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

    Uncovering an allosteric mode of action for a selective inhibitor of human Bloom syndrome protein

    Xiangrong Chen et al.
    Discovery and characterisation of a novel allosteric inhibitor-binding site in human Bloom syndrome protein.
    1. Cell Biology

    Probing the catalytic functions of Bub1 kinase using the small molecule inhibitors BAY-320 and BAY-524

    Anna P Baron et al.
    Chemical inhibition of Bub1 shows that the catalytic activity is not required for normal mitotic progression, but it makes chromosome segregation and cell proliferation more sensitive to the effects of the anti-cancer drug Paclitaxel.
    1. Cell Biology

    Unique integrated stress response sensors regulate cancer cell susceptibility when Hsp70 activity is compromised

    Sara Sannino et al.
    Unique integrate stress response sensors differentially trigger pro-survival versus pro-apoptotic responses in cells confronted with Hsp70 inhibitor-associated proteotoxic challenges.
    1. Biochemistry and Chemical Biology
    2. Cell Biology

    Permeant fluorescent probes visualize the activation of SARM1 and uncover an anti-neurodegenerative drug candidate

    Wan Hua Li et al.
    The first-in-class cell-permeant fluorescent probe provides direct and visual evidence of SARM1 activation in axonal degeneration and identified the first covalent, allosteric inhibitor of SARM1 acting on the NAD-binding pocket in the ARM domain.
    1. Computational and Systems Biology
    2. Medicine

    NICEdrug.ch, a workflow for rational drug design and systems-level analysis of drug metabolism

    Homa MohammadiPeyhani et al.
    NICEdrug.ch is a resource allowing systematic and large-scale computational analysis of drug biochemistry, enzymatic targets, and toxicity in the context of cellular metabolism.
    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. Cell Biology

    Extensive cargo identification reveals distinct biological roles of the 12 importin pathways

    Makoto Kimura et al.
    Transport-based high-throughput identification of cargo proteins specific to all 12 human importin-β family nuclear import receptors revealed biological processes that the cargo cohorts of each receptor are involved in.
    1. Biochemistry and Chemical Biology

    Structure-guided microbial targeting of antistaphylococcal prodrugs

    Justin J Miller et al.
    Prodrug antibiotics can be designed that are serum-stable but readily cleaved inside bacterial pathogens.
    1. Biochemistry and Chemical Biology
    2. Genetics and Genomics

    Genome mining unearths a hybrid nonribosomal peptide synthetase-like-pteridine synthase biosynthetic gene cluster

    Hyun Bong Park et al.
    A new type of hybrid nonribosomal peptide synthetase (NRPS)-like-pteridine synthase biosynthetic pathway has been illuminated via genome mining.