3,555 results found
    1. Structural Biology and Molecular Biophysics

    Nucleotide inhibition of the pancreatic ATP-sensitive K+ channel explored with patch-clamp fluorometry

    Samuel G Usher, Frances M Ashcroft, Michael C Puljung
    Simultaneous measurements of ligand binding and channel currents are used to understand gating of the ATP-sensitive K+ channel.
    1. Biochemistry and Chemical Biology

    Delayed inhibition mechanism for secondary channel factor regulation of ribosomal RNA transcription

    Sarah K Stumper, Harini Ravi ... Jeff Gelles
    Single-molecule observations reveal a mechanism that may be used by multiple competing regulatory proteins to control ribosomal RNA production during rapid bacterial cell growth.
    1. Computational and Systems Biology
    2. Neuroscience

    Nonlinearities between inhibition and T-type calcium channel activity bidirectionally regulate thalamic oscillations

    Adam C Lu, Christine Kyuyoung Lee ... Mark P Beenhakker
    A multi-scale integration of experimental and computational approaches shows how a non-linear dependence of T-type calcium channel gating on GABAB receptor activity regulates thalamic network oscillations.
    1. Biochemistry and Chemical Biology

    Therapeutic inhibition of keratinocyte TRPV3 sensory channel by local anesthetic dyclonine

    Qiang Liu, Jin Wang ... Jing Yao
    Identifying and understanding that local anesthetic dyclonine targets TRPV3 channels will help to conceive therapeutic interventions.
    1. Structural Biology and Molecular Biophysics

    BK channel inhibition by strong extracellular acidification

    Yu Zhou, Xiao-Ming Xia, Christopher J Lingle
    Analysis of iconic and gating currents of wild type and mutated BK channels reveals a strong inhibition of this channel by extracellular acidification and elucidates the underlying mechanism that is potentially applicable to other voltage-dependent cation channels.
    1. Structural Biology and Molecular Biophysics

    Structural insights into human acid-sensing ion channel 1a inhibition by snake toxin mambalgin1

    Demeng Sun, Sanling Liu ... Lei Liu
    Mambalgin1 binds to the thumb domain of human ASIC1a channel and inhibits the channel through hindering the proton-induced transitions from the resting closed state to the active and/or desensitized state.
    1. Structural Biology and Molecular Biophysics

    Inhibition of the proton-activated chloride channel PAC by PIP2

    Ljubica Mihaljević, Zheng Ruan ... Zhaozhu Qiu
    PIP2 inhibits the proton-activated chloride (PAC) channel by selectively stabilizing its desensitized state.
    1. Neuroscience

    Novel charged sodium and calcium channel inhibitor active against neurogenic inflammation

    Seungkyu Lee, Sooyeon Jo ... Bruce P Bean
    A cationic molecule derived from an uncharged Cav2.2 calcium channel inhibitor powerfully inhibits both sodium and calcium channels with extracellular application and inhibits both pain and neurogenic inflammation.
    1. Cell Biology

    Histidine phosphorylation relieves copper inhibition in the mammalian potassium channel KCa3.1

    Shekhar Srivastava, Saswati Panda ... Edward Y Skolnik
    The mammalian potassium channel KCa3.1, which is important for T- and B-cell activation, is inhibited by cytoplasmic copper, mediated by a histidine residue (His358) that is phosphorylated to activate the channel.
    1. Neuroscience

    NBI-921352, a first-in-class, NaV1.6 selective, sodium channel inhibitor that prevents seizures in Scn8a gain-of-function mice, and wild-type mice and rats

    JP Johnson, Thilo Focken ... James R Empfield
    NBI-921352 (formerly XEN901) is a precision medicine in development for individuals with SCN8A gain-of-function mutations causing SCN8A related epilepsy syndrome (SCN8A-RES), as well as other epilepsy indications, include adult focal onset seizures (FOS).

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