932 results found
    1. Biochemistry and Chemical Biology
    2. Chromosomes and Gene Expression

    Small-molecule inhibitors identify the RAD52-ssDNA interaction as critical for recovery from replication stress and for survival of BRCA2 deficient cells

    Sarah R Hengel, Eva Malacaria ... Maria Spies
    Small molecule inhibitors identified in a biophysical high-throughout screening assay confirm the importance of the interaction between single-stranded DNA and the protein RAD52 for the survival of BRCA2-depleted cells.
    1. Medicine

    Binding blockade between TLN1 and integrin β1 represses triple-negative breast cancer

    Yixiao Zhang, Lisha Sun ... Caigang Liu
    The upregulation of TLN1 contributes to the metastasis of triple-negative breast cancer (TNBC), and a small-molecule C67399 was screened for blocking TLN1 and integrin β1 may hold promise for the treatment of TNBC.
    1. Neuroscience
    2. Stem Cells and Regenerative Medicine

    High-content synaptic phenotyping in human cellular models reveals a role for BET proteins in synapse assembly

    Martin H Berryer, Gizem Rizki ... Lindy E Barrett
    An automated synaptic phenotyping platform combined with small molecule screening reveals modulators of human neuron synapse formation.
    1. Biochemistry and Chemical Biology
    2. Cell Biology

    Small molecule proteostasis regulators that reprogram the ER to reduce extracellular protein aggregation

    Lars Plate, Christina B Cooley ... Jeffery W Kelly
    Small molecule proteostasis regulators that activate the unfolded protein response transcription factor ATF6 reduce the secretion of amyloid disease-associated proteins.
    1. Structural Biology and Molecular Biophysics

    An expanded allosteric network in PTP1B by multitemperature crystallography, fragment screening, and covalent tethering

    Daniel A Keedy, Zachary B Hill ... James S Fraser
    By measuring how multiple conformations shift in response to temperature, a new allosteric binding site is discovered for the phosphatase PTP1B.
    1. Cell Biology

    Ceapins are a new class of unfolded protein response inhibitors, selectively targeting the ATF6α branch

    Ciara M Gallagher, Carolina Garri ... Peter Walter
    Ceapins enable selective pharmacological inhibition of the cytoprotective transcriptional response to endoplasmic reticulum stress through ATF6α without affecting other branches of the unfolded protein response.
    1. Biochemistry and Chemical Biology

    Reserpine maintains photoreceptor survival in retinal ciliopathy by resolving proteostasis imbalance and ciliogenesis defects

    Holly Y Chen, Manju Swaroop ... Anand Swaroop
    High-throughput screening of over 6000 drugs using cells and retina tissue with a CEP290 ciliopathy mutation identified a small molecule, reserpine, which enhanced photoreceptor survival in retinal organoids and in a mouse disease model by partially restoring balance in proteostasis.
    1. Cell Biology

    Counteracting suppression of CFTR and voltage-gated K+ channels by a bacterial pathogenic factor with the natural product tannic acid

    Yajamana Ramu, Yanping Xu ... Zhe Lu
    Tannic acid acts as an ‘antidote’ against the negative effects of a bacterial enzyme, which can both aggravate cystic fibrosis and enable the anthrax bacteria to evade the immune responses elicited by a typical live vaccine.
    1. Cell Biology
    2. Genetics and Genomics

    A high-throughput small molecule screen identifies farrerol as a potentiator of CRISPR/Cas9-mediated genome editing

    Weina Zhang, Yu Chen ... Zhiyong Mao
    Farrerol promotes the efficiency of CRISPR/Cas9-mediated genome editing in both cells and embryos.
    1. Biochemistry and Chemical Biology
    2. Microbiology and Infectious Disease

    Discovery of a small molecule that inhibits bacterial ribosome biogenesis

    Jonathan M Stokes, Joseph H Davis ... Eric D Brown
    The anticonvulsant drug lamotrigine inhibits bacterial ribosome biogenesis and reveals an unexplored role for initiation factor 2 (IF2) in ribosome assembly.

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