estrogen receptor-alpha (erα)

PAC is a chemical conjugate consisting of an ADCs linker and PROTACs linked to an antibody. When PAC is conjugated to an antibody, it exhibits enhanced degradation of estrogen receptor-alpha (ERα) in comparison to PROTAC alone.

PROTAC ERα Degrader-1 is a chemical compound. It consists of a ubiquitin E3 ligase binding group, a linker, and a protein binding group. This compound serves as a degrader of estrogen receptor-alpha (ERα).

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 ER Degrader-3, an intermediate for the synthesis of PAC, specifically compound LP2. PAC serves as the linker for ADCs and PROTACs that are conjugated to an antibody. Notably, when PAC is conjugated to an antibody, it exhibits enhanced degradation of estrogen receptor-alpha (ERα) compared to PROTAC alone [1].

PROTACERαY537S degrader-1 包含泛素 E3 连接酶结合基团，linker 和靶蛋白结合基团。PROTACERαY537S degrader-1 是雌激素受体-α (ERα) Y537S 的降解剂。

PROTACERα Degrader-7 (compound i-320) 作为一种高效的雌激素受体 α (estrogen receptor alpha (ERα)) PROTAC降解剂，其 DC50 值仅为0.000006 µM。该化合物具备小分子 LBM 部分与配体 ERBM 的连接，其中配体 ERBM 能特异性地结合ERα，并且含有苯并稠合部分以及饱和的6元碳环或杂环结构。