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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
来源： ClinicalTrials.gov, Johnson & Johnson Services, Inc.

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

PubMedCells2026-10-26

Selective Estradiol Sensitivity in 12Z Human Endometriotic Epithelial Cell Line.

Banerjee Shohini S, Chopra Esha E, Smith Ian M IM, Stroka Kimberly M KM

Estradiol (E2) is a potent estrogen molecule that plays a crucial role in regulating numerous healthy and pathophysiological processes. To model estrogen-dependent cellular activities in vitro in a physiologically meaningful way, cells chosen for experimentation should exhibit sensitivity to E2. The 12Z human endometriotic epithelial cell line is gaining attention as a model for estrogen-dependent conditions, but its functional responsiveness to E2 has not been well characterized. For the passage range in the following study, we found that E2 does not statistically significantly influence 12Z proliferation, wound closure, or single-cell migration. However, 12Zs were selectively responsive to E2 in 3D migration models where the cells were physically confined. Upregulating ESR1, the primary mediator of estrogenic action, in the 12Zs did not enhance their functional E2 sensitivity. These results highlight the importance of verifying hormone responsiveness when using 12Z cells to model estrogen-dependent processes and conditions.

PMID 42929847
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PubMedInternational journal of fertility & sterility2026-10-26

Treatment Approach to Disseminated Peritoneal Leiomyomatosis in A Patient Desiring Future Fertility: A Case Report.

Neal Samantha E SE, Ryles Hannah T HT, Koomson Christabel C, Madueke-Laveaux Obianuju Sandra OS et al.

Disseminated peritoneal leiomyomatosis (DPL) is a rare condition in which fibroids diffusely grow in extrauterine locations. Given its low prevalence, the literature is limited, making evidence-based treatment particularly challenging, especially in premenopausal patients. This case report describes a 34-year-old nulligravid woman with a history of two prior myomectomies who presented with upper abdominal bulk symptoms. Abdominal and pelvic magnetic resonance imaging (MRI) revealed multiple mesenteric and omental masses concerning for recurrent DPL. She underwent exploratory laparotomy with removal of 13 abdominal fibroids ranging from 2 to 12 cm. Postoperatively, her symptoms improved, and she was treated with a gonadotropin-releasing hormone (GnRH) analog (relugolix/estradiol/ norethindrone acetate) with a favorable response and sustained remission on follow up. Our case report demonstrates the efficacy of a novel medical therapy and our scoping review highlights the importance of aggressive surgical management followed by medical therapy for the treatment of DPL in patients with future fertility desires.

PMID 42929007
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PubMedAdvanced science (Weinheim, Baden-Wurttemberg, Germany)2026-10-26

Plasma Membrane Lipid Asymmetry Dynamically Regulates Passive Diffusion.

Ping Jieming J, Wang Wenliang W, Xu Jinnuo J, Yang Mengyun M et al.

Plasma membrane (PM) phospholipid asymmetry is a fundamental feature of eukaryotic cells that regulates signaling, trafficking, and cell fate. Whether it also controls passive diffusion across the PM remains unknown. Here, we show that phospholipid asymmetry is a critical determinant of PM permeability to hydrophobic molecules. Using genetic and biochemical approaches, we demonstrate that disruption of lipid asymmetry by the Ca2 +-activated scramblase TMEM16F or apoptotic scramblase XKR8 profoundly alters the permeation and intracellular accumulation of diverse hydrophobic compounds, including widely used fluorescent probes, while preserving the barrier to membrane-impermeable molecules. Lipid scrambling is sufficient to remodel membrane permeability to lipophilic molecules, alter membrane biophysical properties, and differentially affect their intracellular accumulation, suggesting selective regulation of passive diffusion rather than nonspecific membrane leakage. Physiological lipid scrambling during T cell activation was also accompanied by altered membrane permeability. Moreover, lipid asymmetry regulates the cellular entry of doxorubicin, 17β-estradiol, and all-trans retinoic acid. Together, our findings identify PM lipid asymmetry as a previously unrecognized regulator of membrane permeability and establish a link between membrane organization and molecular transport.

PMID 42928505
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PubMedPeerJ2026-10-26

In vitro evaluation of N-acetylcysteine, calcium hydroxide, chlorhexidine digluconate and their combinations effect against five dental obligate anaerobic bacteria.

de Carvalho Lara Steffany LS, de Oliveira Júlia Andrade JA, Cezarino Gabriel Manente GM, Dos Santos Luiz Augusto Rodrigues LAR et al.

This study aimed to evaluate the antibacterial action of N-acetylcysteine (NAC), calcium hydroxide Ca(OH)2, chlorhexidine digluconate (CHX), and their combinations against five obligate anaerobic bacteria including Fusobacterium nucleatum, Porphyromonas endodontalis, Porphyromonas gingivalis, Prevotella intermedia, and Parvimonas micra in planktonic and biofilm forms. Eight experimental groups were evaluated in this study including saline solution (SS) (control group), Ca(OH)2, CHX, NAC, NAC + Ca(OH)2, NAC + CHX, Ca(OH)2 + CHX, and NAC + Ca(OH)2 + CHX. The anti-planktonic evaluation was performed by determination of minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) following Clinical and Laboratory Standards Institute guidelines (CLSI M11). The antibiofilm was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and crystal violet (CV) assays. Data were analyzed statistically considering a significant level of (α ≤ 0.05). It was found that the MIC and MBC values of the tested intracanal medications ranged from 1.95-500 mg/mL. MTT and CV assays showed significant, species-dependent antibiofilm activity. CHX was most effective against F. nucleatum; NAC-based medications, especially combined with Ca(OH)2 and/or CHX, were superior against P. endodontalis, P. intermedia, and P. micra. Ca(OH)2-containing groups were particularly effective against P. gingivalis. Therefore, NAC + Ca(OH)2 and NAC + Ca(OH)2 + CHX can be considered as effective combinations of intracanal medication against different obligate anaerobic bacteria.

PMID 42928779
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PubMedG3 (Bethesda, Md.)2026-10-26

Evaluation of Trialling Efficiency of the Australian Wheatbelt.

Arief Vivi V, Ramakers Jip J C JJC, Fernandez Javier J, Boer Martin P MP et al.

The Australian wheatbelt is divided into three main growing regions: the North (New South Wales and Queensland), the South (Victoria, South Australia and Tasmania), and the West (Western Australia). Using wheat yield data from the 2015-2022 multi-environmental trials (METs) conducted by the National Variety Trials (NVT), this study examines genotype-by-environment interactions (G×E) and trialling efficiencies, within and across regions. The North had the highest mean yield (390 gm-2) and the largest proportion of phenotypic variance explained by G×E (64%), while the West had the lowest yield (355 gm-2) and the lowest G×E contribution (44%). Despite regional differences, yield gains were approximately 1.4 gm-2 per year (or ∼ 0.5% annually) across all regions. The West also showed the highest repeatability (0.85 ± 0.02) and the lowest least significance difference (5% LSD, 22 gm-2 ± 1 gm-2) for a benchmark five-year MET, compared to the South (0.70 ± 0.04, 35 ± 1.4 gm-2) and the North (0.59 ± 0.05, 35 ± 1.4 gm-2). Modelling results were consistent across regions and indicated that 2 years of testing at 20 sites per year delivered efficiencies that could not be improved very much further.

PMID 42928464
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PubMedThe New phytologist2026-10-26

Phosphatidylcholine acyl turnover facilitates thylakoid lipid remodeling and promotes plant survival under heat stress.

Xie Dongling D, Wang Shasha S, Fan Jilian J, Xu Changcheng C

Heat stress destabilizes chloroplast membranes, requiring rapid lipid remodeling to maintain photosynthetic function. Although thylakoid lipid remodeling and triacylglycerol (TAG) accumulation are established heat responses, the role of phosphatidylcholine (PC) acyl turnover remains unclear. We investigated lysophosphatidylcholine acyltransferase 1 and 2 (LPCAT1/2), REDUCED OLEATE DESATURATION1 (ROD1), phospholipid:diacylglycerol acyltransferase 1 (PDAT1), and lipins in heat-induced lipid remodeling and thermotolerance in Arabidopsis thaliana. Using genetic, lipidomic, physiological, and photosynthetic analyses, we examined mutants defective in PC acyl editing, PC-diacylglycerol (DAG) interconversion, TAG synthesis, and phosphatidic acid dephosphorylation during heat stress. Loss of LPCAT1/2 severely impaired basal and acquired thermotolerance, caused irreversible photosystem II damage, and disrupted thylakoid lipid remodeling. rod1 showed minor defects, whereas rod1 lpcat1/2 exhibited enhanced thermosensitivity. In mature vegetative plants, pdat1-2 showed thermotolerance and photosystem II defects comparable to lpcat1/2. Lipin-mediated phosphatidic acid dephosphorylation provided the major DAG source for heat-induced TAG synthesis. Defective PC acyl turnover also increased free fatty acids and lipid peroxidation. These findings establish LPCAT1/2-mediated PC acyl turnover as a central regulator of heat-induced membrane remodeling and thermotolerance and link lipin-dependent DAG production and TAG synthesis with chloroplast membrane homeostasis.

PMID 42928459
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