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Items: 18

1.

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.

PMID:
29717000
2.

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.

PMID:
29653090
3.

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.

PMID:
29466332
4.

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.

5.

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.

6.

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.

PMID:
27040440
7.

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.

8.

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.

9.

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.

10.

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.

11.

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.

12.

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.

PMID:
23356279
13.

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.

14.

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.

15.

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.

16.

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.

17.

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.

18.

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 OL, Miller LJ, Summers RJ, Christopoulos A, Sexton PM.

Mol Pharmacol. 2010 Sep;78(3):456-65. doi: 10.1124/mol.110.065664. Epub 2010 Jun 14.

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