli J, Farb TB, Bokvist K, Alsina-Fernandez J, Furness SG, Christopoulos A, Sexton PM, Sloop KW.

Mol Pharmacol. 2012 Dec;82(6):1066-73. doi: 10.1124/mol.112.080432. Epub 2012 Aug 28.


Allosteric modulation of endogenous metabolites as an avenue for drug discovery.

Wootten D, Savage EE, Valant C, May LT, Sloop KW, Ficorilli J, Showalter AD, Willard FS, Christopoulos A, Sexton PM.

Mol Pharmacol. 2012 Aug;82(2):281-90. doi: 10.1124/mol.112.079319. Epub 2012 May 10.


RAMPs and CGRP receptors.

Barwell J, Wootten D, Simms J, Hay DL, Poyner DR.

Adv Exp Med Biol. 2012;744:13-24. doi: 10.1007/978-1-4614-2364-5_2. Review.


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, Wootten D, Simms J, Miller LJ, Christopoulos A, Sexton PM.

J Biol Chem. 2012 Feb 3;287(6):3642-58. doi: 10.1074/jbc.M111.309328. Epub 2011 Dec 6.


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

Koole C, Wootten D, Simms J, Savage EE, Miller LJ, Christopoulos A, Sexton PM.

J Biol Chem. 2012 Feb 3;287(6):3659-73. doi: 10.1074/jbc.M111.309369. Epub 2011 Dec 6.


Lifting the lid on GPCRs: the role of extracellular loops.

Wheatley M, Wootten D, Conner MT, Simms J, Kendrick R, Logan RT, Poyner DR, Barwell J.

Br J Pharmacol. 2012 Mar;165(6):1688-1703. doi: 10.1111/j.1476-5381.2011.01629.x. Review.


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

Furness SG, Wootten D, Christopoulos A, Sexton PM.

Br J Pharmacol. 2012 May;166(1):98-109. doi: 10.1111/j.1476-5381.2011.01571.x. Review.


Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation.

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

Mol Pharmacol. 2011 Sep;80(3):486-97. doi: 10.1124/mol.111.072884. Epub 2011 May 26. Erratum in: Mol Pharmacol. 2012 Jul;82(1):142.


Agonist-specific requirement for a glutamate in transmembrane helix 1 of the oxytocin receptor.

Wootten DL, Simms J, Massoura AJ, Trim JE, Wheatley M.

Mol Cell Endocrinol. 2011 Feb 10;333(1):20-7. doi: 10.1016/j.mce.2010.11.029. Epub 2010 Dec 3.


Modulation of the glucagon-like peptide-1 receptor signaling by naturally occurring and synthetic flavonoids.

Wootten D, Simms J, Koole C, Woodman OL, Summers RJ, Christopoulos A, Sexton PM.

J Pharmacol Exp Ther. 2011 Feb;336(2):540-50. doi: 10.1124/jpet.110.176362. Epub 2010 Nov 12.

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