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Cholesterol-dependent dynamic changes in the conformation of the type 1 cholecystokinin receptor affect ligand binding and G protein coupling.
Harikumar KG, Zhao P, Cary BP, Xu X, Desai AJ, Dong M, Mobbs JI, Toufaily C, Furness SGB, Christopoulos A, Belousoff MJ, Wootten D, Sexton PM, Miller LJ. Harikumar KG, et al. Among authors: furness sgb. PLoS Biol. 2024 Jul 31;22(7):e3002673. doi: 10.1371/journal.pbio.3002673. eCollection 2024 Jul. PLoS Biol. 2024. PMID: 39083706 Free PMC article.
Structures of the human cholecystokinin 1 (CCK1) receptor bound to Gs and Gq mimetic proteins provide insight into mechanisms of G protein selectivity.
Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM. Mobbs JI, et al. Among authors: furness sgb. PLoS Biol. 2021 Jun 4;19(6):e3001295. doi: 10.1371/journal.pbio.3001295. eCollection 2021 Jun. PLoS Biol. 2021. Update in: PLoS Biol. 2024 Jul 31;22(7):e3002673. doi: 10.1371/journal.pbio.3002673 PMID: 34086670 Free PMC article. Updated.
Discovery of a Positive Allosteric Modulator of Cholecystokinin Action at CCK1R in Normal and Elevated Cholesterol.
Harikumar KG, Coudrat T, Desai AJ, Dong M, Dengler DG, Furness SGB, Christopoulos A, Wootten D, Sergienko EA, Sexton PM, Miller LJ. Harikumar KG, et al. Among authors: furness sgb. Front Endocrinol (Lausanne). 2021 Dec 7;12:789957. doi: 10.3389/fendo.2021.789957. eCollection 2021. Front Endocrinol (Lausanne). 2021. PMID: 34950108 Free PMC article.
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. Wootten D, et al. Among authors: furness sgb. Cell. 2016 Jun 16;165(7):1632-1643. doi: 10.1016/j.cell.2016.05.023. Cell. 2016. PMID: 27315480 Free PMC article.
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. Wootten D, et al. Biochem Pharmacol. 2016 Oct 15;118:68-87. doi: 10.1016/j.bcp.2016.08.015. Epub 2016 Aug 26. Biochem Pharmacol. 2016. PMID: 27569426 Free PMC article.
55 results