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Drug: Estradiol

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Total 353 results found since Jan 2013.

17 β-Estradiol activates Cl < sup > - < /sup > channels via the estrogen receptor α pathway in human thyroid cells
In this study, the effects of estrogen on chloride channel activities in human thyroid Nthy-ori3-1 cells were therefore investigated using the whole cell patch-clamp technique. The results showed that the extracellular application of 17β-estradiol (E2) activated Cl- currents, which reversed at a potential close to Cl- equilibrium potential and showed remarkable outward rectification and an anion permeability of I- > Br- > Cl- > gluconate. The Cl- currents were inhibited by the chloride channel blockers, NPPB and tamoxifen. Quantitative Real-time PCR results demonstrated that ClC-3 expression was highest in ClC fa...
Source: Channels - August 20, 2021 Category: Molecular Biology Authors: Meisheng Yu Yuan Wei Yanfang Zheng Lili Yang Long Meng Jiawei Lin Peisheng Xu Sanaa Ahmed Nagi Abdu Mahdy Linyan Zhu Shuang Peng Lixin Chen Liwei Wang Source Type: research

PARP1 Regulates ER{alpha}-dependent Transcription Signal Transduction
In this study, we examined the interplay between PARP1 and ERα, and identified PARP1 as an important regulator of ERα-dependent transcription. We showed that PARP1 could directly bind to ERα, and ERα could be poly(ADP-ribosyl)ated by PARP1. Poly(ADP-ribosyl)ation increased ERα binding to estrogen response element (ERE) present in the promoter of target genes and promoted ERα-mediated gene transcription. Estradiol, the ligand of ERα, increased PARP enzymatic activity and enhanced poly(ADP-ribosyl)ation of ERα. Upon treatment with estradiol, ERα binding to ERE- and ERα-dependent gene expression was dramatically inc...
Source: Journal of Biological Chemistry - April 19, 2013 Category: Chemistry Authors: Zhang, F., Wang, Y., Wang, L., Luo, X., Huang, K., Wang, C., Du, M., Liu, F., Luo, T., Huang, D., Tags: Gene Regulation Source Type: research

4-Hydroxytamoxifen-stimulated processing of cyclin E is mediated via G protein-coupled receptor 30 (GPR30) and accompanied by enhanced migration in MCF-7 breast cancer cells.
Abstract Over-expression of cleaved cyclin E in breast tumors is closely associated with tumor progression and resistance to antiestrogens. 17β-Estradiol (E2) has been recently shown to induce cyclin E processing in breast cancer cells. Tamoxifen has been used in patients with estrogen-sensitive breast cancer, yet resistance to antiestrogens and recurrence will appear in some of the patients after its continued use. We therefore addressed possible effects of tamoxifen on the generation of cleaved cyclin E and its signal mechanism(s) in estrogen-responsive MCF-7 breast cancer cells that express both G protein-coup...
Source: Toxicology - April 25, 2013 Category: Toxicology Authors: Li Y, Chen Y, Zhu ZX, Liu XH, Yang L, Wan L, Lei TW, Wang XD Tags: Toxicology Source Type: research

Pathogen-associated molecular patterns initiate inflammation and perturb the endocrine function of bovine granulosa cells from ovarian dominant follicles via TLR2 and TLR4 pathways.
In conclusion, bacterial PAMPs initiate inflammation and perturb the endocrine function of bovine granulosa cells from dominant follicles via TLR2 and TLR4 pathways.Précis: A rapid inflammatory response to pathogen-associated molecular patterns mediated by TLR2 and TLR4 pathways in granulosa cells provides a molecular explanation of how bacterial infections distant to the ovary can perturb dominant follicle function. PMID: 23825132 [PubMed - as supplied by publisher]
Source: Endocrinology - July 3, 2013 Category: Endocrinology Authors: Price JC, Bromfield JJ, Sheldon IM Tags: Endocrinology Source Type: research

GPER mediates the inhibitory actions of estrogen on adipogenesis in 3T3-L1 cells through perturbation of mitotic clonal expansion.
Abstract G-protein-coupled estrogen receptor 1 (GPER) mediates non-genomic signaling of estrogenic events. Here we showed for the first time that Gper/GPER is expressed in Swiss 3T3 mouse embryo preadipocytes 3T3-L1, and that Gper/GPER is up-regulated during differentiation of the cells induced by monocyte differentiation-inducing (MDI) cocktail. Activation of GPER by the natural ligand 17β-estradiol (E2), and the specific agonist G1, was shown to inhibit lipid accumulation in 3T3-L1 cells, while such inhibition was reversed upon knockdown of GPER using specific siRNA. GPER was also found to mediate perturbation ...
Source: General and Comparative Endocrinology - July 17, 2013 Category: Endocrinology Authors: Zhu P, Yuen JM, Sham KW, Cheng CH Tags: Gen Comp Endocrinol Source Type: research

Granulosa Cells from Emerged Antral Follicles of the Bovine Ovary Initiate Inflammation in Response to Bacterial Pathogen-Associated Molecular Patterns via Toll-Like Receptor Pathways.
In conclusion, bovine granulosa cells from emerged follicles sense bacterial PAMPs and initiate inflammatory responses via TLR2 and TLR4 pathways. PMID: 24089202 [PubMed - as supplied by publisher]
Source: Reproductive Biology - October 2, 2013 Category: Reproduction Medicine Authors: Price JC, Sheldon IM Tags: Biol Reprod Source Type: research

Glutathione transferase mu 2 protects glioblastoma cells against aminochrome toxicity by preventing autophagy and lysosome dysfunction.
Abstract U373MG cells constitutively express glutathione S-transferase mu 2 (GSTM2) and exhibit (3)H-dopamine uptake, which is inhibited by 2 µM of nomifensine and 15 µM of estradiol. We generated a stable cell line (U373MGsiGST6) expressing an siRNA against GSTM2 that resulted in low GSTM2 expression (26% of wild-type U373MG cells). A significant increase in cell death was observed when U373MGsiGST6 cells were incubated with 50 µM purified aminochrome (18-fold increase) compared with wild-type cells. The incubation of U373MGsiGST6 cells with 75 µM aminochrome resulted in the formation of autophagic vacuoles c...
Source: Autophagy - January 14, 2014 Category: Cytology Authors: Huenchuguala S, Muñoz P, Zavala P, Villa M, Cuevas C, Ahumada U, Graumann R, Nore BF, Couve E, Mannervik B, Paris I, Segura-Aguilar J Tags: Autophagy Source Type: research

α-Mangostin-induced apoptosis is mediated by estrogen receptor α in human breast cancer cells.
In this study, we evaluated the effects of α-mangostin on cell growth inhibition and induction of apoptosis in MCF-7 ERα-positive human breast cancer cells. Our results showed that α-mangostin inhibited MCF-7 cell proliferation whereas ERα-negative MDA-MB-231 cells were less sensitive to the agent. Additionally, α-mangostin effectively induced apoptosis as evidenced by the appearance of apoptotic nuclei observed with Hoechst 33258 staining and evaluation of sub-G1 DNA contents by flow cytometry. α-Mangostin also activated caspases-8, -9, and -7; increased the protein levels of Bax, p53, and cytosolic cytochrome c; an...
Source: Food and Chemical Toxicology - January 28, 2014 Category: Food Science Authors: Won YS, Lee JH, Kwon SJ, Kim JY, Park KH, Lee MK, Seo KI Tags: Food Chem Toxicol Source Type: research

p53 inactivation decreases dependence on estrogen/ERK signalling for proliferation but promotes EMT and susceptility to 3-bromopyruvate in ERα+ breast cancer MCF-7 cells.
Conclusions.- a) ERα(+) breast cancer cells dysfunctional for TP53 which proliferate irrespective of low estrogen and chemical MEK inhibition are likely to increase metabolic consumption becoming increasingly susceptible to 3-BrPA; b) targeting the pyruvate pathway may improve response to endocrine therapy in ERα(+) breast cancer with p53 dysfunction. PMID: 24486524 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - January 28, 2014 Category: Drugs & Pharmacology Authors: Rieber M, Strasberg-Rieber M Tags: Biochem Pharmacol Source Type: research

Apoptotic effects of high estradiol concentrations on endometrial glandular cells.
Conclusions: High E2 concentrations induced EGCs apoptosis through enhancing IκB-α expression, which in turn suppressed NF-κB expression. The decreased nuclear NF-κB subsequently inhibited Bcl-2 expression and accordingly enhanced EGCs apoptosis. PMID: 24552218 [PubMed - as supplied by publisher]
Source: The Journal of Clinical Endocrinology and Metabolism - February 19, 2014 Category: Endocrinology Authors: Chen SU, Chou CH, Chen MJ, Chen TH, Yang YS, Yang JH Tags: J Clin Endocrinol Metab Source Type: research

MicroRNA Let-7a and dicer are important in the activation and implantation of delayed implanting mouse embryos
STUDY QUESTION Does Let-7a have a functional role in modulating dicer expression to activate dormant mouse blastocysts for implantation? SUMMARY ANSWER Let-7a post-transcriptionally regulates dicer expression altering microRNA expression to affect the implantation competency of the activated blastocysts. WHAT IS KNOWN ALREADY The Let-7a microRNA is up-regulated during blastocyst dormancy and its forced-expression suppresses embryo implantation in vitro and in vivo. Dicer is a Let-7 target, which processes pre-microRNA to mature microRNA. STUDY DESIGN, SIZE, DURATION The effects on the expression of Let-7a and dicer in d...
Source: Human Reproduction - March 11, 2014 Category: Reproduction Medicine Authors: Cheong, A. W. Y., Pang, R. T. K., Liu, W.-M., Kottawatta, K. S. A., Lee, K.-F., Yeung, W. S. B. Tags: Reproductive biology Source Type: research

PFKFB3 Regulation by Estradiol Metabolism
Estradiol (E2) administered to estrogen receptor-positive (ER+) breast cancer patients stimulates glucose uptake by tumors. Importantly, this E2-induced metabolic flare is predictive of the clinical effectiveness of anti-estrogens and, as a result, downstream metabolic regulators of E2 are expected to have utility as targets for the development of anti-breast cancer agents. The family of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatases (PFKFB1–4) control glycolytic flux via their product, fructose-2,6-bisphosphate (F26BP), which activates 6-phosphofructo-1-kinase (PFK-1). We postulated that E2 might promote PFKFB3 e...
Source: Journal of Biological Chemistry - March 28, 2014 Category: Chemistry Authors: Imbert-Fernandez, Y., Clem, B. F., O'Neal, J., Kerr, D. A., Spaulding, R., Lanceta, L., Clem, A. L., Telang, S., Chesney, J. Tags: Metabolism Source Type: research

Epidermal growth factor receptor signalling in human breast cancer cells operates parallel to estrogen receptor alpha signalling and results in tamoxifen insensitive proliferation
Conclusions: Our data indicate that enhanced EGFR-driven signalling is sufficient to overrule the TAM- mediated inhibition of E2-driven cell proliferation. This may have profound implications for the anti-estrogen treatment of ER-positive breast cancers that have increased levels of EGFR.
Source: BMC Cancer - April 23, 2014 Category: Cancer & Oncology Authors: Marja MoerkensYinghui ZhangLynn WesterBob van de WaterJohn Meerman Source Type: research

PCB153, TCDD and estradiol compromise the Benzoapyrene-induced p53-response via FoxO3a.
Abstract TCDD, polychlorinated biphenyls (PCB) and polycyclic aromatic hydrocarbons (PAH) coexist in the environment. However, there are few studies on combined effects of these compounds. We have studied the effect of TCDD, PCB153 and estradiol on p53 signaling induced by PAHs. We show that all three compounds amplified the accumulation of nuclear p53, elicited by benzo[a]pyrene (BaP) or dibenzo[al]pyrene (DBP). This effect was associated with an attenuated PAH-induced apoptosis and with decreased levels of phosphorylated FoxO3a Thr32. Thr32 phosphorylation of FoxO3a may promote a translocation of FoxO3a-p53 comp...
Source: Chemico-Biological Interactions - June 19, 2014 Category: Molecular Biology Authors: Al-Anati L, Kadekar S, Högberg J, Stenius U Tags: Chem Biol Interact Source Type: research

The GPR30-MAGUK-AKAP5 Complex Inhibits cAMP Production Cell Biology
GPR30, or G protein-coupled estrogen receptor, is a G protein-coupled receptor reported to bind 17β-estradiol (E2), couple to the G proteins Gs and Gi/o, and mediate non-genomic estrogenic responses. However, controversies exist regarding the receptor pharmacological profile, effector coupling, and subcellular localization. We addressed the role of the type I PDZ motif at the receptor C terminus in receptor trafficking and coupling to cAMP production in HEK293 cells and CHO cells ectopically expressing the receptor and in Madin-Darby canine kidney cells expressing the native receptor. GPR30 was localized both intracellula...
Source: Journal of Biological Chemistry - August 7, 2014 Category: Chemistry Authors: Broselid, S., Berg, K. A., Chavera, T. A., Kahn, R., Clarke, W. P., Olde, B., Leeb-Lundberg, L. M. F. Tags: Signal Transduction Source Type: research