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Page 1
Discovery of HC-7366: An Orally Bioavailable and Efficacious GCN2 Kinase Activator.
Thomson CG, Aicher TD, Cheng W, Du H, Dudgeon C, Li AH, Li B, Lightcap E, Luo D, Mulvihill M, Pan P, Rahemtulla BF, Rigby AC, Sherborne B, Sood S, Surguladze D, Talbot EPA, Tameire F, Taylor S, Wang Y, Wojnarowicz P, Xiao F, Ramurthy S. Thomson CG, et al. Among authors: taylor s. J Med Chem. 2024 Apr 11;67(7):5259-5271. doi: 10.1021/acs.jmedchem.3c02384. Epub 2024 Mar 26. J Med Chem. 2024. PMID: 38530741
PERK Inhibition by HC-5404 Sensitizes Renal Cell Carcinoma Tumor Models to Antiangiogenic Tyrosine Kinase Inhibitors.
Stokes ME, Calvo V, Fujisawa S, Dudgeon C, Huang S, Ballal N, Shen L, Gasparek J, Betzenhauser M, Taylor SJ, Staschke KA, Rigby AC, Mulvihill MJ, Bose N, Lightcap ES, Surguladze D. Stokes ME, et al. Among authors: taylor sj. Clin Cancer Res. 2023 Dec 1;29(23):4870-4882. doi: 10.1158/1078-0432.CCR-23-1182. Clin Cancer Res. 2023. PMID: 37733811 Free PMC article.
Discovery of a novel series of selective macrocyclic PKCTheta inhibitors.
Crosignani S, Campos S, Bouix-Peter C, Harris C, Talbot E, Hu H, Wang S, Maclean J, Zanelli U, Taylor S, Foote K, Hacini-Rachinel F, Nicodeme E, Julia V. Crosignani S, et al. Among authors: taylor s. Bioorg Med Chem Lett. 2024 Mar 1;100:129630. doi: 10.1016/j.bmcl.2024.129630. Epub 2024 Feb 1. Bioorg Med Chem Lett. 2024. PMID: 38307441
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.
Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.
Jones KL, Beaumont DM, Bernard SG, Bit RA, Campbell SP, Chung CW, Cutler L, Demont EH, Dennis K, Gordon L, Gray JR, Haase MV, Lewis AJ, McCleary S, Mitchell DJ, Moore SM, Parr N, Robb OJ, Smithers N, Soden PE, Suckling CJ, Taylor S, Walker AL, Watson RJ, Prinjha RK. Jones KL, et al. Among authors: taylor s. J Med Chem. 2021 Aug 26;64(16):12200-12227. doi: 10.1021/acs.jmedchem.1c00855. Epub 2021 Aug 13. J Med Chem. 2021. PMID: 34387088
Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit.
Rianjongdee F, Atkinson SJ, Chung CW, Grandi P, Gray JRJ, Kaushansky LJ, Medeiros P, Messenger C, Phillipou A, Preston A, Prinjha RK, Rioja I, Satz AL, Taylor S, Wall ID, Watson RJ, Yao G, Demont EH. Rianjongdee F, et al. Among authors: taylor s. J Med Chem. 2021 Aug 12;64(15):10806-10833. doi: 10.1021/acs.jmedchem.1c00412. Epub 2021 Jul 12. J Med Chem. 2021. PMID: 34251219
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.
Wellaway CR, Bamborough P, Bernard SG, Chung CW, Craggs PD, Cutler L, Demont EH, Evans JP, Gordon L, Karamshi B, Lewis AJ, Lindon MJ, Mitchell DJ, Rioja I, Soden PE, Taylor S, Watson RJ, Willis R, Woolven JM, Wyspiańska BS, Kerr WJ, Prinjha RK. Wellaway CR, et al. Among authors: taylor s. J Med Chem. 2020 Sep 10;63(17):9020-9044. doi: 10.1021/acs.jmedchem.0c00566. Epub 2020 Aug 3. J Med Chem. 2020. PMID: 32787145 Free article.
Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.
Lucas SCC, Atkinson SJ, Chung CW, Davis R, Gordon L, Grandi P, Gray JJR, Grimes T, Phillipou A, Preston AG, Prinjha RK, Rioja I, Taylor S, Tomkinson NCO, Wall I, Watson RJ, Woolven J, Demont EH. Lucas SCC, et al. Among authors: taylor s. J Med Chem. 2021 Aug 12;64(15):10711-10741. doi: 10.1021/acs.jmedchem.1c00344. Epub 2021 Jul 14. J Med Chem. 2021. PMID: 34260229 Free article.
9,277 results