Abstract:
:1-deoxy-D-xylulose-5-phosphate reductoisomerase (Dxr) represents an essential enzyme of the mevalonate-independent pathway of the isoprenoid biosynthesis. Using fosmidomycin as a specific inhibitor of Dxr, this enzyme was previously validated as target for the treatment of malaria and bacterial infections. The replacement of the formyl residue of fosmidomycin by spacious acyl residues yielded inhibitors active in the micromolar range. As predicted by flexible docking, evidence was obtained for the formation of a hydrogen bond between an appropriately placed carbonyl group in the acyl residue and the main-chain NH of Met214 located in the flexible catalytic loop of the enzyme.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Ortmann R,Wiesner J,Silber K,Klebe G,Jomaa H,Schlitzer Mdoi
10.1002/ardp.200700149subject
Has Abstractpub_date
2007-09-01 00:00:00pages
483-90issue
9eissn
0365-6233issn
1521-4184journal_volume
340pub_type
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