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MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool
Cancers have dysfunctional redox regulation resulting in reactive oxygen species production, damaging both DNA and free dNTPs. The MTH1 protein sanitizes oxidized dNTP pools to prevent incorporationExpand
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Crystal structure, biochemical and cellular activities demonstrate separate functions of MTH1 and MTH2
Deregulated redox metabolism in cancer leads to oxidative damage to cellular components including deoxyribonucleoside triphosphates (dNTPs). Targeting dNTP pool sanitizing enzymes, such as MTH1, is aExpand
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Crystal Structure of the Emerging Cancer Target MTHFD2 in Complex with a Substrate-Based Inhibitor.
To sustain their proliferation, cancer cells become dependent on one-carbon metabolism to support purine and thymidylate synthesis. Indeed, one of the most highly upregulated enzymes duringExpand
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Glycans Confer Specificity to the Recognition of Ganglioside Receptors by Botulinum Neurotoxin A.
The highly poisonous botulinum neurotoxins, produced by the bacterium Clostridium botulinum, act on their hosts by a high-affinity association to two receptors on neuronal cell surfaces as the firstExpand
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Fragment-Based Discovery and Optimization of Enzyme Inhibitors by Docking of Commercial Chemical Space.
Fragment-based lead discovery has emerged as a leading drug development strategy for novel therapeutic targets. Although fragment-based drug discovery benefits immensely from access toExpand
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Crystal structures of OrfX2 and P47 from a Botulinum neurotoxin OrfX‐type gene cluster
Botulinum neurotoxins are highly toxic substances and are all encoded together with one of two alternative gene clusters, the HA or the OrfX gene cluster. Very little is known about the function andExpand
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Crystal Structure of Botulinum Neurotoxin A2 in Complex with the Human Protein Receptor SV2C Reveals Plasticity in Receptor Binding
Botulinum neurotoxins (BoNTs) are a family of highly dangerous bacterial toxins, with seven major serotypes (BoNT/A-G). Members of BoNTs, BoNT/A1 and BoNT/B1, have been utilized to treat anExpand
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Short‐Term Kinetics of the Humoral Anti‐Clq Response in SLE Using the ELISPOT Method: Fast Decline in Production in Response to Steroids
Twenty four systemic lupus erythaematosus patients and 17 patients with other diagnoses were investigated regarding the presence of cells producing Clq reactive antibodies in peripheral bloodExpand
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Large-Scale Synthesis of a Lewis b Tetrasaccharide Derivative, its Acrylamide Copolymer, and Related DI- and Trisaccharides for Use in Adhesion Inhibition Studies with Helicobacter Pylori.
ABSTRACT The 2-aminoethyl glycoside of O-α-L-fucopyranosyl-(1→2)-O-β-D-galactopyranosyl-(1→3)-[O-α-L-fucopyranosyl-(1→4)]-2-acetamido-2-deoxy-β-D-glucopyranose (Lewis B tetrasaccharide) wasExpand
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