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7,838 results
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Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor.
Biggadike K, Bledsoe RK, Coe DM, Cooper TW, House D, Iannone MA, Macdonald SJ, Madauss KP, McLay IM, Shipley TJ, Taylor SJ, Tran TB, Uings IJ, Weller V, Williams SP. Biggadike K, et al. Proc Natl Acad Sci U S A. 2009 Oct 27;106(43):18114-9. doi: 10.1073/pnas.0909125106. Epub 2009 Oct 12. Proc Natl Acad Sci U S A. 2009. PMID: 19822747 Free PMC article.
Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity.
Diallo H, Angell DC, Barnett HA, Biggadike K, Coe DM, Cooper TW, Craven A, Gray JR, House D, Jack TI, Keeling SP, Macdonald SJ, McLay IM, Oliver S, Taylor SJ, Uings IJ, Wellaway N. Diallo H, et al. Among authors: taylor sj. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1126-33. doi: 10.1016/j.bmcl.2010.12.121. Epub 2010 Dec 31. Bioorg Med Chem Lett. 2011. PMID: 21257309
Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
Demont EH, Arpino S, Bit RA, Campbell CA, Deeks N, Desai S, Dowell SJ, Gaskin P, Gray JR, Harrison LA, Haynes A, Heightman TD, Holmes DS, Humphreys PG, Kumar U, Morse MA, Osborne GJ, Panchal T, Philpott KL, Taylor S, Watson R, Willis R, Witherington J. Demont EH, et al. Among authors: taylor s. J Med Chem. 2011 Oct 13;54(19):6724-33. doi: 10.1021/jm200609t. Epub 2011 Sep 9. J Med Chem. 2011. PMID: 21838322
Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists.
Barnett HA, Coe DM, Cooper TW, Jack TI, Jones HT, Macdonald SJ, McLay IM, Rayner N, Sasse RZ, Shipley TJ, Skone PA, Somers GI, Taylor S, Uings IJ, Woolven JM, Weingarten GG. Barnett HA, et al. Among authors: taylor s. Bioorg Med Chem Lett. 2009 Jan 1;19(1):158-62. doi: 10.1016/j.bmcl.2008.10.128. Epub 2008 Nov 5. Bioorg Med Chem Lett. 2009. PMID: 19019676
Discovery of a Selective S1P1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate.
Demont EH, Andrews BI, Bit RA, Campbell CA, Cooke JW, Deeks N, Desai S, Dowell SJ, Gaskin P, Gray JR, Haynes A, Holmes DS, Kumar U, Morse MA, Osborne GJ, Panchal T, Patel B, Perboni A, Taylor S, Watson R, Witherington J, Willis R. Demont EH, et al. Among authors: taylor s. ACS Med Chem Lett. 2011 Mar 24;2(6):444-9. doi: 10.1021/ml2000214. eCollection 2011 Jun 9. ACS Med Chem Lett. 2011. PMID: 24900328 Free PMC article.
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.
Demont EH, Bailey JM, Bit RA, Brown JA, Campbell CA, Deeks N, Dowell SJ, Eldred C, Gaskin P, Gray JR, Haynes A, Hirst DJ, Holmes DS, Kumar U, Morse MA, Osborne GJ, Renaux JF, Seal GA, Smethurst CA, Taylor S, Watson R, Willis R, Witherington J. Demont EH, et al. Among authors: taylor s. J Med Chem. 2016 Feb 11;59(3):1003-20. doi: 10.1021/acs.jmedchem.5b01512. Epub 2016 Jan 22. J Med Chem. 2016. PMID: 26751273
BET bromodomain inhibitors show anti-papillomavirus activity in vitro and block CRPV wart growth in vivo.
Morse MA, Balogh KK, Brendle SA, Campbell CA, Chen MX, Furze RC, Harada IL, Holyer ID, Kumar U, Lee K, Prinjha RK, Rüdiger M, Seal JT, Taylor S, Witherington J, Christensen ND. Morse MA, et al. Among authors: taylor s. Antiviral Res. 2018 Jun;154:158-165. doi: 10.1016/j.antiviral.2018.03.012. Epub 2018 Apr 11. Antiviral Res. 2018. PMID: 29653131 Free PMC article.
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