estrogen receptor alpha

Propyl pyrazole triol (PPT) 是雌激素受体 α(ERα)选择性激动剂。它对 ERα 的相对结合亲和力 (ERα: 49%) 比雌激素受体 β (ERβ: 0.12%) 高 410 倍。

Alpha-Estradiol (Epiestradiol) 是一种雌性激素，可抑制5α-reductase，在雄原性脱发的研究中有潜力。

(-)-(S)-Equol (4',7-Dihydroxyisoflavan) 是雌激素受体β的高亲和力配体。

XCT790 是 ERRα的一种选择性反向激动剂，IC50值为 0.37 μM。它在化疗过程中诱导癌细胞死亡。

MPP dihydrochloride is a highly selective antagonist of estrogen receptor alpha (ERα).

α-Zearalenol 是一种霉菌毒素，对雌激素受体具有高亲和力。它是 zearalenone (ZEN) 的一种衍生物，由于其异种雌激素效应可引起动物的生殖障碍。

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].

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 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 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].

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).

(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].

Trioxifene (LY133314) 是一种选择性雌激素受体调节剂 (SERM)，具有与雌二醇竞争性结合雌激素受体 alpha (ERalpha) 的活性，并对ERalpha介导的基因表达具有拮抗作用。

ERα degrader12 (Compound RA3) 是一种具有抗肿瘤活性的雌激素受体 α (ERα) 降解剂。在乳腺癌异种移植小鼠模型中，ERα degrader12 能显著抑制肿瘤生长。

AZD9496 maleate is a highly potent and selective antagonist of the estrogen receptor alpha (ERα), exhibiting an IC50 value of 0.28 nM. This compound, AZD9496 maleate, is an orally bioavailable selective estrogen receptor degrader (SERD).

DK3 是雌激素相关受体 α(ERRα)的一种有效的选择性激动剂，ERRα是癌症和代谢性疾病的潜在药物靶点[1]。

DS20362725是一种选择性的雌激素相关受体α（ERRα）激动剂，能够结合ERRα并增强其转录活性，同时阻止ERRα与其抑制因子，受体相互作用蛋白140（RIP140），结合，常用于研究代谢紊乱疾病。

(Rac)-ErSO-DFP 是一种 ErSO-DFP 的衍生物，也是一种选择性小分子 Erα 生物调节剂。(Rac)-ErSO-DFP 能够过度激活 ERα+ 依赖性的预期未折叠蛋白反应，表现出抗雌激素受体 α 阳性乳腺癌 (包括其抗性肿瘤) 的作用。

OBHS 是一种雌激素受体 α (ERα) 的抑制剂。

Estrogen receptor antagonist 2 是 estrogen receptor 的选择性下调剂。雌激素 (E2) 和雌激素 α 受体 (ERα) 是乳腺癌发展的重要驱动因素。Estrogen receptor antagonist 2 对乳腺癌疾病具有研究潜力。

ERα antagonist 1 是选择性的、有效的、共价雌激素受体 α (ERα)拮抗剂。ERα antagonist 1 能够将 MCF-7 细胞的细胞周期阻滞在 G0 G1 期，并诱导其凋亡 (apoptosis)。

TAS-108, also known as SR16234, is a synthetic, antiestrogenic steroidal compound with potential antitumor activity. TAS-108 binds to and inhibits estrogenic receptor alpha (ERa), mainly expressed in the mammary gland and uterus and upregulated in estrogen-dependent tumors. Blockage of ERa by TAS-108 prevents the binding and effects of estrogen and may lead to an inhibition of estrogen-dependent cancer cell proliferation. TAS-108 also is a partial agonist of the estrogenic receptor beta (ERb), expressed in many tissues including the central nervous system, urogenital tract, bone and cardiovascular system, thereby exerting a positive effect on these tissues.

TTC-352 is an orally bioavailable selective human estrogen receptor alpha (ERalpha; ESR1; ERa) partial agonist (ShERPA), with potential antineoplastic activity. Upon administration, TTC-352 mimics the naturally-occurring 17beta-estradiol (E2) and targets and binds to ERa located in the nucleus. This causes translocation of ERa to extranuclear sites. Nuclear export of ERa prevents normal ER-mediated signaling and inhibits proliferation of ER-positive tumor cells.