2023年10月30日 · Cereblon (CRBN) is a ubiquitin ligase (E3) substrate receptor protein co-opted by CRBN E3 ligase modulatory drug (CELMoD) agents that target therapeutically relevant proteins for degrdn.

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. Despite this...

2021年1月1日 · Cereblon (CRBN), the substrate receptor of an E3 ubiquitin ligase complex, is a target of thalidomide and thalidomide-derived immunomodulatory drugs (IMiDs). The binding of these IMiDs to CRBN alters the substrate specificity of the ligase, thereby mediating multiple effects that are exploited in cancer therapy.

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 of a new cereblon...

2022年6月5日 · CRBN modulators could promote the binding of CRBN to specific target proteins or block the binding of CRBN to some endogenous proteins. In this way, CRBN modulators suppress various tumor cells by modulating the interactions …

2021年8月9日 · In the case of CRBN, an in vitro site-directed mutagenesis study on CRBN TBD has shown that mutation of any of the 4 cysteines involved in the Zn finger formation led to protein misfolding and...

Increasing the molecular structure of the CRBN ligand significantly elevated lipophilicity and was accompanied by higher HSA binding values. Among the four new PROTACs tested, 13a–13d induced pronounced degradation of BRD4 (Fig. 5A), and appropriate control experiments demonstrated the involvement of the ubiquitin-proteasome system (Fig. 5B).

近年来，CRBN配体逐渐成为一个非常流行的E3连接酶配体，不仅可以用作E3连接酶配体来设计合成PROTACs，也可以用来设计分子胶降解剂，在PROTACs和分子胶领域中起着非常重要的作用。

2022年11月22日 · Cereblon（CRBN）是细胞中主要蛋白质处理系统的一部分。 该系统用称为泛素的分子标记靶向蛋白质，有效地标记蛋白质，以通过称为蛋白酶体的流动蛋白质分解复合物进行破坏。

MST traces and affinities of the BODIPY-uracil reporter and reference compounds to the bacterial MsCI4 and the thalidomide binding domain of human CRBN (hTBD). The affinity of BODIPY-uracil was determined via initial fluorescence measurements.