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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. Among authors: lu cc, lu g. Blood. 2021 Feb 4;137(5):661-677. doi: 10.1182/blood.2020008676. Blood. 2021. PMID: 33197925 Free PMC article.
CC-122, a pleiotropic pathway modifier, mimics an interferon response and has antitumor activity in DLBCL.
Hagner PR, Man HW, Fontanillo C, Wang M, Couto S, Breider M, Bjorklund C, Havens CG, Lu G, Rychak E, Raymon H, Narla RK, Barnes L, Khambatta G, Chiu H, Kosek J, Kang J, Amantangelo MD, Waldman M, Lopez-Girona A, Cai T, Pourdehnad M, Trotter M, Daniel TO, Schafer PH, Klippel A, Thakurta A, Chopra R, Gandhi AK. Hagner PR, et al. Among authors: lu g. Blood. 2015 Aug 6;126(6):779-89. doi: 10.1182/blood-2015-02-628669. Epub 2015 May 22. Blood. 2015. PMID: 26002965 Free PMC article. Clinical Trial.
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. Among authors: lu cc. Elife. 2018 Sep 20;7:e40958. doi: 10.7554/eLife.40958. Elife. 2018. PMID: 30234487 Free PMC article.
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: lu g. 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
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: lu cc, lu g. Nature. 2016 Jul 14;535(7611):252-7. doi: 10.1038/nature18611. Epub 2016 Jun 22. Nature. 2016. PMID: 27338790
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: lu cc, lu g. 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
Crystal structure of the SALL4-pomalidomide-cereblon-DDB1 complex.
Matyskiela ME, Clayton T, Zheng X, Mayne C, Tran E, Carpenter A, Pagarigan B, McDonald J, Rolfe M, Hamann LG, Lu G, Chamberlain PP. Matyskiela ME, et al. Among authors: lu g. Nat Struct Mol Biol. 2020 Apr;27(4):319-322. doi: 10.1038/s41594-020-0405-9. Epub 2020 Apr 6. Nat Struct Mol Biol. 2020. PMID: 32251415
8,092 results