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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

Over-expression of miR-451a can enhance the sensitivity of breast cancer cells to tamoxifen by regulating 14-3-3ζ, estrogen receptor α, and autophagy
Publication date: Available online 17 February 2016 Source:Life Sciences Author(s): Zhen-Ru Liu, Yi Song, Li-Hong Wan, Yuan-Yuan Zhang, Li-Mimg Zhou Aim To investigate the effects and mechanisms of miR-451a in the tamoxifen (TAM) resistance of breast cancer cells. Materials and methods TAM sensitive cells (MCF-7) and resistant cells (LCC2) were employed in the study. The lentivirus vectors of Lv-miR-451a, Lv-miR-451a sponge, and Lv-miR-451a NC were employed to increase or decrease the expression of miR-451a, respectively. SiRNA to 14-3-3ζ was used to inhibit expression of 14-3-3ζ. MTT assay was utilized to detect...
Source: Life Sciences - February 18, 2016 Category: Biology Source Type: research

UCP2 inhibition sensitizes breast Cancer cells to therapeutic agents by increasing oxidative stress.
In conclusion, UCP2 could be a therapeutic target in breast cancer, especially in those patients treated with tamoxifen. PMID: 25960046 [PubMed - as supplied by publisher]
Source: Free Radical Biology and Medicine - May 7, 2015 Category: Biology Authors: Pons DG, Nadal-Serrano M, Torrens-Mas M, Valle A, Oliver J, Roca P Tags: Free Radic Biol Med Source Type: research