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CC-90009: A Cereblon E3 Ligase Modulating Drug That Promotes Selective Degradation of GSPT1 for the Treatment of Acute Myeloid Leukemia.
Hansen JD, Correa M, Alexander M, Nagy M, Huang D, Sapienza J, Lu G, LeBrun LA, Cathers BE, Zhang W, Tang Y, Ammirante M, Narla RK, Piccotti JR, Pourdehnad M, Lopez-Girona A. Hansen JD, et al. Among authors: sapienza j. J Med Chem. 2021 Feb 25;64(4):1835-1843. doi: 10.1021/acs.jmedchem.0c01489. Epub 2021 Feb 16. J Med Chem. 2021. PMID: 33591756
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
Mortensen DS, Perrin-Ninkovic SM, Shevlin G, Zhao J, Packard G, Bahmanyar S, Correa M, Elsner J, Harris R, Lee BG, Papa P, Parnes JS, Riggs JR, Sapienza J, Tehrani L, Whitefield B, Apuy J, Bisonette RR, Gamez JC, Hickman M, Khambatta G, Leisten J, Peng SX, Richardson SJ, Cathers BE, Canan SS, Moghaddam MF, Raymon HK, Worland P, Narla RK, Fultz KE, Sankar S. Mortensen DS, et al. Among authors: sapienza j. J Med Chem. 2015 Jul 9;58(13):5323-33. doi: 10.1021/acs.jmedchem.5b00626. Epub 2015 Jun 26. J Med Chem. 2015. PMID: 26083478
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: sapienza j. 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
Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115.
Mortensen DS, Perrin-Ninkovic SM, Shevlin G, Elsner J, Zhao J, Whitefield B, Tehrani L, Sapienza J, Riggs JR, Parnes JS, Papa P, Packard G, Lee BG, Harris R, Correa M, Bahmanyar S, Richardson SJ, Peng SX, Leisten J, Khambatta G, Hickman M, Gamez JC, Bisonette RR, Apuy J, Cathers BE, Canan SS, Moghaddam MF, Raymon HK, Worland P, Narla RK, Fultz KE, Sankar S. Mortensen DS, et al. Among authors: sapienza j. J Med Chem. 2015 Jul 23;58(14):5599-608. doi: 10.1021/acs.jmedchem.5b00627. Epub 2015 Jul 8. J Med Chem. 2015. PMID: 26102506
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: sapienza j. 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
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
Mortensen DS, Sapienza J, Lee BG, Perrin-Ninkovic SM, Harris R, Shevlin G, Parnes JS, Whitefield B, Hickman M, Khambatta G, Bisonette RR, Peng S, Gamez JC, Leisten J, Narla RK, Fultz KE, Sankar S. Mortensen DS, et al. Among authors: sapienza j. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1588-91. doi: 10.1016/j.bmcl.2013.01.110. Epub 2013 Jan 30. Bioorg Med Chem Lett. 2013. PMID: 23414803
Lead identification of a potent benzopyranone selective estrogen receptor modulator.
McKie JA, Bhagwat SS, Brady H, Doubleday M, Gayo L, Hickman M, Jalluri RK, Khammungkhune S, Kois A, Mortensen D, Richard N, Sapienza J, Shevlin G, Stein B, Sutherland M. McKie JA, et al. Among authors: sapienza j. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3407-10. doi: 10.1016/j.bmcl.2004.04.081. Bioorg Med Chem Lett. 2004. PMID: 15177442
59 results