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Items: 35


VEGFA From Early Osteoblast Lineage Cells (Osterix+) Is Required in Mice for Fracture Healing.

Buettmann EG, McKenzie JA, Migotsky N, Sykes DA, Hu P, Yoneda S, Silva MJ.

J Bone Miner Res. 2019 Sep;34(9):1690-1706. doi: 10.1002/jbmr.3755. Epub 2019 Aug 1.


Pharmacological Characterization of a Novel 5-Hydroxybenzothiazolone-Derived β 2-Adrenoceptor Agonist with Functional Selectivity for Anabolic Effects on Skeletal Muscle Resulting in a Wider Cardiovascular Safety Window in Preclinical Studies.

Koziczak-Holbro M, Rigel DF, Dumotier B, Sykes DA, Tsao J, Nguyen NH, Bösch J, Jourdain M, Flotte L, Adachi Y, Kiffe M, Azria M, Fairhurst RA, Charlton SJ, Richardson BP, Lach-Trifilieff E, Glass DJ, Ullrich T, Hatakeyama S.

J Pharmacol Exp Ther. 2019 May;369(2):188-199. doi: 10.1124/jpet.118.255307. Epub 2019 Feb 28.


Binding kinetics of ligands acting at GPCRs.

Sykes DA, Stoddart LA, Kilpatrick LE, Hill SJ.

Mol Cell Endocrinol. 2019 Apr 5;485:9-19. doi: 10.1016/j.mce.2019.01.018. Epub 2019 Feb 8. Review.


Reply to 'Antipsychotics with similar association kinetics at dopamine D2 receptors differ in extrapyramidal side-effects'.

Sykes DA, Lane JR, Szabo M, Capuano B, Javitch JA, Charlton SJ.

Nat Commun. 2018 Sep 3;9(1):3568. doi: 10.1038/s41467-018-05678-4. No abstract available.


Single Step Determination of Unlabeled Compound Kinetics Using a Competition Association Binding Method Employing Time-Resolved FRET.

Sykes DA, Charlton SJ.

Methods Mol Biol. 2018;1824:177-194. doi: 10.1007/978-1-4939-8630-9_10.


Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors.

Sykes DA, Moore H, Stott L, Holliday N, Javitch JA, Lane JR, Charlton SJ.

Nat Commun. 2017 Oct 2;8(1):763. doi: 10.1038/s41467-017-00716-z.


Correction to "Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma".

Sandham DA, Barker L, Brown L, Brown Z, Budd D, Charlton SJ, Chatterjee D, Cox B, Dubois G, Duggan N, Hall E, Hatto J, Leblanc C, Maas J, Manini J, Profit R, Riddy D, Ritchie C, Sohal B, Shaw D, Stringer R, Sykes DA, Thomas M, Turner KL, Watson SJ, West R, Willard E, Williams G, Willis J.

ACS Med Chem Lett. 2017 Sep 1;8(9):987. doi: 10.1021/acsmedchemlett.7b00353. eCollection 2017 Sep 14.


Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma.

Sandham DA, Barker L, Brown L, Brown Z, Budd D, Charlton SJ, Chatterjee D, Cox B, Dubois G, Duggan N, Hall E, Hatto J, Maas J, Manini J, Profit R, Riddy D, Ritchie C, Sohal B, Shaw D, Stringer R, Sykes DA, Thomas M, Turner KL, Watson SJ, West R, Willard E, Williams G, Willis J.

ACS Med Chem Lett. 2017 Apr 25;8(5):582-586. doi: 10.1021/acsmedchemlett.7b00157. eCollection 2017 May 11. Erratum in: ACS Med Chem Lett. 2017 Sep 01;8(9):987.


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.

J Med Chem. 2016 Jun 23;59(12):5780-9. doi: 10.1021/acs.jmedchem.6b00358. Epub 2016 Jun 7.


Fevipiprant (QAW039), a Slowly Dissociating CRTh2 Antagonist with the Potential for Improved Clinical Efficacy.

Sykes DA, Bradley ME, Riddy DM, Willard E, Reilly J, Miah A, Bauer C, Watson SJ, Sandham DA, Dubois G, Charlton SJ.

Mol Pharmacol. 2016 May;89(5):593-605. doi: 10.1124/mol.115.101832. Epub 2016 Feb 25.


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.

Nat Commun. 2016 Feb 24;7:10842. doi: 10.1038/ncomms10842.


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.

Mol Pharmacol. 2016 Apr;89(4):467-75. doi: 10.1124/mol.115.101253. Epub 2016 Jan 15.


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.

J Biomol Screen. 2016 Mar;21(3):243-51. doi: 10.1177/1087057115619597. Epub 2015 Dec 7.


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.

Br J Pharmacol. 2015 Nov;172(21):5037-49. doi: 10.1111/bph.13263. Epub 2015 Oct 22.


Comparing the cardiovascular therapeutic indices of glycopyrronium and tiotropium in an integrated rat pharmacokinetic, pharmacodynamic and safety model.

Trifilieff A, Ethell BT, Sykes DA, Watson KJ, Collingwood S, Charlton SJ, Kent TC.

Toxicol Appl Pharmacol. 2015 Aug 15;287(1):9-16. doi: 10.1016/j.taap.2015.05.012. Epub 2015 May 27.


Investigating the molecular mechanisms through which FTY720-P causes persistent S1P1 receptor internalization.

Sykes DA, Riddy DM, Stamp C, Bradley ME, McGuiness N, Sattikar A, Guerini D, Rodrigues I, Glaenzel A, Dowling MR, Mullershausen F, Charlton SJ.

Br J Pharmacol. 2014 Nov;171(21):4797-807. doi: 10.1111/bph.12620.


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.

Mol Pharmacol. 2014 Apr;85(4):608-17. doi: 10.1124/mol.113.090209. Epub 2014 Jan 29.


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.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6280-5. doi: 10.1016/j.bmcl.2012.07.096. Epub 2012 Aug 4.


The Influence of receptor kinetics on the onset and duration of action and the therapeutic index of NVA237 and tiotropium.

Sykes DA, Dowling MR, Leighton-Davies J, Kent TC, Fawcett L, Renard E, Trifilieff A, Charlton SJ.

J Pharmacol Exp Ther. 2012 Nov;343(2):520-8. doi: 10.1124/jpet.112.194456. Epub 2012 Aug 1.


Reassessment of the pharmacology of Sphingosine-1-phosphate S1P3 receptor ligands using the DiscoveRx PathHunter™ and Ca2+ release functional assays.

Riddy DM, Stamp C, Sykes DA, Charlton SJ, Dowling MR.

Br J Pharmacol. 2012 Oct;167(4):868-80. doi: 10.1111/j.1476-5381.2012.02032.x.


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

Sykes DA, Charlton SJ.

Br J Pharmacol. 2012 Apr;165(8):2672-83. doi: 10.1111/j.1476-5381.2011.01639.x.


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.

Curr Protoc Pharmacol. 2010 Sep;Chapter 9:Unit 9.14. doi: 10.1002/0471141755.ph0914s50.


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.

Mol Pharmacol. 2009 Sep;76(3):543-51. doi: 10.1124/mol.108.054452. Epub 2009 Jun 4.


Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists.

McDonald IM, Austin C, Buck IM, Dunstone DJ, Gaffen J, Griffin E, Harper EA, Hull RA, Kalindjian SB, Linney ID, Low CM, Patel D, Pether MJ, Raynor M, Roberts SP, Shaxted ME, Spencer J, Steel KI, Sykes DA, Wright PT, Xun W.

J Med Chem. 2007 Oct 4;50(20):4789-92. Epub 2007 Sep 12.


Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion.

McDonald IM, Black JW, Buck IM, Dunstone DJ, Griffin EP, Harper EA, Hull RA, Kalindjian SB, Lilley EJ, Linney ID, Pether MJ, Roberts SP, Shaxted ME, Spencer J, Steel KI, Sykes DA, Walker MK, Watt GF, Wright L, Wright PT, Xun W.

J Med Chem. 2007 Jun 28;50(13):3101-12. Epub 2007 May 31.


Optimization of the in vitro and in vivo properties of a novel series of 2,4,5-trisubstituted imidazoles as potent cholecystokinin-2 (CCK2) antagonists.

Buck IM, Black JW, Cooke T, Dunstone DJ, Gaffen JD, Griffin EP, Harper EA, Hull RA, Kalindjian SB, Lilley EJ, Linney ID, Low CM, McDonald IM, Pether MJ, Roberts SP, Shankley NP, Shaxted ME, Steel KI, Sykes DA, Tozer MJ, Watt GF, Walker MK, Wright L, Wright PT.

J Med Chem. 2005 Nov 3;48(22):6803-12.


Reduced renal hemodynamic response to atrial natriuretic peptide in elderly volunteers.

Mulkerrin EC, Brain A, Hampton D, Penney MD, Sykes DA, Williams JD, Coles GA, Woodhouse KW.

Am J Kidney Dis. 1993 Oct;22(4):538-44.


Correlation between Korotkoff's sounds and ultrasonics of the brachial artery in healthy and normotensive subjects.

Sykes DA, McCarty K, Mulkerrin E, Fisher DJ, Woodcock JP.

Clin Phys Physiol Meas. 1991 Nov;12(4):327-31.


Lumbar sagittal mobility and low back symptoms in patients treated with manipulation.

Burton AK, Tillotson KM, Edwards VA, Sykes DA.

J Spinal Disord. 1990 Sep;3(3):262-8.


Effect of head position on the efficacy of topical treatment of chronic mucopurulent rhinosinusitis.

Wilson R, Sykes DA, Chan KL, Cole PJ, Mackay IS.

Thorax. 1987 Aug;42(8):631-2. No abstract available.


Deleterious effects of purulent sputum sol on human ciliary function in vitro: at least two factors identified.

Sykes DA, Wilson R, Greenstone M, Currie DC, Steinfort C, Cole PJ.

Thorax. 1987 Apr;42(4):256-61.


Beat frequency of cilia from sites of purulent infection.

Wilson R, Sykes DA, Currie D, Cole PJ.

Thorax. 1986 Jun;41(6):453-8.

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