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Structural basis of CX‐4945 binding to human protein kinase CK2
Protein kinase CK2 (CK2), a constitutively active serine/threonine kinase, is involved in a variety of roles essential to the maintenance of cellular homeostasis. Elevated levels of CK2 expressionExpand
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Selective small-molecule inhibition of an RNA structural element
Riboswitches are non-coding RNA structures located in messenger RNAs that bind endogenous ligands, such as a specific metabolite or ion, to regulate gene expression. As such, riboswitches serve as aExpand
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Mechanism of Action and Epitopes of Clostridium difficile Toxin B-neutralizing Antibody Bezlotoxumab Revealed by X-ray Crystallography
Background: Bezlotoxumab is a neutralizing antibody targeting toxin B of Clostridium difficile. Results: The structure of bezlotoxumab bound to a fragment of toxin B reveals its epitopes andExpand
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Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40
Clinical studies indicate that partial agonists of the G-protein-coupled, free fatty acid receptor 1 GPR40 enhance glucose-dependent insulin secretion and represent a potential mechanism for theExpand
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TarO-specific inhibitors of wall teichoic acid biosynthesis restore β-lactam efficacy against methicillin-resistant staphylococci
New inhibitors of wall teichoic acid biosynthesis restore susceptibility of drug-resistant staphylococci to β-lactam antibiotics. Addressing antibiotic resistance with nonantibiotic adjuvants CoupledExpand
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Novel benzimidazole inhibitors bind to a unique site in the kinesin spindle protein motor domain.
Affinity selection-mass spectrometry (AS-MS) screening of kinesin spindle protein (KSP) followed by enzyme inhibition studies and temperature-dependent circular dichroism (TdCD) characterization wasExpand
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Thermodynamics of nucleotide and inhibitor binding to wild-type and ispinesib-resistant forms of human kinesin spindle protein.
Current antimitotic cancer chemotherapy based on vinca alkaloids and taxanes target tubulin, a protein required not only for mitotic spindle formation but also for the overall structural integrity ofExpand
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Chemical Genetic Analysis and Functional Characterization of Staphylococcal Wall Teichoic Acid 2-Epimerases Reveals Unconventional Antibiotic Drug Targets
Here we describe a chemical biology strategy performed in Staphylococcus aureus and Staphylococcus epidermidis to identify MnaA, a 2-epimerase that we demonstrate interconverts UDP-GlcNAc andExpand
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Broad Coverage of Genetically Diverse Strains of Clostridium difficile by Actoxumab and Bezlotoxumab Predicted by In Vitro Neutralization and Epitope Modeling
ABSTRACT Clostridium difficile infections (CDIs) are the leading cause of hospital-acquired infectious diarrhea and primarily involve two exotoxins, TcdA and TcdB. Actoxumab and bezlotoxumab areExpand
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Biochemical basis for the functional switch that regulates hepatocyte growth factor receptor tyrosine kinase activation.
Ligand-induced dimerization of receptor tyrosine kinases (RTKs) modulates a system of linked biochemical reactions, sharply switching the RTK from a quiescent state to an active state that becomesExpand
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