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estradiol (E2III)

✓ Approved

Johnson & Johnson Services, Inc. · ESR1 · 小分子

什么是 estradiol?

estradiol 是一种小分子,由Johnson & Johnson Services, Inc.研发。该药已获批,用于治疗相关适应症,给药途径:Transdermal。

药物档案

商品名E2III
公司Johnson & Johnson Services, Inc.
药物类别小分子
分子靶点ESR1
给药途径Transdermal
状态Approved

作用机制

分子靶点

estradiol 作用于 1 个分子靶点:

ESR1estrogen receptor 1 (ER, ESR)
需要更深入的分析?Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

estradiol 针对 1 个适应症,涉及 1 个治疗领域。

治疗领域疾病/病症分期
Surgical and medical proceduresHormone replacement therapy✓ Approved

相关研究文献

PubMedThe journal of physical chemistry letters2026-09-10

Unraveling the Molecular Origin of the Unprecedented ortho-Chloride Effect in Cobalt-Catalyzed Asymmetric Hydrogenation of 1,1-Diarylethenes.

Mahato Akhilesh A, Mahato Anupama A, Pramanik Anup A, Sarkar Pranab P

The molecular origin of the unusual ortho-chloride effect in cobalt-catalyzed asymmetric hydrogenation of 1,1-diarylethenes has been investigated using density functional theory. The complete catalytic cycle, including alkene coordination, alkene insertion, hydrogen activation, and catalyst regeneration, was elucidated on the relevant spin surfaces. The calculations identify alkene insertion into the Co-H bond via TS1 as the enantiodetermining step, whereas catalyst regeneration is the turnover-determining step. The preferred Si-face hydride transfer is favored by 3.79 kcal/mol, corresponding to a predicted 99.6% enantiomeric excess, in excellent agreement with the experimentally observed more than 90% ee. Activation strain, AIM, NCI, and NBO analyses reveal that reduced structural distortion together with enhanced noncovalent and donor-acceptor interactions stabilizes the transition state leading to the S enantiomer. Systematic investigation of substituent effects demonstrates that only the ortho-chloro substituent provides the optimal energetic balance, whereas meta- and para-substitution or replacement by other ortho substituents substantially diminishes enantioselectivity. These findings provide the first molecular-level explanation of the ortho-chloride effect and offer guiding principles for designing highly enantioselective cobalt catalysts.

PMID 42720340
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PubMedJournal of medicinal chemistry2026-09-10

Bright rRNA-Associated Merocyanine Probes Highlight Tumor Extensions in Ovarian Cancer.

Corn Devorah D, Boocholez Alon A, Das Prasenjit P, Zisman Martinez Shirly S et al.

We report a structure-activity relationship of merocyanine quinolinium dyes optimized as fluorogenic rRNA-associated probes. A series of analogs (11a-h) bearing electron-withdrawing groups (EWGs) or electron-donating groups (EDGs) on the phenolic "push" ring (ortho vs meta; mono vs disubstitution) was synthesized to evaluate electronic and steric effects on photophysical performance. Emission extended to 658 nm, fluorescence turn-on reached 570-fold, and brightness to 8 mM-1 cm-1. ortho-EWGs and meta-EDGs enhanced fluorescence, whereas steric hindrance (e.g., meta-dichloro) reduced planarity and diminished performance, consistent with DFT analysis. Dye 11f (meta-dimethoxy) emerged as the lead compound, combining strong fluorogenic response, brightness, stability, rapid membrane permeability, and low cytotoxicity. Enzymatic and pharmacologic perturbation experiments supported preferential cellular association of 11f with rRNA-rich compartments. U2OS cancer cells showed higher fluorescence intensity than HFF primary fibroblasts, consistent with increased rRNA-rich compartments in cancer cells. In ex vivo ovarian tumor specimens, 11f demonstrated enhanced visualization of malignant regions and small tumor extensions within surrounding adipose tissue.

PMID 42720477
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PubMedNature synthesis2026-09-10

Handle-free attachment of small molecules on single-walled carbon nanotubes.

Piletsky Stanislav S SS, Keblish Erin E EE, Goffin Alec R AR, Jin Xiaojia X et al.

Few chemical methods controllably generate sp 3 defects on single-walled carbon nanotubes, and fewer still create quantum wells that localize excitons and enhance near-infrared emission. Here we describe an aqueous, nanotube-catalysed Fenton reaction that enables the conjugation of an extensive range of small molecules lacking traditional single-walled carbon nanotube conjugation handles, generating quantum well defects with tunable electro-optical properties. We demonstrate the attachment of over 150 unique small molecules, including alcohols, amines, carbonyls, acrylates, amino acids and peptides. The resulting optical properties are governed by the electronic structure of the attached group, which determines the relative configuration of defects (ortho or para) within the graphitic lattice. Time-dependent density functional theory calculations confirm the assignment of the observed emission peaks to specific defect configurations. These molecularly driven effects enable precise control over the optical properties of the nanotubes, broadening the design space of rationally engineered quantum well-bearing nanomaterials.

PMID 42718616
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PubMedBiology of reproduction2026-09-10

Galectin-1 Signaling Dysregulation Impairs Stromal Senescence and Decidualization in Recurrent Implantation Failure.

Huang Xu X, Lin Zhi Z, Chen Min M, Zheng Zi-Meng ZM et al.

Endometrial decidualization is indispensable for embryo implantation, and moderate cellular senescence has recently been recognized as a functional component of this process. However, how this senescence response is regulated upstream and whether its disruption contributes to recurrent implantation failure (RIF) remain unclear. Here, we identify Galectin-1 (GAL1) as a potential regulator of senescence-associated decidual responses in human endometrial stromal cells. Moderate senescence induction in human endometrial stromal cells and primary decidual stromal cells (DSCs) was accompanied by enhanced decidualization responses, which was further supported by the co-localization of senescence markers with bone morphogenetic protein 2 (Bmp2) in the murine decidual zone during early gestation. GAL1 promoted senescence-associated and decidualization responses, whereas GAL1 inhibition or LGALS1 knockdown attenuated these effects. Estradiol and progesterone treatment increased GAL1 secretion and the expression of GAL1-associated extracellular components, while integrin inhibition reduced GAL1-induced decidual responses. In RIF endometrium, GAL1 expression was elevated, whereas genes associated with GAL1 signaling were downregulated in stromal cells, accompanied by reduced senescence marker expression. Collectively, our findings identify GAL1 signaling dysregulation as a potential mechanism underlying insufficient stromal senescence and impaired decidualization in a subset of RIF endometrium, providing new insights into the molecular heterogeneity of RIF.

PMID 42720313
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PubMedJournal of medicinal chemistry2026-09-10

Structure-Function Analysis of the Benzyloxy Moiety of the Delta-Opioid Receptor Positive Modulator BMS-986187: Identification of a Derivative with High Selectivity for the Delta-Opioid Receptor over the Mu-Opioid Receptor In Vitro and In Vivo.

Li Mengchu M, Zhang Sherrice S, Powell Alexander J AJ, Stewart Hannah C HC et al.

Positive allosteric modulators (PAMs) of the delta-opioid receptor (DOR) enhance endogenous opioid signaling while avoiding the convulsant liability of orthosteric agonists. However, the prototypical DOR-PAM, BMS-986187, also potentiates mu-opioid receptor (MOR) signaling, raising concerns regarding respiratory depression and abuse liability. Here, we report a structure-activity study of the benzyloxy moiety of BMS-986187 to improve selectivity for DOR over MOR, while retaining DOR-PAM potency. Fifty-two new analogues and 12 previously reported ones featuring mono- and disubstitution of the benzyl ring and phenyl-heterocycle replacements were synthesized and evaluated in β-arrestin2 recruitment assays. Ortho-substituted derivatives consistently enhanced DOR-PAM potency, although often increased MOR-PAM activity. One pyridyl derivative (compound 35) retained high DOR-PAM potency and efficacy (EC50 = 0.1 μM, Emax = 91%) with no detectable MOR activity. In mice, compound 35 enhanced DOR-mediated reversal of nitroglycerin-induced hyperalgesia, an effect absent in DOR-knockout mice, without enhancing MOR-mediated antinociception, demonstrating in vivo selectivity.

PMID 42720491
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PubMedInternational journal of women's health2026-09-10

Achieving Minimal-to-No Pain in Women with Endometriosis Treated with Relugolix Combination Therapy: SPIRIT Extension Trial.

Lukes Andrea S AS, Venturella Roberta R, Dynowski Krzysztof K, Wagman Rachel B RB et al.

Relugolix is an oral, non-peptide gonadotropin-releasing hormone receptor antagonist administered as once-daily combination therapy (relugolix-CT; 40 mg relugolix, 1 mg estradiol, 0.5 mg norethindrone acetate) to reduce endometriosis symptoms while potentially minimizing hypoestrogenic effects. In the 24-week SPIRIT1&2 studies, relugolix-CT significantly improved endometriosis-associated pain versus placebo, with improvements sustained over the 80-week open-label Long-Term Extension (LTE; all received relugolix-CT). This post hoc analysis of SPIRIT1, 2 and LTE data assessed temporal effects of relugolix-CT on minimal-to-no pain, amenorrhea, and analgesic-free status. This analysis included women who received relugolix-CT, delayed relugolix-CT, or placebo in SPIRIT 1 or 2 and entered the LTE. Cumulative probability and median time to minimal-to-no pain for dysmenorrhea and non-menstrual pelvic pain (NMPP), amenorrhea, and analgesic-free status were assessed. In SPIRIT1&2, 802/1261 women entered the LTE; 501/802 completed 104-week treatment. Median time to minimal-to-no pain for dysmenorrhea was 8 weeks for relugolix-CT and delayed relugolix-CT and was not reached with placebo within 24 weeks; cumulative probability of minimal-to-no dysmenorrhea at Week 24 was 82.5%, 86.4%, and 22.4%, respectively, increasing to 95.3%, 95.9%, and 94.9% at Week 104. Amenorrhea paralleled dysmenorrhea. Median time to minimal-to-no NMPP was 32, 28, and 40 weeks in the relugolix-CT, delayed relugolix-CT, and placebo groups, respectively; cumulative probability of minimal-to-no NMPP was 42.6%, 42.2%, and 28.9% at Week 24, increasing to 70.5%, 74.7%, and 74.3% at Week 104. In the relugolix-CT group, median time to analgesic-free status was 16 weeks; 68.8% and 94.9% were analgesic-free at Weeks 24 and 104. Delayed relugolix-CT results were similar. Analgesic-free status improved in the placebo group after relugolix-CT initiation. In this post hoc analysis, women receiving relugolix-CT for up to 104 weeks had rapid dysmenorrhea improvement with amenorrhea and reduced analgesic use, with longer treatment associated with further NMPP reduction.

PMID 42719373
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