protac er degrader 2

PROTAC ER Degrader-2 serves as a synthesis intermediate for the production of PAC, a compound that incorporates the ADCs linker and PROTACs, which are subsequently conjugated to an antibody. PAC, exhibits a greater capability to degrade estrogen receptor-alpha (ERα) compared to PROTAC (without the presence of an antibody)[1].

PROTAC ERα Degrader-2 comprises a cIAP1 ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

ER ligand-2 作为ER的特定配体，可用于合成PROTAC ER Degrader-11。

PROTAC ER Degrader-14 (compound 86) 是一种 PROTAC 类型的 Estrogen Receptor ERR 降解剂，由以下部分组成：E3 泛素连接酶配体 (blue part)(S)-Deoxy-thalidomide、PROTAC Linker (black part) N-Boc-piperazine，以及靶蛋白配体 (red part) ER ligand-6。E3 连接酶加上 Linker 共同构成了 tert-Butyl (S)-4-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)piperazine-1-carboxylate。