832 results found
    1. Cancer Biology

    Breast Cancer: Targeting mutant estrogen receptors

    Suzanne E Wardell et al.
    A drug used in hormone replacement therapy can target estrogen receptors that have become resistant to breast cancer treatments.
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    1. Cancer Biology

    Estrogen receptor coregulator binding modulators (ERXs) effectively target estrogen receptor positive human breast cancers

    Ganesh V Raj et al.
    A novel first-in-class small molecule (ERX-11) that interacts with and disrupts the interactome of the estrogen receptor (ER), blocks the growth of ER-positive breast cancers, including those that are resistant to currently approved hormonal agents.
    1. Chromosomes and Gene Expression
    2. Computational and Systems Biology

    Genome-wide Estrogen Receptor-α activation is sustained, not cyclical

    Andrew N Holding et al.
    Activation of the Estrogen Receptor by estra-2-diol results in sustained binding and the previously described cyclical response kinetics are likely an artefact of observing a highly variable process without replicates.
    1. Structural Biology and Molecular Biophysics
    2. Human Biology and Medicine

    Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation

    Sean W Fanning et al.
    Two common mutant versions of estrogen receptor alpha achieve constitutive activity and hormone-resistance by preferentially adopting a suite of conformations that expose the coregulator-binding surface.
    1. Structural Biology and Molecular Biophysics
    2. Chromosomes and Gene Expression

    Resveratrol modulates the inflammatory response via an estrogen receptor-signal integration network

    Jerome C Nwachukwu et al.
    Anti-inflammatory effects of resveratrol are mediated by the estrogen receptor to coordinate a complex array of transcriptional coregulators, suggesting that estrogenic effects must be considered in the complex polypharmacology of resveratrol.
    1. Developmental Biology

    Oviductal estrogen receptor α signaling prevents protease-mediated embryo death

    Wipawee Winuthayanon et al.
    Cyclic estrogen signaling in oviduct epithelial cells suppresses oviduct luminal protease activity to allow survival and development of preimplantation embryos
    1. Cancer Biology
    2. Human Biology and Medicine

    The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer

    James D Joseph et al.
    GDC-0810 is a novel, orally bioavailable SERD that exhibits robust pre-clinical activity in models of ER+ breast cancer, including models of tamoxifen resistance, and those that express the ERα mutations, ER.Y537S and ER.D538G.
    1. Cancer Biology

    Activation of G protein-coupled estrogen receptor signaling inhibits melanoma and improves response to immune checkpoint blockade

    Christopher A Natale et al.
    Driving melanoma differentiation through G protein-coupled estrogen receptor signaling decreases proliferative capacity, decreases expression of the oncodriver and stem cell marker c-Myc, and increases the effectiveness of immunotherapy.
    1. Developmental Biology
    2. Human Biology and Medicine

    RUNX1, a transcription factor mutated in breast cancer, controls the fate of ER-positive mammary luminal cells

    Maaike PA van Bragt et al.
    Loss of RUNX1, a key regulator of estrogen receptor-positive luminal breast cells, impairs mammary epithelial differentiation and contributes to luminal breast cancer via genetic interactions with a loss of p53 or RB1.

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