5 results found
    1. Structural Biology and Molecular Biophysics

    Cystic fibrosis drug ivacaftor stimulates CFTR channels at picomolar concentrations

    László Csanády, Beáta Töröcsik
    Aqueous solubility of cystic fibrosis drug ivacaftor is ~200-fold lower, whereas the potency of its stimulatory effect on the CFTR channel is >100-fold higher, than reported, and is fully reversible.
    1. Immunology and Inflammation

    Different CFTR modulator combinations downregulate inflammation differently in cystic fibrosis

    Heledd H Jarosz-Griffiths et al.
    CFTR modulators have potent innate anti-inflammatory properties that can be measured in clinic, both ex vivo and in vitro, which can be used to predict treatment efficacy.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Obligate coupling of CFTR pore opening to tight nucleotide-binding domain dimerization

    Csaba Mihályi et al.
    Coupling of CFTR pore opening to nucleotide binding domain dimerization does not depend on ATP binding, but is an inherent property of the channel protein and likely other ABC transporters.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Molecular basis for activation of lecithin:cholesterol acyltransferase by a compound that increases HDL cholesterol

    Kelly A Manthei et al.
    Structure of lecithin:cholesterol acyltransferase with a covalent acyl-intermediate mimic and a small molecule activator reveals an active conformation and that the enzyme can be activated via its membrane binding domain.
    1. Computational and Systems Biology
    2. Human Biology and Medicine

    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.

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