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PDBsum entry 6j3c
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Oxidoreductase/oxidoreductase inhibitor
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PDB id
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6j3c
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References listed in PDB file
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Key reference
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Title
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A novel series of human dihydroorotate dehydrogenase inhibitors discovered by in vitro screening: inhibition activity and crystallographic binding mode.
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Authors
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T.Zeng,
Z.Zuo,
Y.Luo,
Y.Zhao,
Y.Yu,
Q.Chen.
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Ref.
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FEBS Open Bio, 2019,
9,
1348-1354.
[DOI no: ]
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PubMed id
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Abstract
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Human dihydroorotate dehydrogenase (DHODH), the enzyme that catalyzes the
rate-limiting step in de novo pyrimidine biosynthesis, is considered to be an
attractive target for potential treatment of autoimmune disease and cancer.
Here, we present a novel class of human DHODH inhibitors with high inhibitory
potency. The high-resolution crystal structures of human DHODH complexed with
various agents reveal the details of their interactions. Comparisons with the
binding modes of teriflunomide and brequinar provide insights that may
facilitate the development of new inhibitors targeting human DHODH.
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