Sykes D - Search Results

1

HDL-like discs for assaying membrane proteins in drug discovery.

Fiez-Vandal C, Leder L, Freuler F, Sykes D, Charlton SJ, Siehler S, Schopfer U, Duckely M. Fiez-Vandal C, et al. Among authors: sykes d. Biophys Chem. 2012 May;165-166:56-61. doi: 10.1016/j.bpc.2012.03.005. Epub 2012 Mar 19. Biophys Chem. 2012. PMID: 22542136

2

Slow receptor dissociation is not a key factor in the duration of action of inhaled long-acting β2-adrenoceptor agonists.

Sykes DA, Charlton SJ. Sykes DA, et al. Br J Pharmacol. 2012 Apr;165(8):2672-83. doi: 10.1111/j.1476-5381.2011.01639.x. Br J Pharmacol. 2012. PMID: 21883146 Free PMC article.

3

Measuring receptor target coverage: a radioligand competition binding protocol for assessing the association and dissociation rates of unlabeled compounds.

Sykes DA, Dowling MR, Charlton SJ. Sykes DA, et al. Curr Protoc Pharmacol. 2010 Sep;Chapter 9:Unit 9.14. doi: 10.1002/0471141755.ph0914s50. Curr Protoc Pharmacol. 2010. PMID: 22294377

4

Observed drug-receptor association rates are governed by membrane affinity: the importance of establishing "micro-pharmacokinetic/pharmacodynamic relationships" at the β2-adrenoceptor.

Sykes DA, Parry C, Reilly J, Wright P, Fairhurst RA, Charlton SJ. Sykes DA, et al. Mol Pharmacol. 2014 Apr;85(4):608-17. doi: 10.1124/mol.113.090209. Epub 2014 Jan 29. Mol Pharmacol. 2014. PMID: 24476583

5

An Alternative Thiol-Reactive Dye to Analyze Ligand Interactions with the Chemokine Receptor CXCR2 Using a New Thermal Shift Assay Format.

Bergsdorf C, Fiez-Vandal C, Sykes DA, Bernet P, Aussenac S, Charlton SJ, Schopfer U, Ottl J, Duckely M. Bergsdorf C, et al. J Biomol Screen. 2016 Mar;21(3):243-51. doi: 10.1177/1087057115619597. Epub 2015 Dec 7. J Biomol Screen. 2016. PMID: 26644402

6

Long Receptor Residence Time of C26 Contributes to Super Agonist Activity at the Human β2 Adrenoceptor.

Rosethorne EM, Bradley ME, Gherbi K, Sykes DA, Sattikar A, Wright JD, Renard E, Trifilieff A, Fairhurst RA, Charlton SJ. Rosethorne EM, et al. Among authors: sykes da. Mol Pharmacol. 2016 Apr;89(4):467-75. doi: 10.1124/mol.115.101253. Epub 2016 Jan 15. Mol Pharmacol. 2016. PMID: 26772612

7

Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.

Dickson CJ, Hornak V, Velez-Vega C, McKay DJ, Reilly J, Sandham DA, Shaw D, Fairhurst RA, Charlton SJ, Sykes DA, Pearlstein RA, Duca JS. Dickson CJ, et al. Among authors: sykes da. J Med Chem. 2016 Jun 23;59(12):5780-9. doi: 10.1021/acs.jmedchem.6b00358. Epub 2016 Jun 7. J Med Chem. 2016. PMID: 27239696

8

Exploring the kinetic selectivity of drugs targeting the β₁ -adrenoceptor.

Sykes DA, Jiménez-Rosés M, Reilly J, Fairhurst RA, Charlton SJ, Veprintsev DB. Sykes DA, et al. Pharmacol Res Perspect. 2022 Aug;10(4):e00978. doi: 10.1002/prp2.978. Pharmacol Res Perspect. 2022. PMID: 35762357 Free PMC article.

9

Simulating the influence of plasma protein on measured receptor affinity in biochemical assays reveals the utility of Schild analysis for estimating compound affinity for plasma proteins.

Blakeley D, Sykes DA, Ensor P, Bertran E, Aston PJ, Charlton SJ. Blakeley D, et al. Among authors: sykes da. Br J Pharmacol. 2015 Nov;172(21):5037-49. doi: 10.1111/bph.13263. Epub 2015 Oct 22. Br J Pharmacol. 2015. PMID: 26211929 Free PMC article.

10

Exploring the mechanism of agonist efficacy: a relationship between efficacy and agonist dissociation rate at the muscarinic M3 receptor.

Sykes DA, Dowling MR, Charlton SJ. Sykes DA, et al. Mol Pharmacol. 2009 Sep;76(3):543-51. doi: 10.1124/mol.108.054452. Epub 2009 Jun 4. Mol Pharmacol. 2009. PMID: 19498041

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