174 results found
    1. Cancer Biology

    Overcoming mutation-based resistance to antiandrogens with rational drug design

    Minna D Balbas, Michael J Evans ... Charles L Sawyers
    Mutagenesis studies identified an androgen receptor mutation that converts enzalutamide-a drug recently approved for the treatment of advanced prostate cancer-into an androgen receptor agonist, and modeling studies informed the design of novel drugs that are effective against the mutant receptor.
    1. Cell Biology

    Nuclear receptor LRH-1/NR5A2 is required and targetable for liver endoplasmic reticulum stress resolution

    Jennifer L Mamrosh, Jae Man Lee ... David D Moore
    LRH-1/NR5A2 responds to ER stress by inducing a novel pathway that is required for stress resolution in mice and can be targeted by LRH-1 agonists.
    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, Sathish Srinivasan ... Kendall W Nettles
    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. Chromosomes and Gene Expression

    p50-associated COX-2 extragenic RNA (PACER) activates COX-2 gene expression by occluding repressive NF-κB complexes

    Michal Krawczyk, Beverly M Emerson
    A long non-coding RNA removes the transcriptional repressor p50 to regulate recruitment of co-activator p300 and RNA Polymerase II complexes to activate the COX-2 gene in human mammary epithelial cells and macrophages.
    1. Cell Biology
    2. Chromosomes and Gene Expression

    Expression site attenuation mechanistically links antigenic variation and development in Trypanosoma brucei

    Christopher Batram, Nicola G Jones ... Markus Engstler
    The VSG gene controls its monoallelic expression, and expression site activity determines developmental progression.
    1. Chromosomes and Gene Expression

    MicroRNAs down-regulate homologous recombination in the G1 phase of cycling cells to maintain genomic stability

    Young Eun Choi, Yunfeng Pan ... Dipanjan Chowdhury
    MicroRNAs tightly control the cellular level of homologous recombination (HR) factors in the G1 phase, and failure of this control system results in an ectopic increase in HR proteins in G1 cells leading to impaired DNA repair.
    1. Cell Biology
    2. Cancer Biology

    MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells

    Yubao Wang, Young-Mi Lee ... Jean J Zhao
    Maternal embryonic leucine zipper kinase (MELK) is a new anti-cancer target that is highly selective for basal-like breast cancer.
    1. Genetics and Genomics

    Mismatch repair deficiency endows tumors with a unique mutation signature and sensitivity to DNA double-strand breaks

    Hui Zhao, Bernard Thienpont ... Diether Lambrechts
    A comprehensive catalogue of somatic mutations accumulating in MMR-deficient tumors highlights their relevance in the context of human genetic evolution, for the diagnosis of microsatellite instability and the provision of targeted treatment options.
    1. Cell Biology

    The role of IMP dehydrogenase 2 in Inauhzin-induced ribosomal stress

    Qi Zhang, Xiang Zhou ... Hua Lu
    The small molecule Inauhzin possesses a dual targeting ability, and activates p53 by targeting two enzymes—SIRT1 and IMP dehydrogenase 2 (IMPDH2)—which are highly expressed in human cancers.
    1. Cell Biology
    2. Immunology and Inflammation

    Sharpin prevents skin inflammation by inhibiting TNFR1-induced keratinocyte apoptosis

    Snehlata Kumari, Younes Redouane ... Fumiyo Ikeda
    The adaptor proteins FADD and TRADD play an important role in the Sharpin-dependent anti-apoptosis signaling pathway in keratinocytes and regulate skin homeostasis.

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