多发性骨髓瘤治疗靶点：CRL4 E3连接酶 - 脉脉
2022年12月19日 · 研究表明，IMiDs主要通过结合CRL4 E3泛素连接酶 (CRL4CRBN) 复合物的底物受体蛋白Cereblon (CRBN) 发挥其抗骨髓瘤活性。 通过结合CRBN，IMiDs改变了其底物的 …
CRL4 CRBN E3 Ligase Complex as a Therapeutic Target in …
Cereblon (CRBN), a target of IMiDs, forms the CRL4 E3 ubiquitin ligase complex (CRL4 CRBN) with DDB1, CUL4A and RBX1. The insight into the molecular mechanism of IMiDs action has …
The E3 ubiquitin ligase component, Cereblon, is an ... - Nature
2021年9月6日 · Binding of IMiDs to Cereblon (CRBN), the substrate receptor of the CRL4 CRBN E3 ubiquitin ligase, induces cancer cell death by targeting key neo-substrates for degradation. …
A novel cereblon modulator recruits GSPT1 to the CRL4 CRBN …
2016年6月22日 · Immunomodulatory drugs bind to cereblon (CRBN) to confer differentiated substrate specificity on the CRL4 CRBN E3 ubiquitin ligase. Here we report the identification …
CRBN配体的作用和最新进展 - 知乎
最新的AACR会议上，已经有一批公司使用新型CRBN配体，包括 Arvinas公司 的第二代AR降解剂ARV-766， C4公司 的BRD9 降解剂CFT8634和BRAF V600E降解剂CFT1946，以及Kymera …
CRL4 CRBN E3 Ligase Complex as a Therapeutic Target in
2022年9月16日 · It is now known that IMiDs exert their anti-myeloma activity mainly by binding cereblon (CRBN), the substrate receptor protein of the CRL4 E3 ubiquitin ligase (CRL4 CRBN) …
Structural basis of lenalidomide-induced CK1α degradation by the CRL4 ...
2016年2月24日 · Thalidomide and its derivative lenalidomide bind the CRL4CRBN E3 ubiquitin ligase and target protein substrates for degradation; structural and functional data determined …
Protein Degradation via CRL4 - ACS Publications
2017年3月30日 · Synthesis of novel glutarimide ligands for the E3 ligase substrate receptor Cereblon (CRBN): Investigation of their binding mode and antiproliferative effects against …
The E3 ubiquitin ligase component, Cereblon, is an ... - PubMed
2021年9月6日 · Binding of IMiDs to Cereblon (CRBN), the substrate receptor of the CRL4 CRBN E3 ubiquitin ligase, induces cancer cell death by targeting key neo-substrates for degradation. …
A novel cereblon modulator recruits GSPT1 to the CRL4(CRBN …
2016年7月14日 · Immunomodulatory drugs bind to cereblon (CRBN) to confer differentiated substrate specificity on the CRL4 (CRBN) E3 ubiquitin ligase. Here we report the identification …