4,005 results found
    1. Biochemistry and Chemical Biology
    2. Cell Biology

    Subcellular drug targeting illuminates local kinase action

    Paula J Bucko, Chloe K Lombard ... John D Scott
    Genetically-encoded platforms direct kinase inhibitor drugs to organelles to reveal new dimensions of local kinase signaling.
    1. Computational and Systems Biology

    Decoding mechanism of action and sensitivity to drug candidates from integrated transcriptome and chromatin state

    Caterina Carraro, Lorenzo Bonaguro ... Barbara Gatto
    Combined analyses of transcriptome and chromatin accessibility elucidated the mechanisms underlying cancer cell lines response to antitumor candidates and provided a versatile perturbation-informed basal signature able to predict drug sensitivity.
    1. Biochemistry and Chemical Biology
    2. Computational and Systems Biology

    SIMMER employs similarity algorithms to accurately identify human gut microbiome species and enzymes capable of known chemical transformations

    Annamarie E Bustion, Renuka R Nayak ... Katherine S Pollard
    Computational reaction representations and profile hidden Markov model searches of metagenomics databases can be harnessed to accurately predict bacterial species and enzyme sequences responsible for biotransformations in the human gut microbiome.
    1. Computational and Systems Biology

    Unravelling druggable signalling networks that control F508del-CFTR proteostasis

    Ramanath Narayana Hegde, Seetharaman Parashuraman ... Alberto Luini
    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. Neuroscience

    Catecholaminergic challenge uncovers distinct Pavlovian and instrumental mechanisms of motivated (in)action

    Jennifer C Swart, Monja I Froböse ... Hanneke EM den Ouden
    Motivational coupling of action to reward and inhibition to punishment is subserved by dissociable learning and choice processes, and is modulated by dopamine/noradrenaline transporter blockade.
    1. Immunology and Inflammation
    2. Microbiology and Infectious Disease

    Scorpionfish BPI is highly active against multiple drug-resistant Pseudomonas aeruginosa isolates from people with cystic fibrosis

    Jonas Maurice Holzinger, Martina Toelge ... Sigrid Bülow
    Bactericidal/permeability-increasing protein (BPI) from the scorpionfish Sebastes schlegelii escapes detection by BPI autoantibodies derived from people with cystic fibrosis and reveals excellent anti-inflammatory potency as well as profound antimicrobial activity towards Pseudomonas aeruginosa, including multiple drug-resistant strains.
    1. Cancer Biology
    2. Medicine

    Improving drug discovery using image-based multiparametric analysis of the epigenetic landscape

    Chen Farhy, Santosh Hariharan ... Alexey V Terskikh
    A novel phenotypic screening platform based on immunofluorescent imaging of histone modifications enables accurate identification of cell fates and environmental perturbations.
    1. Biochemistry and Chemical Biology
    2. Cell Biology

    PPP1R15A-mediated dephosphorylation of eIF2α is unaffected by Sephin1 or Guanabenz

    Ana Crespillo-Casado, Joseph E Chambers ... David Ron
    The notion that the drug-like small molecule Sephin1 protects against protein misfolding by selectively disrupting a cellular phosphatase is refuted.
    1. Biochemistry and Chemical Biology

    Immunomodulatory drug discovery from herbal medicines: Insights from organ-specific activity and xenobiotic defenses

    Jue Shi, Jui-Hsia Weng, Timothy J Mitchison
    Organ-selective drug action of traditional Chinese medicine that generates systemic immune mediators is proposed and reviewed as a novel mechanistic angle to develop new immunomodulatory drugs.
    1. Neuroscience
    2. Structural Biology and Molecular Biophysics

    Modulation of the Erwinia ligand-gated ion channel (ELIC) and the 5-HT3 receptor via a common vestibule site

    Marijke Brams, Cedric Govaerts ... Chris Ulens
    Development of nanobodies against a model pentameric ligand-gated ion channel demonstrates they can be functionally active as negative or positive allosteric modulators and offers opportunities for future drug development.

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