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Comparative Study
. 2006 Mar 15;16(6):1610-5.
doi: 10.1016/j.bmcl.2005.12.029. Epub 2006 Jan 10.

Brequinar derivatives and species-specific drug design for dihydroorotate dehydrogenase

Darrell E Hurt  1 , Amanda E Sutton, Jon Clardy
Affiliations
Comparative Study

Brequinar derivatives and species-specific drug design for dihydroorotate dehydrogenase

Darrell E Hurt et al. Bioorg Med Chem Lett. .

Abstract

Therapeutic agents brequinar sodium and leflunomide (Arava) work by binding in a hydrophobic tunnel formed by a highly variable N-terminus of family 2 dihydroorotate dehydrogenase (DHODH). The X-ray crystallographic structure of an analog of brequinar bound to human DHODH was determined. In silico screening of a library of compounds suggested another subset of brequinar analogs that do not inhibit human DHODH as potentially effective inhibitors of Plasmodium falciparum DHODH.

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