4mjp

E. coli sliding clamp in complex with (R)-VedaprofenE. coli sliding clamp in complex with (R)-Vedaprofen

Structural highlights 4mjp is a 2 chain structure with sequence from Ecoli. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: , , , , Related: 4mjq, 4mjr Gene: b3701, dnaN, JW3678 (ECOLI) Activity: DNA-directed DNA polymerase, with EC number 2.7.7.7 Resources: FirstGlance, OCA, RCSB, PDBsum Publication Abstract from PubMed Evidence suggests that some nonsteroidal anti-inflammatory drugs (NSAIDs) possess antibacterial properties with an unknown mechanism. We describe the in vitro antibacterial properties of the NSAIDs carprofen, bromfenac, and vedaprofen, and show that these NSAIDs inhibit the Escherichia coli DNA polymerase III beta subunit, an essential interaction hub that acts as a mobile tether on DNA for many essential partner proteins in DNA replication and repair. Crystal structures show that the three NSAIDs bind to the sliding clamp at a common binding site required for partner binding. Inhibition of interaction of the clamp loader and/or the replicative polymerase alpha subunit with the sliding clamp is demonstrated using an in vitro DNA replication assay. NSAIDs thus present promising lead scaffolds for novel antibacterial agents targeting the sliding clamp. DNA replication is the target for the antibacterial effects of nonsteroidal anti-inflammatory drugs.,Yin Z, Wang Y, Whittell LR, Jergic S, Liu M, Harry E, Dixon NE, Kelso MJ, Beck JL, Oakley AJ Chem Biol. 2014 Apr 24;21(4):481-7. doi: 10.1016/j.chembiol.2014.02.009. Epub, 2014 Mar 13. PMID:24631121 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also DNA polymerase

spinqualitylabelsall models 4mjp, resolution 1.85Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image