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Lenalidomide induces ubiquitination and degradation of CK1alpha 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. Nature. 2015 Jul 9;523(7559):183-188. doi: 10.1038/nature14610. Epub 2015 Jul 1. Nature. 2015. PMID: 26131937 Free PMC article.
Here, we demonstrate that lenalidomide induces the ubiquitination of casein kinase 1A1 (CK1alpha) by the E3 ubiquitin ligase CUL4-RBX1-DDB1-CRBN (known as CRL4(CRBN)), resulting in CK1alpha degradation. CK1alpha is encoded b …
Here, we demonstrate that lenalidomide induces the ubiquitination of casein kinase 1A1 (CK1alpha) by the E3 u …
Structural basis of lenalidomide-induced CK1alpha degradation by the CRL4(CRBN) ubiquitin ligase.
Petzold G, Fischer ES, Thomä NH. Petzold G, et al. Nature. 2016 Apr 7;532(7597):127-30. doi: 10.1038/nature16979. Epub 2016 Feb 24. Nature. 2016. PMID: 26909574
Unexpectedly, IMiDs also repurpose the ligase to target new proteins for degradation. Lenalidomide induces degradation of the lymphoid transcription factors Ikaros and Aiolos (also known as IKZF1 and IKZF3), and casein kinase 1alpha (CK1alpha), …
Unexpectedly, IMiDs also repurpose the ligase to target new proteins for degradation. Lenalidomide induces degradati …
Genome-wide screen identifies cullin-RING ligase machinery required for lenalidomide-dependent CRL4(CRBN) activity.
Sievers QL, Gasser JA, Cowley GS, Fischer ES, Ebert BL. Sievers QL, et al. Blood. 2018 Sep 20;132(12):1293-1303. doi: 10.1182/blood-2018-01-821769. Epub 2018 Jul 24. Blood. 2018. PMID: 30042095 Free PMC article.
Lenalidomide mediates the ubiquitination and degradation of Ikaros family zinc finger protein 1 (IKZF1), IKZF3, and casein kinase 1alpha (CK1alpha) by facilitating their interaction with cereblon (CRBN), the substrate receptor for the CRL4(CRBN) E3 …
Lenalidomide mediates the ubiquitination and degradation of Ikaros family zinc finger protein 1 (IKZF1), IKZF3, and cas …