3u2o | pdb_00003u2o
From Proteopedia
Dihydroorotate Dehydrogenase (DHODH) crystal structure in complex with small molecule inhibitor
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Structural highlights
Disease[PYRD_HUMAN] Defects in DHODH are the cause of postaxial acrofacial dysostosis (POADS) [MIM:263750]; also known as Miller syndrome. POADS is characterized by severe micrognathia, cleft lip and/or palate, hypoplasia or aplasia of the posterior elements of the limbs, coloboma of the eyelids and supernumerary nipples. POADS is a very rare disorder: only 2 multiplex families, each consisting of 2 affected siblings born to unaffected, nonconsanguineous parents, have been described among a total of around 30 reported cases.[1] Function[PYRD_HUMAN] Catalyzes the conversion of dihydroorotate to orotate with quinone as electron acceptor. Publication Abstract from PubMedThe structure-activity relationships of a novel series of biaryl dihydroorotate dehydrogenase (DHODH) inhibitors related to teriflunomide are disclosed. These biaryl derivatives were the result of structure-based design and proved to be potent DHODH inhibitors which in addition showed good antiproliferative activities on peripheral blood mononuclear cells and good efficacies in vivo in the rat adjuvant-induced-arthritis model. Biaryl analogues of teriflunomide as potent DHODH inhibitors.,Erra M, Moreno I, Sanahuja J, Andres M, Reinoso RF, Lozoya E, Pizcueta P, Godessart N, Castro-Palomino JC Bioorg Med Chem Lett. 2011 Dec 15;21(24):7268-72. Epub 2011 Oct 20. PMID:22078215[2] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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This page was last modified 05:55, 13 July 2022.