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Page 1
Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate.
Humphreys PG, Atkinson SJ, Bamborough P, Bit RA, Chung CW, Craggs PD, Cutler L, Davis R, Ferrie A, Gong G, Gordon LJ, Gray M, Harrison LA, Hayhow TG, Haynes A, Henley N, Hirst DJ, Holyer ID, Lindon MJ, Lovatt C, Lugo D, McCleary S, Molnar J, Osmani Q, Patten C, Preston A, Rioja I, Seal JT, Smithers N, Sun F, Tang D, Taylor S, Theodoulou NH, Thomas C, Watson RJ, Wellaway CR, Zhu L, Tomkinson NCO, Prinjha RK. Humphreys PG, et al. Among authors: taylor s. J Med Chem. 2022 Feb 10;65(3):2262-2287. doi: 10.1021/acs.jmedchem.1c01747. Epub 2022 Jan 7. J Med Chem. 2022. PMID: 34995458 Free 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
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.
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
Gosmini R, Nguyen VL, Toum J, Simon C, Brusq JM, Krysa G, Mirguet O, Riou-Eymard AM, Boursier EV, Trottet L, Bamborough P, Clark H, Chung CW, Cutler L, Demont EH, Kaur R, Lewis AJ, Schilling MB, Soden PE, Taylor S, Walker AL, Walker MD, Prinjha RK, Nicodème E. Gosmini R, et al. Among authors: taylor s. J Med Chem. 2014 Oct 9;57(19):8111-31. doi: 10.1021/jm5010539. Epub 2014 Sep 24. J Med Chem. 2014. PMID: 25249180
Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.
Skidmore J, Heer J, Johnson CN, Norton D, Redshaw S, Sweeting J, Hurst D, Cridland A, Vesey D, Wall I, Ahmed M, Rivers D, Myatt J, Giblin G, Philpott K, Kumar U, Stevens A, Bit RA, Haynes A, Taylor S, Watson R, Witherington J, Demont E, Heightman TD. Skidmore J, et al. Among authors: taylor s. J Med Chem. 2014 Dec 26;57(24):10424-42. doi: 10.1021/jm5010336. Epub 2014 Dec 15. J Med Chem. 2014. PMID: 25431977
Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.
Picaud S, Fedorov O, Thanasopoulou A, Leonards K, Jones K, Meier J, Olzscha H, Monteiro O, Martin S, Philpott M, Tumber A, Filippakopoulos P, Yapp C, Wells C, Che KH, Bannister A, Robson S, Kumar U, Parr N, Lee K, Lugo D, Jeffrey P, Taylor S, Vecellio ML, Bountra C, Brennan PE, O'Mahony A, Velichko S, Müller S, Hay D, Daniels DL, Urh M, La Thangue NB, Kouzarides T, Prinjha R, Schwaller J, Knapp S. Picaud S, et al. Among authors: taylor s. Cancer Res. 2015 Dec 1;75(23):5106-5119. doi: 10.1158/0008-5472.CAN-15-0236. Epub 2015 Nov 9. Cancer Res. 2015. PMID: 26552700 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.
9,250 results