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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: chamberlain p. Blood. 2021 Feb 4;137(5):661-677. doi: 10.1182/blood.2020008676. Blood. 2021. PMID: 33197925 Free PMC article.
Structure of the human Cereblon-DDB1-lenalidomide complex reveals basis for responsiveness to thalidomide analogs.
Chamberlain PP, Lopez-Girona A, Miller K, Carmel G, Pagarigan B, Chie-Leon B, Rychak E, Corral LG, Ren YJ, Wang M, Riley M, Delker SL, Ito T, Ando H, Mori T, Hirano Y, Handa H, Hakoshima T, Daniel TO, Cathers BE. Chamberlain PP, et al. Nat Struct Mol Biol. 2014 Sep;21(9):803-9. doi: 10.1038/nsmb.2874. Epub 2014 Aug 10. Nat Struct Mol Biol. 2014. PMID: 25108355
Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDS.
Krönke J, Fink EC, Hollenbach PW, MacBeth KJ, Hurst SN, Udeshi ND, Chamberlain PP, Mani DR, Man HW, Gandhi AK, Svinkina T, Schneider RK, McConkey M, Järås M, Griffiths E, Wetzler M, Bullinger L, Cathers BE, Carr SA, Chopra R, Ebert BL. Krönke J, et al. Among authors: chamberlain pp. Nature. 2015 Jul 9;523(7559):183-188. doi: 10.1038/nature14610. Epub 2015 Jul 1. Nature. 2015. PMID: 26131937 Free PMC article.
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: chamberlain pp. 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: chamberlain pp. 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
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: chamberlain pp. 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
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: chamberlain p. Elife. 2018 Sep 20;7:e40958. doi: 10.7554/eLife.40958. Elife. 2018. PMID: 30234487 Free PMC article.
Evolution of Cereblon-Mediated Protein Degradation as a Therapeutic Modality.
Chamberlain PP, D'Agostino LA, Ellis JM, Hansen JD, Matyskiela ME, McDonald JJ, Riggs JR, Hamann LG. Chamberlain PP, et al. ACS Med Chem Lett. 2019 Nov 12;10(12):1592-1602. doi: 10.1021/acsmedchemlett.9b00425. eCollection 2019 Dec 12. ACS Med Chem Lett. 2019. PMID: 31857833 Free PMC article.
315 results