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Drug: Tamoxifen

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Total 112 results found since Jan 2013.

GSE106695 GRHL2 is a key lineage determining factor which collaborates with FOXA1 to establish a targetable collateral pathway in the setting of endocrine therapy-resistant breast cancer
Series Type : Expression profiling by high throughput sequencingOrganism : Homo sapiensThe estrogen receptor (ER) is expressed in the majority of luminal breast cancers and inhibition of its transcriptional activity with selective estrogen receptor modulators, selective estrogen receptor degraders and/or aromatase inhibitors is a standard approach used in the management of this disease. Despite the positive clinical impact of these interventions, de novo and acquired resistance limits the therapeutic lifespan of these classes of drugs. Considering what is known about the complex mechanisms that contribute to the developmen...
Source: GEO: Gene Expression Omnibus - November 20, 2017 Category: Genetics & Stem Cells Tags: Expression profiling by high throughput sequencing Homo sapiens Source Type: research

GSE106694 GRHL2 is a key lineage determining factor which collaborates with FOXA1 to establish a targetable collateral pathway in the setting of endocrine therapy-resistant breast cancer (RNA-Seq data set 2)
Contributors : Jeff S Jasper ; Kimberly J Cocce ; Logan Everett ; Suzanne Wardell ; Thomas Westerling ; Taylor Krebs ; Robert Baldi ; Tricia M Wright ; Alex Yllanes ; Jeremy T Blitzer ; Craig Logsdon ; Daniel Rakiec ; David Ruddy ; Terry Hyslop ; Allison Hall ; Jeffrey R Marks ; Gregory E Crawford ; Myles Brown ; Donald P McdonnellSeries Type : Expression profiling by high throughput sequencingOrganism : Homo sapiensThe estrogen receptor (ER) is expressed in the majority of luminal breast cancers and inhibition of its transcriptional activity with selective estrogen receptor modulators, selective estrogen receptor degrader...
Source: GEO: Gene Expression Omnibus - November 20, 2017 Category: Genetics & Stem Cells Tags: Expression profiling by high throughput sequencing Homo sapiens Source Type: research

GSE106681 GRHL2 is a key lineage determining factor which collaborates with FOXA1 to establish a targetable collateral pathway in the setting of endocrine therapy-resistant breast cancer (RNA-Seq data set 1)
Contributors : Jeff S Jasper ; Kimberly J Cocce ; Logan Everett ; Suzanne Wardell ; Thomas Westerling ; Taylor Krebs ; Robert Baldi ; Tricia M Wright ; Alex Yllanes ; Jeremy T Blitzer ; Craig Logsdon ; Daniel Rakiec ; David Ruddy ; Terry Hyslop ; Allison Hall ; Jeffrey R Marks ; Gregory E Crawford ; Myles Brown ; Donald P McdonnellSeries Type : Expression profiling by high throughput sequencingOrganism : Homo sapiensThe estrogen receptor (ER) is expressed in the majority of luminal breast cancers and inhibition of its transcriptional activity with selective estrogen receptor modulators, selective estrogen receptor degrader...
Source: GEO: Gene Expression Omnibus - November 20, 2017 Category: Genetics & Stem Cells Tags: Expression profiling by high throughput sequencing Homo sapiens Source Type: research

Nonsteroidal estrogen receptor isoform ‐selective biphenyls
Estrogen receptor (ER) has been a therapeutic target to treat ER‐positive breast cancer, most notably by agents known as selective estrogen receptor modulators (SERMs). However, resistance and severe adverse effects of known drugs gave impetus to the search for newer agents with better therapeutic profile. ERα and ERβ are two isoforms sharing 56% identity and having different physiological functions and expressions in various tissues. Only two residues differ in the active sites of the two isoforms motivating us to design isoform‐selective ligands. Guided by computational docking and molecular dynamics simulations, w...
Source: Chemical Biology and Drug Design - November 10, 2017 Category: Biology Authors: Seema Bhatnagar, Anjali Soni, Swati Kaushik, Megha Rikhi, Thankayyan Retnabai Santhoshkumar, Bhyravabhotla Jayaram Tags: RESEARCH ARTICLE Source Type: research

Non ‐steroidal Estrogen Receptor Isoform Selective Biphenyls
This article is protected by copyright. All rights reserved. Novel substituted biphenyl‐2,6‐diethanones are designed and synthesized targeting ERα isoform. MD simulations along with MM‐GBSA accounted for the binding selectivity of 3b towards ERα over ERβ. Co‐treatment and E‐screen studies indicated the ERα selective nature of 3b and anti‐estrogenicity. ERα siRNA silencing experiments further confirmed the isoform selectivity.
Source: Chemical Biology and Drug Design - October 20, 2017 Category: Biology Authors: Seema Bhatnagar, Anjali Soni, Swati Kaushik, Megha Rikhi, T R Santhosh Kumar, B. Jayaram Tags: Research Article Source Type: research

Knockdown of PINCH-1 protein sensitizes the Estrogen positive breast cancer cells to chemotherapy induced apoptosis
Conclusion The results suggest that PINCH-1 may be playing an important role in etiopathogenesis of both subtypes breast cancer. However, enhanced apoptosis observed only in estrogen positive and not in estrogen negative cells upon PINCH-1 knockdown point towards participation of some other protein with redundant functions in the later subtype which needs to be investigated.
Source: Pathology Research and Practice - September 30, 2017 Category: Pathology Source Type: research

The activation of the G protein-coupled estrogen receptor (GPER) inhibits the proliferation of mouse melanoma K1735-M2 cells
Publication date: Available online 22 September 2017 Source:Chemico-Biological Interactions Author(s): Mariana P.C. Ribeiro, Armanda E. Santos, José B.A. Custódio The activation of the G protein-coupled estrogen receptor (GPER) by its specific agonist G-1 inhibits prostate cancer and 17β-estradiol-stimulated breast cancer cell proliferation. Tamoxifen (TAM), which also activates the GPER, decreases melanoma cell proliferation, but its action mechanism remains controversial. Here we investigated the expression and the effects of GPER activation by G-1, TAM and its key metabolite endoxifen (EDX) on melanoma cells. Mouse ...
Source: Chemico Biological Interactions - September 22, 2017 Category: Biochemistry Source Type: research

The activation of the G protein-coupled estrogen receptor (GPER) inhibits the proliferation of mouse melanoma K1735-M2 cells.
Abstract The activation of the G protein-coupled estrogen receptor (GPER) by its specific agonist G-1 inhibits prostate cancer and 17β-estradiol-stimulated breast cancer cell proliferation. Tamoxifen (TAM), which also activates the GPER, decreases melanoma cell proliferation, but its action mechanism remains controversial. Here we investigated the expression and the effects of GPER activation by G-1, TAM and its key metabolite endoxifen (EDX) on melanoma cells. Mouse melanoma K1735-M2 cells expressed GPER and G-1 reduced cell biomass, and the number of viable cells, without increasing cell death. Rather, G-1 decr...
Source: Chemico-Biological Interactions - September 22, 2017 Category: Molecular Biology Authors: Ribeiro MPC, Santos AE, Custódio JBA Tags: Chem Biol Interact Source Type: research

Williams syndrome transcription factor (WSTF) acts as an activator of estrogen receptor signaling in breast cancer cells and the effect can be abrogated by 1 α,25-dihydroxyvitamin D3
This study reports a novel transcription factor critical to 1α,25-dihydroxyvitamin D3-mediated regulation of estrogenic signaling in MCF-7 breast cancer cells. We have investigated the molecular mechanisms for the 1α,25-dihydroxyvitamin D3-mediated down-regulation of CYP19A1 and ERα gene expression in human MCF-7 breast cancer cells and found that Williams syndrome transcription factor (WSTF) plays a key role by binding to the promoters of CYP19A1 and ERα. Although sometimes reported as an inhibitor of gene expression, we found that WSTF acts as an activator of the promoter activity of both CYP19A1 and ERα. Silencing ...
Source: The Journal of Steroid Biochemistry and Molecular Biology - June 11, 2017 Category: Biochemistry Source Type: research

Abstract P3-04-12: Both spliced and unspliced XBP1 regulates breast cancer cell fate response to antiestrogen via NFkappaB signaling
Unfolded protein response (UPR), a stress-induced survival mechanism, may be used by cancer cells to avoid cell death. Antiestrogen therapy, widely applied in the treatment of estrogen receptor-positive (ER+) breast cancer, induces endoplasmic reticulum stress (EnR stress) that leads to activation of each of the three arms of the UPR. One critical prosurvival activator that is regulated by two arms of the UPR is the transcription factor X-box binding protein 1 (XBP1). XBP1 exists in two isoforms, the transcriptionally inactive unspliced XBP1(U) and the spliced, active XBP1(S). Overexpression of XBP1(S) confers estrogen ind...
Source: Cancer Research - February 28, 2017 Category: Cancer & Oncology Authors: R Clarke, R Hu, A Warri, L Jin, A Zwart, R Riggins, H-b Fang Tags: Poster Session Abstracts Source Type: research

Abstract P3-10-04: Disparities in human epidermal growth factor receptor 2 testing completion: A population-based retrospective cohort study, 2010-2013
Unfolded protein response (UPR), a stress-induced survival mechanism, may be used by cancer cells to avoid cell death. Antiestrogen therapy, widely applied in the treatment of estrogen receptor-positive (ER+) breast cancer, induces endoplasmic reticulum stress (EnR stress) that leads to activation of each of the three arms of the UPR. One critical prosurvival activator that is regulated by two arms of the UPR is the transcription factor X-box binding protein 1 (XBP1). XBP1 exists in two isoforms, the transcriptionally inactive unspliced XBP1(U) and the spliced, active XBP1(S). Overexpression of XBP1(S) confers estrogen ind...
Source: Cancer Research - February 13, 2017 Category: Cancer & Oncology Authors: MC Schroeder, JM Neuner, C Xia, A Thomas Tags: Poster Session Abstracts Source Type: research

Abstract P1-08-03: Identification and characterization of a novel endoxifen substrate, PKC{beta}1, and its interaction with the estrogen receptor
Conclusions: Our findings demonstrated that endoxifen binds and inhibits PKCβ1 at relevant concentrations achieved in the endoxifen clinical trial studies. PKCβ1 interacts with cytoplasmic ERα and PKCβ1 knockdown inhibits cell proliferation and enhances ERα turnover. However, in PKCβ1 overexpressing cells, PKCβ1 may exhibit tumor suppressive effects. These data suggest a complex interaction between PKCβ1 and ERα and that endoxifen's effects on PKCβ1 may alter drug response of endocrine therapy. Further studies are ongoing to characterize the role of PKCβ1 and its role in ER biology and response to endoxifen.Cita...
Source: Cancer Research - February 13, 2017 Category: Cancer & Oncology Authors: C Guo, MJ Kuffel, RA Kudgus, Z Huang, AM Bode, J Cheng, VJ Suman, JM Reid, ES Bruinsma, M Subramaniam, MM Ames, JR Hawse, MP Goetz Tags: Poster Session Abstracts Source Type: research

Abstract P4-10-02: Transmembrane protein 33 (TMEM33) induces apoptosis via UPR signaling and autophagy in breast cancer cells
Conclusions: Our findings demonstrated that endoxifen binds and inhibits PKCβ1 at relevant concentrations achieved in the endoxifen clinical trial studies. PKCβ1 interacts with cytoplasmic ERα and PKCβ1 knockdown inhibits cell proliferation and enhances ERα turnover. However, in PKCβ1 overexpressing cells, PKCβ1 may exhibit tumor suppressive effects. These data suggest a complex interaction between PKCβ1 and ERα and that endoxifen's effects on PKCβ1 may alter drug response of endocrine therapy. Further studies are ongoing to characterize the role of PKCβ1 and its role in ER biology and response to endoxifen.Cita...
Source: Cancer Research - February 13, 2017 Category: Cancer & Oncology Authors: R Clarke, R Hu, X Zhang, L Hilakivi-Clarke, U Kasid Tags: Poster Session Abstracts Source Type: research

Effects of long noncoding RNA-ROR on tamoxifen resistance of breast cancer cells by regulating microRNA-205
ConclusionIn MDA-MB-231 cells, down-regulated lncRNA-ROR could inhibit the EMT of breast cancer cells and enhance the sensibility of breast cancer cells to tamoxifen by increasing miR-205 expression and suppressing the expressions of ZEB1 and ZEB2.
Source: Cancer Chemotherapy and Pharmacology - January 5, 2017 Category: Cancer & Oncology Source Type: research

MiR-148a and miR-152 reduce tamoxifen resistance in ER+ breast cancer via downregulating ALCAM.
In this study, we studied the association between ALCAM expression and tamoxifen resistance in ER + breast cancer and further investigated how ALCAM is regulated in the cancer cells. IHC staining data showed that the tumor tissues from non-responders (N = 20) generally had significantly stronger ALCAM staining than that from tamoxifen responders (N = 16). In vitro cell assay also confirmed ALCAM upregulation in tamoxifen resistant (TamR) MCF-7 cells than in tamoxifen sensitive (TamS) MCF-7 cells. ALCAM overexpression significantly alleviated 4-Hydroxytestosterone (4-OHT) induced cell viability inhibition and cell a...
Source: Biochemical and Biophysical Research communications - January 3, 2017 Category: Biochemistry Authors: Chen MJ, Cheng YM, Chen CC, Chen YC, Shen CJ Tags: Biochem Biophys Res Commun Source Type: research