Leveraging Ligand Affinity and Properties: Discovery of Novel …
2023年10月30日 · Immunomodulatory imide drugs (IMiDs) such as thalidomide, pomalidomide, and lenalidomide are the most common cereblon (CRBN) recruiters in proteolysis-targeting …
Design of a Cereblon construct for crystallographic and …
2024年10月15日 · We present the design of CRBN midi, a construct that readily expresses from E. coli with high yields as soluble, stable protein without DDB1. We benchmark CRBN midi for …
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 …
Facilitating the development of molecular glues: Opportunities …
2024年1月5日 · Considerable efforts have demonstrated that cereblon (CRBN), a ubiquitously expressed protein that is part of the cullin-4-containing E3 ubiquitin ligase complex …
Discovery of potential novel CRBN modulators by virtual …
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 …
Science | 靶向蛋白降解途径突破，几乎可用于任何疾病相关蛋白
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 …
NanoTemper MST分子互作经典案例集锦_CLpro_检测_蛋白 - 搜狐
2023年7月18日 · MST技术用于Protac药物的筛选，灵敏度高，检测范围广，而且在液体条件下进行检测，无需分子固定，可以保证二元复合物处于可控的平衡状态，固定的话会影响二元复合 …
2024年1月25日 · Specialized suite of biochemical and cellular assays to assess proximity and degradation in high throughput. Proprietary database of >100 cryo-EM and crystal structures …
Identification and structural basis of C-terminal cyclic imides as ...
2022年12月31日 · Cereblon (CRBN) is a ubiquitously expressed E3 ligase substrate receptor and a key player in pharmaceutical targeted protein degradation. Despite substantial insight gained …
Mining the CRBN Target Space Redefines Rules for Molecular
2024年10月9日 · Through computational mining of the human proteome using structure-based approaches, we predict over 1,400 CRBN-compatible β-hairpin G-loop proteins across diverse …
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