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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. Wootten D, et al. Among authors: koole c. Mol Pharmacol. 2016 Mar;89(3):335-47. doi: 10.1124/mol.115.101246. Epub 2015 Dec 23. Mol Pharmacol. 2016. PMID: 26700562 Free PMC article.
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. Koole C, et al. Mol Pharmacol. 2010 Sep;78(3):456-65. doi: 10.1124/mol.110.065664. Epub 2010 Jun 14. Mol Pharmacol. 2010. PMID: 20547734 Free PMC article.
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. Koole C, et al. J Biol Chem. 2012 Feb 3;287(6):3659-73. doi: 10.1074/jbc.M111.309369. Epub 2011 Dec 6. J Biol Chem. 2012. PMID: 22147709 Free PMC article.
The glucagon-like peptide-1 receptor (GLP-1R) is a prototypical family B G protein-coupled receptor that exhibits physiologically important pleiotropic coupling and ligand-dependent signal bias. In our accompanying article (Koole, C., Wootten, D., Simms, J., Miller, …
The glucagon-like peptide-1 receptor (GLP-1R) is a prototypical family B G protein-coupled receptor that exhibits physiologically important …
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. Harikumar KG, et al. Among authors: koole c. Proc Natl Acad Sci U S A. 2012 Nov 6;109(45):18607-12. doi: 10.1073/pnas.1205227109. Epub 2012 Oct 22. Proc Natl Acad Sci U S A. 2012. PMID: 23091034 Free PMC article.
24 results