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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.
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 …
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.
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. Liang YL, et al. Among authors: koole c. Nature. 2018 Mar 1;555(7694):121-125. doi: 10.1038/nature25773. Epub 2018 Feb 21. Nature. 2018. PMID: 29466332
24 results