ERRα

PROTAC ERRα ligand 1 是一种雌激素相关受体 α (ERRα) 拮抗剂，能够作用于 ERRα (IC50:0.04 μM)和 ERRγ (IC50:2.8 μM)。

PROTAC ERRα ligand 2 是雌激素相关受体 α （ERRα）反向激动剂。它对 ERRα (IC50=5.67 nM) 的抑制作用比 XCT790 (IC50=61.3 nM) 高效约 11 倍。

ERRα Ligand-Linker Conjugates 1 refers to a chemical compound that consists of a ligand targeting estrogen-related receptor alpha (ERRα), and a PROTAC linker that facilitates the recruitment of E3 ligases MDM2. It finds utility in the synthesis of a range of PROTACs, including one known as PROTAC ERRalpha Degrader-1. With its capability to induce degradation of ERRα, PROTAC ERRalpha Degrader-1 functions as an ERRα degrader[1].

PROTAC ERRα Degrader-2 is a compound consisting of an MDM2 ligand binding group, a linker, and an estrogen-related receptor alpha (ERRα) binding group. This compound is designed to specifically degrade estrogen-related receptor alpha (ERRα), acting as an ERRα degrader[1].

(rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1, which is an estrogen-related receptor alpha (ERRa) degrader. PROTAC ERRα Degrader-1 consists of an MDM2 ligand binding moiety, a linker and an ERRa binding moiety [1].

PROTAC ERRα Degrader-3 is a highly effective and selective von Hippel-Lindau-based ligand that efficiently degrades the ERRα protein. At a concentration of 30 nM, this compound exhibits a remarkable degradation capability, reducing the ERRα protein levels by >80%. Importantly, PROTAC ERRα Degrader-3 shows no activity against the ERRβ and ERRγ proteins.

Vepdegestrant （ARV-471） 是一种雌激素受体 (ER) α PROTAC 分子，可降解 ER 阳性乳腺癌细胞系中的 ER，DC50 约为 1 nM。它可以通过降解 ER 来降低经典调节的 ER 靶基因的表达并抑制 ER 依赖性细胞系（包括表达 ESR1 变体的细胞系，例如 Y537S 和 D538G）的生长。

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。

ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively).ERD-308 is a highly potent PROTAC degrade

PROTAC ER Degrader-4 is a PROTAC degrader of the estrogen receptor (ER) with an IC50 of 0.8 nM.

Estrone-N-O-C1-amido (ERα ligand 1) is an estrogen ligand derived from Estrone that specifically binds to estrogen receptor α (ERα). Through a linker, Estrone-N-O-C1-amido (ERα ligand 1) forms a complex with the cIAP1 ligand Bestatin, leading to the creation of SNIPER[1].

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-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-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].

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).

SNIPER(ER)-110 comprises a cIAP1 ligand and an estrogen ligand connected by a linker. SNIPER(ER)-51 induces estrogen receptor (ER) protein degradation with DC50s of <3 nM and 7.7 nM after 4 h and 48 h, respectively [1].

SNIPER(ER)-87 is a chemical compound composed of a derivative of the inhibitor of apoptosis protein (IAP) ligand LCL161 conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen using a PEG linker. It effectively degrades the ERα protein with an IC50 value of 0.097 μM. Within cells, SNIPER(ER)-87 selectively recruits XIAP to ERα, and XIAP functions as the primary E3 ubiquitin ligase responsible for the degradation of ERα induced by SNIPER(ER)-87[1][2].

ERD-1233，一种雌激素受体 (estrogen receptor) PROTAC降解剂，具有高效性和可口服的特点，其DC50值仅为0.9 nM。该化合物在ER+乳腺癌的研究中展示出关键作用。

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

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。

ER ligand-6 是 PROTAC ER Degrader-14 的靶蛋白配体 (target protein ligand)。

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。

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。