
SPR-Measured Dissociation Kinetics of PROTAC Ternary …
Here we utilized a comprehensive characterization of the ligand-dependent CRBN-BRD4 interaction to demonstrate that binding between proteins that have not evolved to interact is …
Delineating the role of cooperativity in the design of potent …
2018年7月16日 · Surface plasmon resonance (SPR) is used to generate binary binding affinities of PROTACs to BTK and CRBN (Fig. 3 A and B and SI Appendix, Fig. S5). Based on previous …
Structural and biophysical comparisons of the pomalidomide
2023年12月12日 · To identify the minimal SALL4 binding domain that interacts with human cereblon complexed with IMiD molecules pomalidomide and CC-220, we examined the SPR …
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 …
SPR-Measured Dissociation Kinetics of PROTAC Ternary …
Here, we develop an SPR-based assay to quantify the stability of PROTAC-induced ternary complexes by measuring for the first time the kinetics of their formation and dissociation in …
Affinity and cooperativity modulate ternary complex formation to …
2023年7月13日 · SPR and ITC methods reveal that ternary complex formation can be potently influenced by both protein-protein interactions (PPIs) and protein-small molecule interactions.
Discovery of Highly Potent CRBN Ligands and Insight into Their …
2023年3月1日 · Cereblon (CRBN) is a substrate receptor of E3 ubiquitin ligase as well as the target of thalidomide and lenalidomide, plays a vital role in endogenous protein degradation. In …
The Development and Application of Biophysical Assays for …
2024年1月12日 · For this system, robust SPR, BLI, and ITC assays were developed that reproduced published results demonstrating the cooperativity of ternary complex formation. In …
Cereblon CULT Domain SPR Assay Service - Reaction Biology
Surface Plasmon Resonance (SPR) technique for evaluating direct binding of cereblon CULT domain to molecules
CRBN配体的作用和最新进展 - 知乎 - 知乎专栏
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 …