protac erα degrader 1

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).

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。

PROTACER Degrader-10 是一种有效的PROTACER 降解剂，可用于癌症研究。

PROTA CER Degrader-11 (Example 26-1) 作为一种高效的PROTA CER降解剂，其IC50仅为0.66 nM，主要在癌症研究领域发挥关键作用。

PROTAC ER Degrader-15 (Compound 40) 是口服有效的雌激素受体 (ER) 降解剂，具有抗癌特性，可用于乳腺癌研究。

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。

PROTACERαDegrader-8 (compound ii-56) 作为一种高效的ErαPROTAC降解剂，其在MCF7细胞中的DC50仅为0.000006 μM。

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。

ERD-3111 (Compound 44) 是一种口服活性PROTAC ERα降解剂，DC50为0.5 nM。该化合物有效抑制含野生型ER的MCF-7异种移植模型以及两种携带ESR1突变的临床相关小鼠模型中的肿瘤生长，可用于研究ER+乳腺癌。

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].

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].