2,089 results found
    1. Cancer Biology
    2. Medicine

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

    Chen Farhy et al.
    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. Structural Biology and Molecular Biophysics

    Distinct inactive conformations of the dopamine D2 and D3 receptors correspond to different extents of inverse agonism

    J Robert Lane et al.
    The occupation of a sub-pocket near the Na+-binding site in D2R by the Na+-insensitive antagonists is the structural basis for their greater inverse agonism than that of the Na+-sensitive ligands.
    1. Developmental Biology
    2. Neuroscience

    Large-scale phenotypic drug screen identifies neuroprotectants in zebrafish and mouse models of retinitis pigmentosa

    Liyun Zhang et al.
    Using a cross-species phenotypic drug discovery pipeline, compounds promoting rod photoreceptor survival in zebrafish and mouse models of retinitis pigmentosa were identified, evidence of additive effects of paired compounds and inhibition of PARP-dependent cell death suggest novel therapeutic strategies.
    1. Computational and Systems Biology
    2. Structural Biology and Molecular Biophysics

    Common activation mechanism of class A GPCRs

    Qingtong Zhou et al.
    Contrary to previous findings, class A GPCRs share a common activation pathway that directly links ligand binding to G-protein activation, as revealed by novel quantitative analysis.
    1. Medicine

    Identification of drug modifiers for RYR1-related myopathy using a multi-species discovery pipeline

    Jonathan R Volpatti et al.
    A multi-species chemical screening platform reveals a conserved role for p38 inhibition in modulating ryanodine receptor-related phenotypes and is adaptable to a range of neuromuscular disorders.
    1. Cancer Biology

    The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer

    James D Joseph et al.
    GDC-0810 is a novel, orally bioavailable SERD that exhibits robust pre-clinical activity in models of ER+ breast cancer, including models of tamoxifen resistance, and those that express the ERα mutations, ER.Y537S and ER.D538G.
    1. Cancer Biology

    Replication Study: Discovery and preclinical validation of drug indications using compendia of public gene expression data

    Irawati Kandela et al.
    Editors' Summary: This Replication Study has reproduced important parts of the original paper.
    1. Cell Biology
    2. Microbiology and Infectious Disease

    Coalescing beneficial host and deleterious antiparasitic actions as an antischistosomal strategy

    John D Chan et al.
    Engagement of both host and parasite signaling pathways proves a novel approach for developing improved anti-parasitic therapies.
    1. Cell Biology
    2. Developmental Biology

    First quantitative high-throughput screen in zebrafish identifies novel pathways for increasing pancreatic β-cell mass

    Guangliang Wang et al.
    A novel high-throughput, whole organism chemical screening platform was used to identify existing drugs that increase pancreatic beta-cell mass in zebrafish, implicating unique roles for the NF-κB and serotonergic signaling pathways in regulating pancreatic biology.
    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.

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