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Page 1
Discovery of the Selective Protein Kinase C-θ Kinase Inhibitor, CC-90005.
Papa P, Whitefield B, Mortensen DS, Cashion D, Huang D, Torres E, Parnes J, Sapienza J, Hansen J, Correa M, Delgado M, Harris R, Hegde S, Norris S, Bahmanyar S, Plantevin-Krenitsky V, Liu Z, Leftheris K, Kulkarni A, Bennett B, Hur EM, Ringheim G, Khambatta G, Chan H, Muir J, Blease K, Burnett K, LeBrun L, Morrison L, Celeridad M, Khattri R, Cathers BE. Papa P, et al. Among authors: blease k. J Med Chem. 2021 Aug 26;64(16):11886-11903. doi: 10.1021/acs.jmedchem.1c00388. Epub 2021 Aug 6. J Med Chem. 2021. PMID: 34355886
Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor.
Plantevin Krenitsky V, Nadolny L, Delgado M, Ayala L, Clareen SS, Hilgraf R, Albers R, Hegde S, D'Sidocky N, Sapienza J, Wright J, McCarrick M, Bahmanyar S, Chamberlain P, Delker SL, Muir J, Giegel D, Xu L, Celeridad M, Lachowitzer J, Bennett B, Moghaddam M, Khatsenko O, Katz J, Fan R, Bai A, Tang Y, Shirley MA, Benish B, Bodine T, Blease K, Raymon H, Cathers BE, Satoh Y. Plantevin Krenitsky V, et al. Among authors: blease k. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1433-8. doi: 10.1016/j.bmcl.2011.12.027. Epub 2011 Dec 10. Bioorg Med Chem Lett. 2012. PMID: 22244937
Discovery of the c-Jun N-Terminal Kinase Inhibitor CC-90001.
Nagy MA, Hilgraf R, Mortensen DS, Elsner J, Norris S, Tikhe J, Yoon W, Paisner D, Delgado M, Erdman P, Haelewyn J, Khambatta G, Xu L, Romanow WJ, Condroski K, Bahmanyar S, McCarrick M, Benish B, Blease K, LeBrun L, Moghaddam MF, Apuy J, Canan SS, Bennett BL, Satoh Y. Nagy MA, et al. Among authors: blease k. J Med Chem. 2021 Dec 23;64(24):18193-18208. doi: 10.1021/acs.jmedchem.1c01716. Epub 2021 Dec 13. J Med Chem. 2021. PMID: 34894681
Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury.
Krenitsky VP, Delgado M, Nadolny L, Sahasrabudhe K, Ayala L, Clareen SS, Hilgraf R, Albers R, Kois A, Hughes K, Wright J, Nowakowski J, Sudbeck E, Ghosh S, Bahmanyar S, Chamberlain P, Muir J, Cathers BE, Giegel D, Xu L, Celeridad M, Moghaddam M, Khatsenko O, Omholt P, Katz J, Pai S, Fan R, Tang Y, Shirley MA, Benish B, Blease K, Raymon H, Bhagwat S, Henderson I, Cole AG, Bennett B, Satoh Y. Krenitsky VP, et al. Among authors: blease k. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1427-32. doi: 10.1016/j.bmcl.2011.12.028. Epub 2011 Dec 11. Bioorg Med Chem Lett. 2012. PMID: 22226655
A Novel Triazolopyridine-Based Spleen Tyrosine Kinase Inhibitor That Arrests Joint Inflammation.
Ferguson GD, Delgado M, Plantevin-Krenitsky V, Jensen-Pergakes K, Bates RJ, Torres S, Celeridad M, Brown H, Burnett K, Nadolny L, Tehrani L, Packard G, Pagarigan B, Haelewyn J, Nguyen T, Xu L, Tang Y, Hickman M, Baculi F, Pierce S, Miyazawa K, Jackson P, Chamberlain P, LeBrun L, Xie W, Bennett B, Blease K. Ferguson GD, et al. Among authors: blease k. PLoS One. 2016 Jan 12;11(1):e0145705. doi: 10.1371/journal.pone.0145705. eCollection 2016. PLoS One. 2016. PMID: 26756335 Free PMC article.
Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor.
Man HW, Schafer P, Wong LM, Patterson RT, Corral LG, Raymon H, Blease K, Leisten J, Shirley MA, Tang Y, Babusis DM, Chen R, Stirling D, Muller GW. Man HW, et al. Among authors: blease k. J Med Chem. 2009 Mar 26;52(6):1522-4. doi: 10.1021/jm900210d. J Med Chem. 2009. PMID: 19256507
Targeting the Wnt signaling pathway through R-spondin 3 identifies an anti-fibrosis treatment strategy for multiple organs.
Zhang M, Haughey M, Wang NY, Blease K, Kapoun AM, Couto S, Belka I, Hoey T, Groza M, Hartke J, Bennett B, Cain J, Gurney A, Benish B, Castiglioni P, Drew C, Lachowicz J, Carayannopoulos L, Nathan SD, Distler J, Brenner DA, Hariharan K, Cho H, Xie W. Zhang M, et al. Among authors: blease k. PLoS One. 2020 Mar 11;15(3):e0229445. doi: 10.1371/journal.pone.0229445. eCollection 2020. PLoS One. 2020. PMID: 32160239 Free PMC article.
47 results