Browse the search results

Page 2 of 4
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics

    Ziva Vuckovic, Jinan Wang ... David M Thal
    Structural biology studies reveal the importance of protein dynamics on understanding molecular mechanisms underlying allosteric modulation of G protein-coupled receptors (GPCR) that offer insights into future GPCR research and drug discovery.
    1. Microbiology and Infectious Disease
    2. Structural Biology and Molecular Biophysics

    A pH-dependent cluster of charges in a conserved cryptic pocket on flaviviral envelopes

    Lorena Zuzic, Jan K Marzinek ... Peter J Bond
    Benzene mapping simulations of envelope protein rafts from six different flaviviruses reveal a conserved cryptic site whose cluster of ionisable residues is likely responsible for orchestrating pH-dependent conformational changes during fusion, thereby representing an attractive target for antiviral development.
    1. Structural Biology and Molecular Biophysics
    2. Biochemistry and Chemical Biology

    A pathogenic human Orai1 mutation unmasks STIM1-independent rapid inactivation of Orai1 channels

    Priscilla S-W Yeung, Megumi Yamashita, Murali Prakriya
    A human Orai1 mutation linked to tubular myopathy activates Orai1 channels independently of STIM1 and unmasks calcium-dependent inactivation of Orai1 channels.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Targeting RNA:protein interactions with an integrative approach leads to the identification of potent YBX1 inhibitors

    Krystel El Hage, Nicolas Babault ... David Pastré
    The development of an integrative computational-experimental approach for identifying small molecules that can disrupt RNA:protein interactions in vitro and in cells led to the identification of several inhibitors of YBX1 in the micromolar range, including a previously approved drug.
    1. Structural Biology and Molecular Biophysics

    Revealing druggable cryptic pockets in the Nsp1 of SARS-CoV-2 and other β-coronaviruses by simulations and crystallography

    Alberto Borsatto, Obaeda Akkad ... Francesco Luigi Gervasio
    A combination of simulations and experiments was used to discover druggable cryptic pockets in non-structural protein 1, a promising but difficult target for coronaviruses, indicating a viable drug discovery approach for otherwise undruggable targets.
    1. Developmental Biology
    2. Neuroscience

    Neuronal temperature perception induces specific defenses that enable C. elegans to cope with the enhanced reactivity of hydrogen peroxide at high temperature

    Francesco A Servello, Rute Fernandes ... Javier Apfeld
    C. elegans nematodes can assess faithfully the threat that H2O2 poses by coupling the induction of their H2O2 defenses to the perception of high temperature—an inherent enhancer of the reactivity of H2O2.
    1. Biochemistry and Chemical Biology

    Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry

    Tiantian Wei, Jue Wang ... Xiaoguang Lei
    A potent and selective DYRK2 inhibitor has been developed and used as a chemical tool to reveal eukaryotic translation initiation factor 4E-binding protein 1 (4E-BP1) and stromal interaction molecule 1 (STIM1) are new substrates for DYRK2.
    1. Cell Biology

    Crotamiton derivative JM03 extends lifespan and improves oxidative and hypertonic stress resistance in Caenorhabditis elegans via inhibiting OSM-9

    Keting Bao, Wenwen Liu ... Jian Li
    In a chemical genetics study, JM03 derived from crotamiton, an inhibitor of trainsient receptor potential vanilloid-4 channels, was identified to extend lifespan and improve oxidative and hypertonic stress resistance in Caenorhabditis elegans via inhibiting OSM-9.
    1. Neuroscience

    A transient postnatal quiescent period precedes emergence of mature cortical dynamics

    Soledad Domínguez, Liang Ma ... Jennifer N Gelinas
    Maturation of cortical network dynamics is characterized by a nadir that signals the shift from local, loosely correlated, prominently sensory-driven patterns to internally organized, spatially distributed, and temporally precise activity.
    1. Computational and Systems Biology
    2. Structural Biology and Molecular Biophysics

    Development of antibacterial compounds that constrain evolutionary pathways to resistance

    Yanmin Zhang, Sourav Chowdhury ... Eugene Shakhnovich
    Integrated multi-scale, multi-tool approach to design novel 'evolution drugs' which can delay the emergence of antibiotic resistance by constraining bacterial evolutionary escape strategies.