Thalidomide-O-C6-azide is a synthesized E3 ligase ligand-linker conjugate (PROTAC technology[1].
PROTAC 包含两个不同的配体,通过一个接头连接;一个是 E3 泛素连接酶的配体,另一个是靶蛋白的配体。 PROTAC 利用细胞内泛素-蛋白酶体系统选择性降解靶蛋白[2]。
[1]. Chen P, et al. α-naphthoflavone-derived cytochrome P450 (CYP)1B1 degraders specific for sensitizing CYP1B1-mediated drug resistance to prostate cancer DU145: Structure activity relationship. Bioorg Chem. 2021 Nov;116:105295.
[2]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-996.
















