Structural highlights
6c7s is a 1 chain structure with sequence from Nocfa. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
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| Ligands: | , , , |
| Related: | 5kow, 5kox |
| Gene: | rox, NFA_35380 (NOCFA) |
| Resources: | FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT |
Publication Abstract from PubMed
Rifampicin monooxygenase (RIFMO) decreases the potency of rifampicin (RIF) by converting it to oxidative products. Further decomposition of RIF has been observed in bacteria producing RIFMO and contributes to RIFMO-mediated drug resistance. Here we report the first crystal structure of RIFMO in complex with the hydroxylated RIF product. The 2.10 A resolution structure reveals a breach of the ansa aliphatic chain of RIF between naphthoquinone C2 and amide N1. Our data suggest that RIFMO catalyzes the hydroxylation of RIF at the C2 atom followed by cleavage of the ansa linkage, which leads to inactivation of the antibiotic by preventing key contacts with the RNA polymerase target.
Structural Evidence for Rifampicin Monooxygenase Inactivating Rifampicin by Cleaving Its Ansa-Bridge.,Liu LK, Dai Y, Abdelwahab H, Sobrado P, Tanner JJ Biochemistry. 2018 Apr 10;57(14):2065-2068. doi: 10.1021/acs.biochem.8b00190., Epub 2018 Mar 30. PMID:29578336[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Liu LK, Dai Y, Abdelwahab H, Sobrado P, Tanner JJ. Structural Evidence for Rifampicin Monooxygenase Inactivating Rifampicin by Cleaving Its Ansa-Bridge. Biochemistry. 2018 Apr 10;57(14):2065-2068. doi: 10.1021/acs.biochem.8b00190., Epub 2018 Mar 30. PMID:29578336 doi:http://dx.doi.org/10.1021/acs.biochem.8b00190
