泛素连接酶
小脑
泛素
蛋白酶体
癌症研究
化学
蛋白质水解
连接器
蛋白质降解
小分子
化学生物学
细胞生物学
生物
生物化学
酶
操作系统
基因
计算机科学
标识
DOI:10.1021/acsmedchemlett.3c00181
摘要
The B-cell lymphoma 2 (BCL-2) protein is the most extensively studied anti-apoptotic member within the BCL-2 protein family. It functions to inhibit programmed cell death by forming a heterodimer with BAX, thereby promoting cellular survival through the extension of tumor cell lifespan and facilitating malignant transformation. This Patent Highlight reveals the development of small molecule degraders that consist of a ligand targeting the protein of interest, BCL-2, an E3 ubiquitin ligase recruitment ligand (such as Cereblon or Von Hippel–Lindau ligands), and a chemical linker that connects the two ligands. The proteolysis-targeting chimera (PROTAC)-mediated heterodimerization of the bound proteins leads to the ubiquitination of the target protein, which is subsequently degraded by the proteasome. This strategy offers innovative therapeutic options for cancer, immunology, and autoimmune disease management.
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