Dual binding mode of a novel series of DHODH inhibitors.

  title={Dual binding mode of a novel series of DHODH inhibitors.},
  author={Roland Baumgartner and Markus Walloschek and Martin Kr{\'a}lik and Astrid Gotschlich and Stefan Tasler and Jan Mies and Johann Leban},
  journal={Journal of medicinal chemistry},
  volume={49 4},
Human dihydroorotate dehydrogenase (DHODH) represents an important target for the treatment of hyperproliferative and inflammatory diseases. In the cell DHODH catalyzes the rate-limiting step of the de novo pyrimidine biosynthesis. DHODH inhibition results in beneficial immunosuppressant and antiproliferative effects in diseases such as rheumatoid arthritis. Here, we present high-resolution X-ray structures of human DHODH in complex with a novel class of low molecular weight compounds that… CONTINUE READING

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