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Page 1
Discovery of highly potent and selective small molecule ADAMTS-5 inhibitors that inhibit human cartilage degradation via encoded library technology (ELT).
Deng H, O'Keefe H, Davie CP, Lind KE, Acharya RA, Franklin GJ, Larkin J, Matico R, Neeb M, Thompson MM, Lohr T, Gross JW, Centrella PA, O'Donovan GK, Bedard KL, van Vloten K, Mataruse S, Skinner SR, Belyanskaya SL, Carpenter TY, Shearer TW, Clark MA, Cuozzo JW, Arico-Muendel CC, Morgan BA. Deng H, et al. Among authors: neeb m. J Med Chem. 2012 Aug 23;55(16):7061-79. doi: 10.1021/jm300449x. Epub 2012 Aug 14. J Med Chem. 2012. PMID: 22891645
Development of potent and selective small-molecule human Urotensin-II antagonists.
McAtee JJ, Dodson JW, Dowdell SE, Girard GR, Goodman KB, Hilfiker MA, Sehon CA, Sha D, Wang GZ, Wang N, Viet AQ, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Yuan CC, Douglas SA, Neeb MJ. McAtee JJ, et al. Bioorg Med Chem Lett. 2008 Jun 15;18(12):3500-3. doi: 10.1016/j.bmcl.2008.05.027. Epub 2008 May 10. Bioorg Med Chem Lett. 2008. PMID: 18502123
Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.
McAtee JJ, Dodson JW, Dowdell SE, Erhard K, Girard GR, Goodman KB, Hilfiker MA, Jin J, Sehon CA, Sha D, Shi D, Wang F, Wang GZ, Wang N, Wang Y, Viet AQ, Yuan CC, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Douglas SA, Neeb MJ. McAtee JJ, et al. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3716-9. doi: 10.1016/j.bmcl.2008.05.058. Epub 2008 May 20. Bioorg Med Chem Lett. 2008. PMID: 18524591
Aminomethylpiperazines as selective urotensin antagonists.
Hilfiker MA, Zhang D, Dowdell SE, Goodman KB, McAtee JJ, Dodson JW, Viet AQ, Wang GZ, Sehon CA, Behm DJ, Wu Z, Carballo LH, Douglas SA, Neeb MJ. Hilfiker MA, et al. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4470-3. doi: 10.1016/j.bmcl.2008.07.067. Epub 2008 Jul 20. Bioorg Med Chem Lett. 2008. PMID: 18674898
2-Aminomethyl piperidines as novel urotensin-II receptor antagonists.
Jin J, Wang Y, Wang F, Shi D, Erhard KF, Wu Z, Guida BF, Lawrence SK, Behm DJ, Disa J, Vaidya KS, Evans C, McMillan LJ, Rivero RA, Neeb MJ, Douglas SA. Jin J, et al. Bioorg Med Chem Lett. 2008 May 1;18(9):2860-4. doi: 10.1016/j.bmcl.2008.03.078. Epub 2008 Apr 8. Bioorg Med Chem Lett. 2008. PMID: 18420409
GSK1562590, a slowly dissociating urotensin-II receptor antagonist, exhibits prolonged pharmacodynamic activity ex vivo.
Behm DJ, Aiyar NV, Olzinski AR, McAtee JJ, Hilfiker MA, Dodson JW, Dowdell SE, Wang GZ, Goodman KB, Sehon CA, Harpel MR, Willette RN, Neeb MJ, Leach CA, Douglas SA. Behm DJ, et al. Among authors: neeb mj. Br J Pharmacol. 2010 Sep;161(1):207-28. doi: 10.1111/j.1476-5381.2010.00889.x. Br J Pharmacol. 2010. PMID: 20718751 Free PMC article.
Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues.
Behm DJ, McAtee JJ, Dodson JW, Neeb MJ, Fries HE, Evans CA, Hernandez RR, Hoffman KD, Harrison SM, Lai JM, Wu C, Aiyar NV, Ohlstein EH, Douglas SA. Behm DJ, et al. Among authors: neeb mj. Br J Pharmacol. 2008 Oct;155(3):374-86. doi: 10.1038/bjp.2008.266. Epub 2008 Jun 30. Br J Pharmacol. 2008. PMID: 18587423 Free PMC article.
56 results