2,048 results found
    1. Biochemistry and Chemical Biology

    Conformation selection by ATP-competitive inhibitors and allosteric communication in ERK2

    Jake W Anderson, David Vaisar ... Natalie G Ahn
    New ATP-competitive inhibitors show properties of conformation selection when complexed with the MAP kinase, ERK2, altering movements around the activation loop.
    1. Structural Biology and Molecular Biophysics

    Empowering AlphaFold2 for protein conformation selective drug discovery with AlphaFold2-RAVE

    Xinyu Gu, Akashnathan Aranganathan, Pratyush Tiwary
    AlphaFold2's inability to generate non-native conformations for docking is addressed by AI-molecular dynamics method AlphaFold2-RAVE, which produces Boltzmann-ranked conformations, enabling the retrospective discovery of type II kinase inhibitors.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Synthetic single domain antibodies for the conformational trapping of membrane proteins

    Iwan Zimmermann, Pascal Egloff ... Markus A Seeger
    Synthetic single domain antibody libraries and a binder selection cascade encompassing ribosome and phage display enable the selection of conformation-specific binders against previously intractable membrane proteins within three weeks.
    1. Biochemistry and Chemical Biology

    The mechanism of error induction by the antibiotic viomycin provides insight into the fidelity mechanism of translation

    Mikael Holm, Chandra Sekhar Mandava ... Suparna Sanyal
    The antibiotic viomycin induces errors during initial codon selection by the ribosome by locking the monitoring bases in their active conformation.
    1. Chromosomes and Gene Expression

    The β-hairpin of 40S exit channel protein Rps5/uS7 promotes efficient and accurate translation initiation in vivo

    Jyothsna Visweswaraiah, Yvette Pittman ... Alan G Hinnebusch
    A structural element of mRNA exit channel protein Rps5 performs a critical role in start codon recognition during translation initiation by stabilizing initiator tRNA binding to the pre-initiation complex.
    1. Structural Biology and Molecular Biophysics

    Isoleucine gate blocks K+ conduction in C-type inactivation

    Werner Treptow, Yichen Liu ... Benoit Roux
    The conformation of an isoleucine gate located along the TM6 segment on the intracellular side below the selectivity filter is a critical component leading to a non-conductive state in the C-type inactivation process of K+ channels.
    1. Structural Biology and Molecular Biophysics

    Conserved conformational selection mechanism of Hsp70 chaperone-substrate interactions

    Ashok Sekhar, Algirdas Velyvis ... Lewis E Kay
    NMR-based flux measurements show that both bacterial and human Hsp70 chaperones interact with helical, as well as sheet substrates predominantly through a conformational selection mechanism.
    1. Developmental Biology

    A human mitofusin 2 mutation can cause mitophagic cardiomyopathy

    Antonietta Franco, Jiajia Li ... Gerald W Dorn
    A rare human mitofusin (MFN) 2 mutation that uniquely impaired Parkin-mediated mitophagy evoked developmental heart disease and increased myocardial sensitivity to doxorubicin in mice, differentiating it from mitophagy-competent MFN2 mutations that cause neuropathy and implicating mitophagy in clinical cardiomyopathy.
    1. Structural Biology and Molecular Biophysics
    2. Cell Biology

    A tethered delivery mechanism explains the catalytic action of a microtubule polymerase

    Pelin Ayaz, Sarah Munyoki ... Luke M Rice
    Using linked TOG domains that each bind a curved conformation of αβ-tubulin, a microtubule polymerase catalyzes fast elongation by concentrating αβ-tubulin near the polymer end.
    1. Structural Biology and Molecular Biophysics

    Gating and selectivity mechanisms for the lysosomal K+ channel TMEM175

    SeCheol Oh, Navid Paknejad, Richard K Hite
    Structures of the non-canonical potassium channel TMEM175 in open and closed states reveal unique mechanisms for channel gating and the selective permeation of K+ ions.

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