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Can residence time offer a useful strategy to target agonist drugs for sustained GPCR responses?
Hothersall JD, Brown AJ, Dale I, Rawlins P. Hothersall JD, et al. Drug Discov Today. 2016 Jan;21(1):90-96. doi: 10.1016/j.drudis.2015.07.015. Epub 2015 Jul 28. Drug Discov Today. 2016. PMID: 26226643 Free article. Review.
Residues W320 and Y328 within the binding site of the μ-opioid receptor influence opiate ligand bias.
Hothersall JD, Torella R, Humphreys S, Hooley M, Brown A, McMurray G, Nickolls SA. Hothersall JD, et al. Neuropharmacology. 2017 May 15;118:46-58. doi: 10.1016/j.neuropharm.2017.03.007. Epub 2017 Mar 7. Neuropharmacology. 2017. PMID: 28283391 Free article.
Structure-Activity Relationships of the Sustained Effects of Adenosine A2A Receptor Agonists Driven by Slow Dissociation Kinetics.
Hothersall JD, Guo D, Sarda S, Sheppard RJ, Chen H, Keur W, Waring MJ, IJzerman AP, Hill SJ, Dale IL, Rawlins PB. Hothersall JD, et al. Mol Pharmacol. 2017 Jan;91(1):25-38. doi: 10.1124/mol.116.105551. Epub 2016 Nov 1. Mol Pharmacol. 2017. PMID: 27803241 Free PMC article.
Sustained wash-resistant receptor activation responses of GPR119 agonists.
Hothersall JD, Bussey CE, Brown AJ, Scott JS, Dale I, Rawlins P. Hothersall JD, et al. Eur J Pharmacol. 2015 Sep 5;762:430-42. doi: 10.1016/j.ejphar.2015.06.031. Epub 2015 Jun 20. Eur J Pharmacol. 2015. PMID: 26101059 Free article.
An efficient asymmetric synthesis of the potent beta-blocker ICI-118,551 allows the determination of enantiomer dependency on biological activity.
Baker JR, Hothersall JD, Fitzmaurice RJ, Tucknott M, Vinter A, Tinker A, Caddick S. Baker JR, et al. Among authors: Hothersall JD. Chem Commun (Camb). 2010 Jun 14;46(22):3953-4. doi: 10.1039/c0cc00142b. Epub 2010 Apr 30. Chem Commun (Camb). 2010. PMID: 20431838
5-Hydroxytryptamine (5-HT) cellular sequestration during chronic exposure delays 5-HT3 receptor resensitization due to its subsequent release.
Hothersall JD, Alexander A, Samson AJ, Moffat C, Bollan KA, Connolly CN. Hothersall JD, et al. J Biol Chem. 2014 Nov 14;289(46):32020-9. doi: 10.1074/jbc.M114.594796. Epub 2014 Oct 3. J Biol Chem. 2014. PMID: 25281748 Free PMC article.
Mupirocin H, a novel metabolite resulting from mutation of the HMG-CoA synthase analogue, mupH in Pseudomonas fluorescens.
Wu J, Cooper SM, Cox RJ, Crosby J, Crump MP, Hothersall J, Simpson TJ, Thomas CM, Willis CL. Wu J, et al. Chem Commun (Camb). 2007 May 28;(20):2040-2. doi: 10.1039/b700613f. Chem Commun (Camb). 2007. PMID: 17713071
Mupirocin W, a novel pseudomonic acid produced by targeted mutation of the mupirocin biosynthetic gene cluster.
Cooper SM, Cox RJ, Crosby J, Crump MP, Hothersall J, Laosripaiboon W, Simpson TJ, Thomas CM. Cooper SM, et al. Chem Commun (Camb). 2005 Mar 7;(9):1179-81. doi: 10.1039/b414781b. Epub 2005 Jan 17. Chem Commun (Camb). 2005. PMID: 15726184
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