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    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor

    Kathryn E Livingston et al.
    Opioid drug efficacy and allosteric modulation is measured using an active state sensor of the mu-opioid receptor.
    1. Structural Biology and Molecular Biophysics
    2. Human Biology and Medicine

    Structure-based discovery of fiber-binding compounds that reduce the cytotoxicity of amyloid beta

    Lin Jiang et al.
    By using structural methods to screen compounds for their ability to interact with amyloid beta, researchers have identified small molecules that stabilize amyloid fibers and reduce the toxic effect of smaller aggregates on cells.
    1. Structural Biology and Molecular Biophysics

    NPAS1-ARNT and NPAS3-ARNT crystal structures implicate the bHLH-PAS family as multi-ligand binding transcription factors

    Dalei Wu et al.
    Detailed structural analysis of NPAS1-ARNT and NPAS3-ARNT complexes, and further comparisons with other bHLH-PAS protein structures, show that this family of mammalian transcription factors have distinct ligand-binding pockets within their molecular architectures.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Structure of PINK1 and mechanisms of Parkinson's disease-associated mutations

    Atul Kumar et al.
    The structure of human PINK1 explains structural regulation and clarity on the impact of loss of function disease-associated mutations, which may stimulate future drug discovery efforts for both familial and idiopathic Parkinson's disease.
    1. Developmental Biology

    A phenotypic screening platform utilising human spermatozoa identifies compounds with contraceptive activity

    Franz S Gruber et al.
    A high-throughput phenotypic human sperm screening platform was developed which allows for major drug discovery programmes for male contraception.
    1. Human Biology and Medicine

    A distinct p53 target gene set predicts for response to the selective p53–HDM2 inhibitor NVP-CGM097

    Sébastien Jeay et al.
    The discovery and preclinical validation of a novel gene signature predictive for response to HDM2-targeting drug NVP-CGM097 could significantly improve the clinical response rate to all p53-HDM2 inhibitors.
    1. Structural Biology and Molecular Biophysics

    Structural basis for pharmacological modulation of the TRPC6 channel

    Yonghong Bai et al.
    Novel drug-binding sites of TRPC6 could potentially facilitate future design of drugs to treat TRPC6-mediated diseases.