一种针对癌症治疗的靶向 SMARCA2 的两面选择性解决方案。
A two-faced selectivity solution to target SMARCA2 for cancer therapy.
机构信息
Dept. of Medicinal Chemistry, GSK, Gunnels Wood Road, Stevenage, SG1 2NY, UK.
出版信息
Nat Commun. 2023 Jan 31;14(1):515. doi: 10.1038/s41467-023-36238-0.
Abstract
Two new studies exploring PROTAC-mediated degradation of SMARCA2 for cancer therapy solve an apparently intractable selectivity challenge with SMARCA4 by utilising the requirement for a productive ternary complex between the protein, PROTAC and ligase complex.
摘要
两项探索利用蛋白、PROTAC 和连接酶复合物之间的三元复合物形成的必需性，来解决 SMARCA4 中明显难以解决的选择性问题的 PROTAC 介导的 SMARCA2 降解用于癌症治疗的新研究。
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