Min, Jaeki; Mayasundari, Anand; Keramatnia, Fatemeh; Jonchere, Barbara; Yang, Seung Wook; Jarusiewicz, Jamie; Actis, Marisa; Das, Sourav; Young, Brandon; Slavish, Jake; Yang, Lei; Li, Yong; Fu, Xiang; Garrett, Shalandus H.; Yun, Mi-Kyung; Li, Zhenmei; Nithianantham, Stanley; Chai, Sergio; Chen, Taosheng; Shelat, Anang; Lee, Richard E.; Nishiguchi, Gisele; White, Stephen W.; Roussel, Martine F.; Potts, Patrick Ryan; Fischer, Marcus; Rankovic, Zoran published an article in 2021. The article was titled 《Phenyl-Glutarimides: Alternative Cereblon Binders for the Design of PROTACs》, and you may find the article in Angewandte Chemie, International Edition.Related Products of 51644-96-3 The information in the text is summarized as follows:
Targeting cereblon (CRBN) is currently one of the most frequently reported proteolysis-targeting chimera (PROTAC) approaches, owing to favorable drug-like properties of CRBN ligands, immunomodulatory imide drugs (IMiDs). However, IMiDs are known to be inherently unstable, readily undergoing hydrolysis in body fluids. Here we show that IMiDs and IMiD-based PROTACs rapidly hydrolyze in commonly utilized cell media, which significantly affects their cell efficacy. We designed novel CRBN binders, Ph glutarimide (PG) analogs, and showed that they retained affinity for CRBN with high ligand efficiency (LE >0.48) and displayed improved chem. stability. Our efforts led to the discovery of PG PROTAC 4 c (SJ995973), a uniquely potent degrader of bromodomain and extra-terminal (BET) proteins that inhibited the viability of human acute myeloid leukemia MV4-11 cells at low picomolar concentrations (IC50=3 pM; BRD4 DC50=0.87 nM). These findings strongly support the utility of PG derivatives in the design of CRBN-directed PROTACs. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Related Products of 51644-96-3)
Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Related Products of 51644-96-3
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