739 results found
    1. Cell Biology

    Nanchangmycin regulates FYN, PTK2, and MAPK1/3 to control the fibrotic activity of human hepatic stellate cells

    Wenyang Li, Jennifer Y Chen ... Alan C Mullen
    A high-throughput small molecule screen defined compounds that inactivate primary human hepatic stellate cells (HSCs) and led to the identification of nanchangmycin, which regulates intracellular Ca2+ levels and the activity of multiple kinases to control HSC fibrotic activity.
    1. Structural Biology and Molecular Biophysics

    Structure-based characterization of novel TRPV5 inhibitors

    Taylor ET Hughes, John Smith Del Rosario ... Vera Y Moiseenkova-Bell
    Structure-based virtual screening reveals multiple novel TRPV5 inhibitors that bind and exert their effect from previously unidentified binding sites as characterized by cryo-electron microscopy and electrophysiology.
    1. Developmental Biology

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

    Franz S Gruber, Zoe C Johnston ... Paul D Andrews
    A high-throughput phenotypic human sperm screening platform was developed which allows for major drug discovery programmes for male contraception.
    1. Biochemistry and Chemical Biology
    2. Computational and Systems Biology

    Structure-based discovery of potent and selective melatonin receptor agonists

    Nilkanth Patel, Xi Ping Huang ... Vsevolod Katritch
    Large scale virtual screening using recently solved structures of Melatonin receptors yield discovery of 10 new high-affinity selective agonists, also revealing novel functional features, including biased signaling at Melatonin receptors.
    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. Microbiology and Infectious Disease

    Highly parallelized droplet cultivation and prioritization of antibiotic producers from natural microbial communities

    Lisa Mahler, Sarah P Niehs ... Miriam A Rosenbaum
    This microscale cultivation strategy will help in the discovery of novel bacterial species and their prioritization for antibiotic screening campaigns.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Modulating FOXO3 transcriptional activity by small, DBD-binding molecules

    Judith Hagenbuchner, Veronika Obsilova ... Michael J Ausserlechner
    The mode of binding and cellular effect of the first FOXO3-DNA-binding-domain targeting small compound discovered by a combined pharmacophore-based/biochemical screening approach is reported.
    1. Stem Cells and Regenerative Medicine
    2. Neuroscience

    Imaging-based chemical screening reveals activity-dependent neural differentiation of pluripotent stem cells

    Yaping Sun, Zhiqiang Dong ... Su Guo
    A chemical screen reveals that a compound used to treat a parasitic disease can trigger pluripotent stem cells to become neurons, uncovering a novel mechanism behind neuronal development.
    1. Medicine
    2. Stem Cells and Regenerative Medicine

    Therapeutic downregulation of neuronal PAS domain 2 (Npas2) promotes surgical skin wound healing

    Yoichiro Shibuya, Akishige Hokugo ... Reza Jarrahy
    A small molecule compound Dwn1, identified through high-throughput screening using Npas2 as the molecular target, enhances wound healing in a murine incisional wound model.
    1. Epidemiology and Global Health
    2. Microbiology and Infectious Disease

    The repurposing of Tebipenem pivoxil as alternative therapy for severe gastrointestinal infections caused by extensively drug-resistant Shigella spp

    Elena Fernández Álvaro, Phat Voong Vinh ... Stephen Baker
    The oral carbapenem 'Tebipenem' has high level antibacterial activity against highly drug-resistant Shigella, and its mode of action and pharmacokinetics make it suitable for the treatment of severe diarrhoea caused by highly drug-resistant bacteria.

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