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Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation.
Lactate dehydrogenase A (LDHA) catalyzes the conversion of pyruvate to lactate, utilizing NADH as a cofactor. It has been identified as a potential therapeutic target in the area of cancerExpand
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Domain Reorientation and Rotation of an Intracellular Assembly Regulate Conduction in Kir Potassium Channels
Potassium channels embedded in cell membranes employ gates to regulate K+ current. While a specific constriction in the permeation pathway has historically been implicated in gating, recent reportsExpand
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Iminosugars Inhibit Dengue Virus Production via Inhibition of ER Alpha-Glucosidases—Not Glycolipid Processing Enzymes
It has long been thought that iminosugar antiviral activity is a function of inhibition of endoplasmic reticulum-resident α-glucosidases, and on this basis, many iminosugars have been investigated asExpand
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Interdomain conformational flexibility underpins the activity of UGGT, the eukaryotic glycoprotein secretion checkpoint
Significance A dedicated endoplasmic reticulum quality control (ERQC) machinery ensures the correct fold of secreted proteins bearing N-linked glycans, which constitute around a fifth of the wholeExpand
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Low pH and Anionic Lipid-dependent Fusion of Uukuniemi Phlebovirus to Liposomes*
Many phleboviruses (family Bunyaviridae) are emerging as medically important viruses. These viruses enter target cells by endocytosis and low pH-dependent membrane fusion in late endosomes. However,Expand
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Structures of mammalian ER α-glucosidase II capture the binding modes of broad-spectrum iminosugar antivirals
Significance Most pathogenic enveloped viruses crucially depend on the quality control (QC) machinery in the endoplasmic reticulum (ER) of the host cell. ERQC inhibitors therefore have the doubleExpand
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Inhibition of endoplasmic reticulum glucosidases is required for in vitro and in vivo dengue antiviral activity by the iminosugar UV-4
The antiviral activity of UV-4 was previously demonstrated against dengue virus serotype 2 (DENV2) in multiple mouse models. Herein, step-wise minimal effective dose and therapeutic window ofExpand
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ToP-DNJ, a Selective Inhibitor of Endoplasmic Reticulum α-Glucosidase II Exhibiting Antiflaviviral Activity
Iminosugars have therapeutic potential against a range of diseases, due to their efficacy as glycosidase inhibitors. A major challenge in the development of iminosugar drugs lies in making a compoundExpand
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HER2 as a prospective novel biomarker in squamous cell carcinomas of the head and neck
For example, in some studies, HER2 has been shown to correlate with other clinicopathological parameters, such as disease‐free survival.[5,6] This may represent a different biologic behaviorExpand
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Molecular characterisation of ILRUN, a novel inhibitor of proinflammatory and antimicrobial cytokines
Regulation of type-I interferon (IFN) production is essential to the balance between antimicrobial defence and autoimmune disorders. The human protein-coding gene ILRUN (inflammation and lipidExpand
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