Structural bases of IMiD selectivity that emerges by 5 ... - Nature
2020年9月14日 · The (S)-5HT-mediated IKZF1–CRBN interaction was detected by the residue-swap Q146V mutation in IKZF1, and the effect was slightly increased by the addition of the …
Expression of CRBN, IKZF1, and IKZF3 does not predict ... - PubMed
Cereblon (CRBN), the direct target of IMiDs, has been proposed as a predictive biomarker of response to IMiDs. Using standard immunohistochemistry in formalin-fixed paraffin embedded …
来那度胺促进 CRBN 介导的 IKZF1 和 IKZF3 泛素化和降解,Blood
2013年11月15日 · 此外，我们证实 ikzf1 和 ikzf3 在来那度胺存在下结合 crbn，支持 crbn 作为底物接头的作用。 与此一致，shRNA 介导的不结合来那度胺的 CRBN 突变体 (CRBN YWAA) 的 …
Defining the human C2H2 zinc finger degrome targeted by ... - Science
2018年11月2日 · These drugs induce rapid ubiquitination and proteasomal degradation of two transcription factors, Ikaros (IKZF1) and Aiolos (IKZF3), by recruiting them to the CRL4 CRBN …
Nature：沙利度胺的作用靶点最终确证为CRBN - 丁香园
2014年7月21日 · 2010年科学家发现沙利度胺与CRBN (cereblon)直接结合，CRBN则与DDB1 (damaged DNA binding protein 1)、Cul4A (Cullin 4A)、ROC1形成E3泛素连接酶复合 …
Structural rationalization of GSPT1 and IKZF1 degradation by ...
2023年1月26日 · Here, we profile 14 closely-related thalidomide derivatives in CRBN occupancy, and IKZF1 and GSPT1 degradation cell-based assays, and use crystal structures, …
IKZF1/3 and CRL4 CRBN E3 ubiquitin ligase mutations and …
Cereblon (CRBN), a target of immunomodulatory drugs (IMiD), forms the CRL4 CRBN E3 ubiquitin ligase (CRL4) complex with DDB1, CUL4B and ROC1. 1,2 Under the influence of …
Identification of cereblon-binding proteins and relationship …
Ten proteins were identified in the CRBN complex by both methods, including IKZF1, a protein that has recently been identified by others as a substrate of CRBN E3 ubiquitin ligase activity. …
Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in ...
2013年11月28日 · In aggregate, our studies demonstrate that lenalidomide acts via a previously unknown mechanism of drug activity—enforced binding of the substrate receptor CRBN to …
Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with ...
2014年7月16日 · IMiDs target the E3 ubiquitin ligase CUL4–RBX1–DDB1–CRBN (known as CRL4 CRBN) and promote the ubiquitination of the IKAROS family transcription factors IKZF1 …