5,535 results found
    1. Structural Biology and Molecular Biophysics

    NPAS1-ARNT and NPAS3-ARNT crystal structures implicate the bHLH-PAS family as multi-ligand binding transcription factors

    Dalei Wu et al.
    Detailed structural analysis of NPAS1-ARNT and NPAS3-ARNT complexes, and further comparisons with other bHLH-PAS protein structures, show that this family of mammalian transcription factors have distinct ligand-binding pockets within their molecular architectures.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Cooperative cobinding of synthetic and natural ligands to the nuclear receptor PPARγ

    Jinsai Shang et al.
    Synthetic PPARγ ligands push and cobind with natural endogenous ligands, instead of compete and displace, which synergistically affects the structure and function of PPARγ.
    1. Structural Biology and Molecular Biophysics

    New capsaicin analogs as molecular rulers to define the permissive conformation of the mouse TRPV1 ligand-binding pocket

    Simon Vu et al.
    Novel capsaicin analogs with conserved chemistry but varying sizes were used as molecular rulers to investigate energetics of conformational changes in the ligand-binding pocket and mechanisms of TRPV1 ligand-gating.
    1. Structural Biology and Molecular Biophysics

    Direct binding of phosphatidylglycerol at specific sites modulates desensitization of a ligand-gated ion channel

    Ailing Tong et al.
    Phosphatidylglycerol binding at multiple sites stabilizes the open state relative to the desensitized state of a pentameric ligand-gated ion channel.
    1. Structural Biology and Molecular Biophysics

    Structure and dynamics underlying elementary ligand binding events in human pacemaking channels

    Marcel P Goldschen-Ohm et al.
    Single-molecule resolution of cAMP binding to the ligand binding domain of pacemaking channels in zero-mode waveguides reveals the dynamics of the distinct steps underlying both binding and isomerization of the binding domain.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    VEGFR-2 conformational switch in response to ligand binding

    Sarvenaz Sarabipour et al.
    A receptor for vascular endothelial growth factor forms dimers in the absence of its ligand, and ligand-binding leads to structural changes that result in increased kinase phosphorylation.
    1. Structural Biology and Molecular Biophysics

    Crystal structure of dopamine receptor D4 bound to the subtype selective ligand, L745870

    Ye Zhou et al.
    The structure of receptor-ligand complex reveals the ligand binding selectivity among different dopamine receptor subtypes and also shows how this ligand class inhibits receptor activity.
    1. Structural Biology and Molecular Biophysics

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

    Samuel G Usher et al.
    Simultaneous measurements of ligand binding and channel currents are used to understand gating of the ATP-sensitive K+ channel.
    1. Developmental Biology

    Fibrodysplasia ossificans progressiva mutant ACVR1 signals by multiple modalities in the developing zebrafish

    Robyn S Allen et al.
    The human Fibrodysplasia-Ossificans-Progressiva BMP-receptor mutant signals in zebrafish in the absence of ligand-binding, displays BMP ligand-responsive hyperactivity, neither requiring other type-I-BMP receptors, unlike wild-type, challenging views of the pathological mechanism.
    1. Structural Biology and Molecular Biophysics

    Ligand recognition and gating mechanism through three ligand-binding sites of human TRPM2 channel

    Yihe Huang et al.
    High-resolution structures of human TRPM2 in different functional states provided the mechanism underlying ligand recognition, channel activation and inhibition.

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