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Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor.
Burford NT, Livingston KE, Canals M, Ryan MR, Budenholzer LM, Han Y, Shang Y, Herbst JJ, O'Connell J, Banks M, Zhang L, Filizola M, Bassoni DL, Wehrman TS, Christopoulos A, Traynor JR, Gerritz SW, Alt A. Burford NT, et al. Among authors: christopoulos a. J Med Chem. 2015 May 28;58(10):4220-9. doi: 10.1021/acs.jmedchem.5b00007. Epub 2015 May 7. J Med Chem. 2015. PMID: 25901762 Free PMC article.
Allostery in GPCRs: 'MWC' revisited.
Canals M, Sexton PM, Christopoulos A. Canals M, et al. Among authors: christopoulos a. Trends Biochem Sci. 2011 Dec;36(12):663-72. doi: 10.1016/j.tibs.2011.08.005. Epub 2011 Sep 14. Trends Biochem Sci. 2011. PMID: 21920759 Review.
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. Among authors: christopoulos a. 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.
In our accompanying article (Koole, C., Wootten, D., Simms, J., Miller, L. J., Christopoulos, A., and Sexton, P. M. (2012) J. Biol. Chem. 287, 3642-3658), we demonstrate, through alanine-scanning mutagenesis, a key role for extracellular loop (ECL) 2 of the r …
In our accompanying article (Koole, C., Wootten, D., Simms, J., Miller, L. J., Christopoulos, A., and Sexton, P. M. (2012) J. …
433 results