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Page 1
RasGRPs are targets of the anti-cancer agent ingenol-3-angelate.
Song X, Lopez-Campistrous A, Sun L, Dower NA, Kedei N, Yang J, Kelsey JS, Lewin NE, Esch TE, Blumberg PM, Stone JC. Song X, et al. PLoS One. 2013 Aug 21;8(8):e72331. doi: 10.1371/journal.pone.0072331. eCollection 2013. PLoS One. 2013. PMID: 23991094 Free PMC article.
α-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists.
Tran PT, Kim HS, Ann J, Kim SE, Kim C, Hong M, Hoang VH, Ngo VT, Hong S, Cui M, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J. Tran PT, et al. Bioorg Med Chem Lett. 2015 Jun 1;25(11):2326-30. doi: 10.1016/j.bmcl.2015.04.024. Epub 2015 Apr 12. Bioorg Med Chem Lett. 2015. PMID: 25937016 Free PMC article.
The SAR analysis of TRPV1 agonists with the α-methylated B-region.
Cho Y, Kim MS, Kim HS, Ann J, Lee J, Pearce LV, Pavlyukovets VA, Morgan MA, Blumberg PM, Lee J. Cho Y, et al. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5227-31. doi: 10.1016/j.bmcl.2012.06.059. Epub 2012 Jun 23. Bioorg Med Chem Lett. 2012. PMID: 22796184 Free PMC article.
2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists.
Ryu H, Seo S, Cho SH, Kim HS, Jung A, Kang DW, Son K, Cui M, Hong SH, Sharma PK, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Schiene K, Christoph T, Frormann S, Lee J. Ryu H, et al. Bioorg Med Chem Lett. 2014 Aug 15;24(16):4039-43. doi: 10.1016/j.bmcl.2014.05.074. Epub 2014 Jun 2. Bioorg Med Chem Lett. 2014. PMID: 24948568 Free PMC article.
2-Sulfonamidopyridine C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists.
Ann J, Ki Y, Yoon S, Kim MS, Lee JU, Kim C, Lee S, Jung A, Baek J, Hong S, Choi S, Pearce LV, Esch TE, Turcios NA, Lewin NE, Ogunjirin AE, Herold BK, McCall AK, Blumberg PM, Lee J. Ann J, et al. Bioorg Med Chem. 2016 Mar 15;24(6):1231-40. doi: 10.1016/j.bmc.2016.01.051. Epub 2016 Jan 28. Bioorg Med Chem. 2016. PMID: 26860926 Free PMC article.
Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists.
Ann J, Jung A, Kim MY, Kim HM, Ryu H, Kim S, Kang DW, Hong S, Cui M, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J. Ann J, et al. Bioorg Med Chem. 2015 Nov 1;23(21):6844-54. doi: 10.1016/j.bmc.2015.10.001. Epub 2015 Oct 9. Bioorg Med Chem. 2015. PMID: 26474664 Free PMC article.
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