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Biased M1-muscarinic-receptor-mutant mice inform the design of next-generation drugs.
Bradley SJ, Molloy C, Valuskova P, Dwomoh L, Scarpa M, Rossi M, Finlayson L, Svensson KA, Chernet E, Barth VN, Gherbi K, Sykes DA, Wilson CA, Mistry R, Sexton PM, Christopoulos A, Mogg AJ, Rosethorne EM, Sakata S, John Challiss RA, Broad LM, Tobin AB. Bradley SJ, et al. Among authors: sykes da. Nat Chem Biol. 2020 Mar;16(3):240-249. doi: 10.1038/s41589-019-0453-9. Epub 2020 Feb 20. Nat Chem Biol. 2020. PMID: 32080630 Free article.
The role of kinetic context in apparent biased agonism at GPCRs.
Klein Herenbrink C, Sykes DA, Donthamsetti P, Canals M, Coudrat T, Shonberg J, Scammells PJ, Capuano B, Sexton PM, Charlton SJ, Javitch JA, Christopoulos A, Lane JR. Klein Herenbrink C, et al. Among authors: sykes da. Nat Commun. 2016 Feb 24;7:10842. doi: 10.1038/ncomms10842. Nat Commun. 2016. PMID: 26905976 Free PMC article.
An investigation into the structure-activity relationships associated with the systematic modification of the β(2)-adrenoceptor agonist indacaterol.
Beattie D, Beer D, Bradley ME, Bruce I, Charlton SJ, Cuenoud BM, Fairhurst RA, Farr D, Fozard JR, Janus D, Rosethorne EM, Sandham DA, Sykes DA, Trifilieff A, Turner KL, Wissler E. Beattie D, et al. Among authors: sykes da. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6280-5. doi: 10.1016/j.bmcl.2012.07.096. Epub 2012 Aug 4. Bioorg Med Chem Lett. 2012. PMID: 22932315
Development of High-Specificity Fluorescent Probes to Enable Cannabinoid Type 2 Receptor Studies in Living Cells.
Sarott RC, Westphal MV, Pfaff P, Korn C, Sykes DA, Gazzi T, Brennecke B, Atz K, Weise M, Mostinski Y, Hompluem P, Koers E, Miljuš T, Roth NJ, Asmelash H, Vong MC, Piovesan J, Guba W, Rufer AC, Kusznir EA, Huber S, Raposo C, Zirwes EA, Osterwald A, Pavlovic A, Moes S, Beck J, Benito-Cuesta I, Grande T, Ruiz de Martı N Esteban S, Yeliseev A, Drawnel F, Widmer G, Holzer D, van der Wel T, Mandhair H, Yuan CY, Drobyski WR, Saroz Y, Grimsey N, Honer M, Fingerle J, Gawrisch K, Romero J, Hillard CJ, Varga ZV, van der Stelt M, Pacher P, Gertsch J, McCormick PJ, Ullmer C, Oddi S, Maccarrone M, Veprintsev DB, Nazaré M, Grether U, Carreira EM. Sarott RC, et al. Among authors: sykes da. J Am Chem Soc. 2020 Oct 7;142(40):16953-16964. doi: 10.1021/jacs.0c05587. Epub 2020 Sep 29. J Am Chem Soc. 2020. PMID: 32902974
GPCR Solubilization and Quality Control.
Miljus T, Sykes DA, Harwood CR, Vuckovic Z, Veprintsev DB. Miljus T, et al. Among authors: sykes da. Methods Mol Biol. 2020;2127:105-127. doi: 10.1007/978-1-0716-0373-4_8. Methods Mol Biol. 2020. PMID: 32112318
Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe.
Gazzi T, Brennecke B, Atz K, Korn C, Sykes D, Forn-Cuni G, Pfaff P, Sarott RC, Westphal MV, Mostinski Y, Mach L, Wasinska-Kalwa M, Weise M, Hoare BL, Miljuš T, Mexi M, Roth N, Koers EJ, Guba W, Alker A, Rufer AC, Kusznir EA, Huber S, Raposo C, Zirwes EA, Osterwald A, Pavlovic A, Moes S, Beck J, Nettekoven M, Benito-Cuesta I, Grande T, Drawnel F, Widmer G, Holzer D, van der Wel T, Mandhair H, Honer M, Fingerle J, Scheffel J, Broichhagen J, Gawrisch K, Romero J, Hillard CJ, Varga ZV, van der Stelt M, Pacher P, Gertsch J, Ullmer C, McCormick PJ, Oddi S, Spaink HP, Maccarrone M, Veprintsev DB, Carreira EM, Grether U, Nazaré M. Gazzi T, et al. Chem Sci. 2022 Apr 1;13(19):5539-5545. doi: 10.1039/d1sc06659e. eCollection 2022 May 18. Chem Sci. 2022. PMID: 35694350 Free PMC article.
Binding kinetics of ligands acting at GPCRs.
Sykes DA, Stoddart LA, Kilpatrick LE, Hill SJ. Sykes DA, et al. Mol Cell Endocrinol. 2019 Apr 5;485:9-19. doi: 10.1016/j.mce.2019.01.018. Epub 2019 Feb 8. Mol Cell Endocrinol. 2019. PMID: 30738950 Free PMC article. Review.
71 results