2,948 results found
    1. Computational and Systems Biology

    Unravelling druggable signalling networks that control F508del-CFTR proteostasis

    Ramanath Narayana Hegde et al.
    Analysis of the mechanism of action of cystic fibrosis corrector drugs reveals signalling pathways potently controlling the proteostasis of the main disease-relevant CFTR mutant.
    1. Cancer Biology
    2. Cell Biology

    The anticancer natural product ophiobolin A induces cytotoxicity by covalent modification of phosphatidylethanolamine

    Christopher Chidley et al.
    An unbiased genetic screen in human cells shows that the molecular target of a natural product with promising anticancer activity is a membrane phospholipid.
    1. Biochemistry and Chemical Biology
    2. Microbiology and Infectious Disease

    Hepatitis B virus core protein allosteric modulators can distort and disrupt intact capsids

    Christopher John Schlicksup et al.
    Small molecule antivirals that drive assembly of HBV capsid protein can also bind to pre-assembled capsids causing them to change morphology or even break, suggesting a complex transduction of binding effects across the capsid.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Coupling of remote alternating-access transport mechanisms for protons and substrates in the multidrug efflux pump AcrB

    Thomas Eicher et al.
    A transport mechanism is uncovered in the major drug-efflux system in E. coli involving two remote alternating-access conformational cycles, which could provide the basis for the development of allosteric inhibitors against multidrug resistance.
    1. Immunology and Inflammation

    LRRC8A is essential for hypotonicity-, but not for DAMP-induced NLRP3 inflammasome activation

    Jack P Green et al.
    Depletion of LRRC8A provides genetic evidence for the importance of Cl- channels in NLRP3 activation.
    1. Cancer Biology

    The identification of dual protective agents against cisplatin-induced oto- and nephrotoxicity using the zebrafish model

    Jaime N Wertman et al.
    L-mimosine and dopamine protect against cisplatin-induced oto- and nephrotoxicity in zebrafish and human cell line models.
    1. Microbiology and Infectious Disease

    Membrane voltage dysregulation driven by metabolic dysfunction underlies bactericidal activity of aminoglycosides

    Giancarlo Noe Bruni, Joel M Kralj
    Aminoglycosides are a class of antibiotics that can kill Escherichia coli by building up internal voltage through disrupting the normal consumption of ATP.
    1. Structural Biology and Molecular Biophysics

    Architectural principles for Hfq/Crc-mediated regulation of gene expression

    Xue Yuan Pei et al.
    Structural insights show how RNA chaperones cooperate to recognise defined target transcripts and suppress gene expression.
    1. Microbiology and Infectious Disease

    Doxycycline has distinct apicoplast-specific mechanisms of antimalarial activity

    Megan Okada et al.
    Doxycycline used at a slightly higher concentration kills Plasmodium falciparum malaria parasites with faster, first-cycle activity through a novel organelle-specific mechanism.
    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.

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