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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: cathers be. 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 CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma.
Hansen JD, Correa M, Nagy MA, Alexander M, Plantevin V, Grant V, Whitefield B, Huang D, Kercher T, Harris R, Narla RK, Leisten J, Tang Y, Moghaddam M, Ebinger K, Piccotti J, Havens CG, Cathers B, Carmichael J, Daniel T, Vessey R, Hamann LG, Leftheris K, Mendy D, Baculi F, LeBrun LA, Khambatta G, Lopez-Girona A. Hansen JD, et al. J Med Chem. 2020 Jul 9;63(13):6648-6676. doi: 10.1021/acs.jmedchem.9b01928. Epub 2020 Mar 19. J Med Chem. 2020. PMID: 32130004
CC-90009, a novel cereblon E3 ligase modulator, targets acute myeloid leukemia blasts and leukemia stem cells.
Surka C, Jin L, Mbong N, Lu CC, Jang IS, Rychak E, Mendy D, Clayton T, Tindall E, Hsu C, Fontanillo C, Tran E, Contreras A, Ng SWK, Matyskiela M, Wang K, Chamberlain P, Cathers B, Carmichael J, Hansen J, Wang JCY, Minden MD, Fan J, Pierce DW, Pourdehnad M, Rolfe M, Lopez-Girona A, Dick JE, Lu G. Surka C, et al. Blood. 2021 Feb 4;137(5):661-677. doi: 10.1182/blood.2020008676. Blood. 2021. PMID: 33197925 Free PMC article.
A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos.
Matyskiela ME, Zhang W, Man HW, Muller G, Khambatta G, Baculi F, Hickman M, LeBrun L, Pagarigan B, Carmel G, Lu CC, Lu G, Riley M, Satoh Y, Schafer P, Daniel TO, Carmichael J, Cathers BE, Chamberlain PP. Matyskiela ME, et al. Among authors: cathers be. J Med Chem. 2018 Jan 25;61(2):535-542. doi: 10.1021/acs.jmedchem.6b01921. Epub 2017 Apr 20. J Med Chem. 2018. PMID: 28425720
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: cathers be. 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 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: cathers be. 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
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: cathers be. 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
A novel cereblon modulator recruits GSPT1 to the CRL4(CRBN) ubiquitin ligase.
Matyskiela ME, Lu G, Ito T, Pagarigan B, Lu CC, Miller K, Fang W, Wang NY, Nguyen D, Houston J, Carmel G, Tran T, Riley M, Nosaka L, Lander GC, Gaidarova S, Xu S, Ruchelman AL, Handa H, Carmichael J, Daniel TO, Cathers BE, Lopez-Girona A, Chamberlain PP. Matyskiela ME, et al. Among authors: cathers be. Nature. 2016 Jul 14;535(7611):252-7. doi: 10.1038/nature18611. Epub 2016 Jun 22. Nature. 2016. PMID: 27338790
UBE2G1 governs the destruction of cereblon neomorphic substrates.
Lu G, Weng S, Matyskiela M, Zheng X, Fang W, Wood S, Surka C, Mizukoshi R, Lu CC, Mendy D, Jang IS, Wang K, Marella M, Couto S, Cathers B, Carmichael J, Chamberlain P, Rolfe M. Lu G, et al. Elife. 2018 Sep 20;7:e40958. doi: 10.7554/eLife.40958. Elife. 2018. PMID: 30234487 Free PMC article.
33 results