Showing 1-30 of 105 results for "M6383"
N Klauber et al.
Cancer research, 57(1), 81-86 (1997-01-01)
2-Methoxyestradiol (2-ME), an endogenous estrogen metabolite which disrupts microtubule function, has been shown to inhibit proliferating cells in vitro and suppress certain murine tumors in vivo. In vitro screening has determined that breast cancer cell lines are most sensitive to...
Low catechol-O-methyltransferase and 2-methoxyestradiol in preeclampsia: more than a unifying hypothesis.
Duska Dragun et al.
Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association, 24(1), 31-33 (2008-11-29)
B T Zhu et al.
Cancer research, 58(11), 2269-2277 (1998-06-11)
Catechol estrogens (2- or 4-hydroxyestradiol and 2- or 4-hydroxyestrone) are chemically reactive estrogen metabolites that are O-methylated to less polar monomethyl ethers by catechol-O-methyltransferase, an enzyme present in many tissues such as the liver, kidney, brain, placenta, uterus, and mammary...
Purab Pal et al.
Journal of ovarian research, 12(1), 49-49 (2019-05-28)
We have previously shown that a whole flaxseed supplemented diet decreased the onset and severity of ovarian cancer in the laying hen, the only known animal model of spontaneous ovarian cancer. Flaxseed is rich in omega-3 fatty acids (OM3FA), mostly...
Yun Hua et al.
Assay and drug development technologies, 12(7), 395-418 (2014-09-03)
The androgen receptor-transcriptional intermediary factor 2 (AR-TIF2) positional protein-protein interaction (PPI) biosensor assay described herein combines physiologically relevant cell-based assays with the specificity of binding assays by incorporating structural information of AR and TIF2 functional domains along with intracellular targeting...
Guodong Wang et al.
Oncology reports, 30(1), 357-363 (2013-05-16)
Lack of effective treatment options for castration-resistant prostate cancer reinforces the great need to develop novel drug therapies. Quercetin is a plant-derived flavonoid that can induce apoptosis in prostate cancer cells. 2-Methoxyestradiol (2-ME) is an endogenous estrogenic metabolite that also...
Jamshed H Shah et al.
Bioorganic & medicinal chemistry, 17(20), 7344-7352 (2009-09-19)
A novel series of 17-modified and 2,17-modified analogs of 2-methoxyestradiol (2ME2) were synthesized and characterized. These analogs were designed to retain or potentiate the biological activities of 2ME2 and have diminished metabolic liability. The analogs were evaluated for antiproliferative activity...
Michael Bonham et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 11(10), 3905-3914 (2005-05-18)
Botanical preparations are widely used by patients with prostate cancer. Scutellaria baicalensis, a botanical with a long history of medicinal use in China, was a constituent of the herbal mixture PC-SPES, a product that inhibited prostate cancer growth in both...
G Schumacher et al.
Journal of cancer research and clinical oncology, 127(7), 405-410 (2001-07-27)
2-Methoxyestradiol (2-ME) is a physiological metabolite of estrogen, which is excreted with the urine. In contrast to most estrogens, tumor growth-inhibiting effects were observed. Further studies have revealed that it may be an effective anticancer compound for many tumor types....
Zhong Wang et al.
Journal of molecular neuroscience : MN, 48(1), 273-280 (2012-04-25)
The current research aimed to investigate the role of hypoxia-inducible factor-1α (HIF-1α), aquaporin-4 (AQP-4), and matrix metalloproteinase-9 (MMP-9) in blood-brain barrier (BBB) dysfunction and cerebral edema formation in a rat subarachnoid hemorrhage (SAH) model. The SAH model was induced by...
Lita S Suwandi et al.
Bioorganic & medicinal chemistry letters, 19(22), 6459-6462 (2009-09-29)
The syntheses of 2-methoxyestradiol analogs with modifications at the 3-position are described. The analogs were assessed for their antiproliferative, antiangiogenic, and estrogenic activities. Several lead substituents were identified with similar or improved antitumor activities and reduced metabolic liability compared to...
Jing Yuan et al.
Nature chemical biology, 5(10), 765-771 (2009-09-08)
Studies of gene function and molecular mechanisms in Plasmodium falciparum are hampered by difficulties in characterizing and measuring phenotypic differences between individual parasites. We screened seven parasite lines for differences in responses to 1,279 bioactive chemicals. Hundreds of compounds were...
Hazem Ali et al.
Therapeutic delivery, 4(2), 161-175 (2013-01-25)
The purpose of this work was to engineer polymeric nanoparticles to encapsulate and deliver 2-methoxyestradiol, a potential antitumor drug for treatment of uterine leiomyoma (fibroids), the most common hormone-dependent pathology affecting women of reproductive age. Encapsulation efficiency and drug release...
Susan L Mooberry
Current opinion in oncology, 15(6), 425-430 (2003-11-19)
2-Methoxyestradiol (2ME2) is a natural metabolite of estradiol with antiangiogenic and antitumor activities. The ability of 2ME2 to target both tumor cells and neovasculature in preclinical models led to ongoing evaluations of 2ME2 in clinical trials. This brief review focuses...
Mohammed Shenaq et al.
Journal of the neurological sciences, 323(1-2), 134-140 (2012-10-09)
The present study, using a rodent model of closed-head diffuse traumatic brain injury (TBI), investigated the role of dysregulated aquaporins (AQP) 4 and 9, as well as hypoxia inducible factor -1α(HIF-1α) on brain edema formation, neuronal injury, and functional deficits....
Aleem Gangjee et al.
Journal of medicinal chemistry, 53(22), 8116-8128 (2010-10-27)
Two classes of molecules were designed and synthesized based on a 6-CH(3) cyclopenta[d]pyrimidine scaffold and a pyrrolo[2,3-d]pyrimidine scaffold. The pyrrolo[2,3-d]pyrimidines were synthesized by reacting ethyl 2-cyano-4,4-diethoxybutanoate and acetamidine, which in turn was chlorinated and reacted with the appropriate anilines to...
Yi-Lin Cheng et al.
Neurobiology of disease, 62, 286-295 (2013-10-22)
Recent findings suggest that Notch-1 signaling contributes to neuronal death in ischemic stroke, but the underlying mechanisms are unknown. Hypoxia inducible factor-1α (HIF-1α), a global regulator of cellular responses to hypoxia, can interact with Notch and modulate its signaling during...
G Schumacher et al.
Deutsche medizinische Wochenschrift (1946), 131(15), 825-830 (2006-04-12)
2-Methoxyestradiol (2-ME2), a physiological metabolite of estrogen, inhibits the growth of different tumor types. Many mechanisms of action have been described. In addition to a strong antiangiogenic effect and induction of apoptosis, there are other important mechanisms, such as the...
R K Dubey et al.
Hypertension (Dallas, Tex. : 1979), 31(1 Pt 2), 522-528 (1998-02-07)
Postmenopausal women (PMW) have increased incidence of cardiovascular disease, and estrogen substitution therapy has been shown to have cardioprotective effects. Since abnormal growth of cardiac fibroblasts (CFs) is associated with hypertension and myocardial infarction and estrogen inhibits vascular smooth muscle...
Allison B Edsall et al.
Journal of medicinal chemistry, 50(26), 6700-6705 (2007-12-07)
A prodrug strategy was investigated to address the problem of limited aqueous solubility and the resulting limited bioavailability of the antitumor agent 2-methoxyestradiol. The 3-phosphate, 17-phosphate, and 3,17-diphosphate of 2-methoxyestradiol were synthesized. 2-methoxyestradiol 3-phosphate was metabolized more efficiently to the...
Alejandra Perez-Sepulveda et al.
Reproductive sciences (Thousand Oaks, Calif.), 20(9), 1020-1029 (2013-03-05)
Preeclampsia (PE) remains a major cause of maternal/fetal morbidity-mortality worldwide. The first stage of PE is characterized by placental hypoxia due to a relative reduction in uteroplacental blood flow, resulting from restricted trophoblast invasion. However, hypoxia is also an essential...
Raghvendra K Dubey et al.
Trends in endocrinology and metabolism: TEM, 20(8), 374-379 (2009-09-08)
2-Methoxyestradiol (2-ME) is a biologically active metabolite of 17beta-estradiol that appears to inhibit key processes associated with cell replication in vitro. The molecule has been suggested to have potent growth-inhibitory effects on proliferating cells, including smooth muscle cells and endothelial...
Wenjie Qin et al.
Oncotarget, 6(37), 39839-39854 (2015-10-27)
Autophagy defect has been shown to be correlated with malignant phenotype and poor prognosis of human cancers, however, the detailed mechanisms remain obscure. In this study, we investigated the biological changes induced by autophagy inhibition in gastric cancer. We showed...
Xinhong Guo et al.
Drug delivery, 19(3), 143-148 (2012-03-21)
Injectable implant would be a potential way for 2-methoxyestradiol (2-ME) for the therapy of breast cancer because of its water-insolubility, short half-life, and low oral bioavailability. So 2-ME microspheres based on poly (DL-lactide-co-glycolide) were prepared by emulsion solvent extraction method...
David Chetrit et al.
The Journal of biological chemistry, 286(7), 5392-5403 (2010-11-26)
Mitotic cells undergo extensive changes in shape and size through the altered regulation and function of their membrane trafficking machinery. Disabled 2 (Dab2), a multidomain cargo-specific endocytic adaptor and a mediator of signal transduction, is a potential integrator of trafficking...
Wensu Yuan et al.
Cardiovascular drugs and therapy, 27(1), 17-22 (2012-12-12)
Our early work showed that the estrogen metabolite 2-methoxyestradiol (2ME) inhibits proliferation of vascular smooth muscle cells (SMCs) and vascular contractility through an endothelium-dependent mechanism. The aim of this study was to examine whether 2ME prevents the development of hypertension...
Franck Belibi et al.
American journal of physiology. Renal physiology, 300(5), F1235-F1243 (2011-01-29)
Cyst expansion in polycystic kidney disease (PKD) results in localized hypoxia in the kidney that may activate hypoxia-inducible factor-1α (HIF-1α). HIF-1α and autophagy, a form of programmed cell repair, are induced by hypoxia. The purposes were to determine HIF-1α expression...
Hsu-Tung Lee et al.
Theranostics, 7(4), 855-875 (2017-04-07)
Inflammatory processes have a detrimental role in the pathophysiology of ischemic stroke. However, little is known about the endogenous anti-inflammatory mechanisms in ischemic brain. Here, we identify CXCL14 as a critical mediator of these mechanisms. CXCL14 levels were upregulated in...
The effect of steroid hormones on ovarian follicle development
Vitamins and Hormones, 107, 155-175 (2018)
Paulina Kohen et al.
Fertility and sterility, 100(5), 1397-1404 (2013-08-21)
To quantitate 2-methoxyestradiol (2-ME) in human corpus luteum (CL) of different ages and to determine the expression of cytochrome-P450-1A1 (CYP1A1) and catechol-O-methyl transferase (COMT) in CL and the action of 2-ME on P, vascular endothelial growth factor (VEGF) secretion, and...

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