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Inhibition of dihydroorotate dehydrogenase by the immunosuppressive agent leflunomide

✍ Scribed by Sharon Greene; Kiyotaka Watanabe; Julie Braatz-Trulson; Lillian Lou


Book ID
115784374
Publisher
Elsevier Science
Year
1995
Tongue
English
Weight
815 KB
Volume
50
Category
Article
ISSN
0006-2952

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The Ͱ-cyano-ͱ-hydroxy enamide 1 is an inhibitor of human dihydroorotate dehydrogenase (IC 50 ϭ 0.26 ȐM), the rate-limiting enzyme in the de novo pyrimidine biosynthesis. A structure-activity analysis based on selected derivatives of 1 demonstrates that both its structural characteristics and its phy