In 2022,Yu, Xufen; Cheng, Meng; Lu, Kaylene; Shen, Yudao; Zhong, Yue; Liu, Jing; Xiong, Yue; Jin, Jian published an article in Journal of Medicinal Chemistry. The title of the article was 《Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras》.Category: esters-buliding-blocks The author mentioned the following in the article:
Several epidermal growth factor receptor (EGFR) proteolysis-targeting chimeras (PROTACs), including MS39 and MS154 developed by us, have been reported to effectively degrade the mutant but not the wild-type (WT) EGFR. However, the mechanism underlying the selectivity in degrading the mutant over the WT EGFR has not been elucidated. Here, we report comprehensive structure-activity relationship studies that led to the discovery of two novel EGFR degraders, 31 (MS9449) and 72 (MS9427), and mechanistic studies of these EGFR degraders. Compounds 31 (I) and 72(II) selectively degraded the mutant but not the WT EGFR through both ubiquitination/proteasome and autophagy/lysosome pathways. Interestingly, we found that the mutant but not the WT EGFR can effectively form EGFR-PROTAC-E3 ligase ternary complexes. Furthermore, we found that PI3K inhibition sensitized WT EGFR to PROTAC-induced degradation and combination treatment with a PI3K inhibitor enhanced antiproliferation activities of EGFR degraders in cancer cells harboring WT EGFR, providing a potential therapeutic strategy for patients with WT EGFR overexpression. The results came from multiple reactions, including the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Category: esters-buliding-blocks)
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).Category: esters-buliding-blocks
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