3r6w | pdb_00003r6w
From Proteopedia
paAzoR1 binding to nitrofurazone
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Structural highlights
Function[AZOR1_PSEAE] Catalyzes the reductive cleavage of azo bond in aromatic azo compounds to the corresponding amines. Requires NADH, but not NADPH, as an electron donor for its activity (By similarity). Publication Abstract from PubMedAzoreductases are well known for azo pro-drug activation by gut flora. We show that azoreductases have a wider role in drug metabolism than previously thought as they can also reduce and hence activate nitrofurazone. Nitrofurazone, a nitroaromatic drug, is a broad spectrum antibiotic which has until now been considered as activated in bacteria by nitroreductases. The structure of the azoreductase with nitrofurazone bound was solved at 2.08 A and shows nitrofurazone in an active conformation. Based on the structural information, the kinetics and stoichiometry of nitrofurazone reduction by azoreductase from P. aeruginosa, we propose a mechanism of activation which accounts for the ability of azoreductases to reduce both azo and nitroaromatic drugs. This mode of activation can explain the cytotoxic side-effects of nitrofurazone through human azoreductase homologues. Activation of nitrofurazone by azoreductases: multiple activities in one enzyme.,Ryan A, Kaplan E, Laurieri N, Lowe E, Sim E Sci Rep. 2011;1:63. Epub 2011 Aug 12. PMID:22355582[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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This page was last modified 20:07, 25 December 2014.