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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.
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
SALL4 mediates teratogenicity as a thalidomide-dependent cereblon substrate.
Matyskiela ME, Couto S, Zheng X, Lu G, Hui J, Stamp K, Drew C, Ren Y, Wang M, Carpenter A, Lee CW, Clayton T, Fang W, Lu CC, Riley M, Abdubek P, Blease K, Hartke J, Kumar G, Vessey R, Rolfe M, Hamann LG, Chamberlain PP. Matyskiela ME, et al. Among authors: lu cc, lu g. Nat Chem Biol. 2018 Oct;14(10):981-987. doi: 10.1038/s41589-018-0129-x. Epub 2018 Sep 6. Nat Chem Biol. 2018. PMID: 30190590
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
8,069 results