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    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Ligand modulation of sidechain dynamics in a wild-type human GPCR

    Lindsay D Clark et al.
    Generation of a highly deuterated 13C-methyl labeled wild-type GPCR sample is used to facilitate characterization of the molecular environments and fast ps-ns dynamics of sidechains when the receptor is bound to ligands of different efficacy.
    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. Developmental Biology
    2. Neuroscience

    A multi-protein receptor-ligand complex underlies combinatorial dendrite guidance choices in C. elegans

    Wei Zou et al.
    LECT-2 guides dendrite growth and branching via a unique ligand-receptor complex.
    1. Structural Biology and Molecular Biophysics

    Distinct gating mechanisms revealed by the structures of a multi-ligand gated K+ channel

    Chunguang Kong et al.
    Structural and functional studies of a potassium ion channel that is opened and closed by different ligands have revealed a novel gating mechanism.
    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. Cell Biology

    The sterol-responsive RNF145 E3 ubiquitin ligase mediates the degradation of HMG-CoA reductase together with gp78 and Hrd1

    Sam A Menzies et al.
    CRISPR/Cas9 genome-wide screens using sterol-sensitive endogenous HMG-CoA reductase (HMGCR) reporter identify the sterol-responsive RNF145 and gp78 as independently responsible for sterol-accelerated degradation of HMGCR, the rate-limiting enzyme of cholesterol biosynthesis.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor

    Kathryn E Livingston et al.
    Opioid drug efficacy and allosteric modulation is measured using an active state sensor of the mu-opioid receptor.
    1. Biochemistry and Chemical Biology
    2. Immunology and Inflammation

    RING finger E3 ligase PPP1R11 regulates TLR2 signaling and innate immunity

    Alison C McKelvey et al.
    Novel post-translational modification of pattern recognition receptor TLR2 has consequences in bacterial infection and inflammatory signaling.
    1. Cell Biology

    FAM150A and FAM150B are activating ligands for anaplastic lymphoma kinase

    Jikui Guan et al.
    The secreted molecules FAM150A and FAM150B bind to the ALK RTK extracellular domain, potently activating the receptor activation and driving downstream signaling events.
    1. Biochemistry and Chemical Biology
    2. Cell Biology

    Multisite dependency of an E3 ligase controls monoubiquitylation-dependent cell fate decisions

    Achim Werner et al.
    Simultaneous phosphorylation of multiple substrate motifs drives switch-like target recognition and monoubiquitylation by an E3 ligase during metazoan development.