2wq5 | pdb_00002wq5

NON-ANTIBIOTIC PROPERTIES OF TETRACYCLINES: STRUCTURAL BASIS FOR INHIBITION OF SECRETORY PHOSPHOLIPASE A2.

spinqualitylabelsall models 2wq5, resolution 1.65Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 2wq5 is a 1 chain structure with sequence from Naja naja. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: CA, MIY, SO4 Related: 1psh, 1ows, 1a3f, 1a3d Activity: Phospholipase A(2), with EC number 3.1.1.4 Resources: FirstGlance, OCA, RCSB, PDBsum Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMed Secretory phospholipase A(2) is involved in inflammatory processes and was previously shown to be inhibited by lipophilic tetracyclines such as minocycline (minoTc) and doxycycline. Lipophilic tetracyclines might be a new lead compound for the design of specific inhibitors of secretory phospholipase A(2), which play a crucial role in inflammatory processes. Our X-ray crystal structure analysis at 1.65 A resolution of the minoTc complex of phospholipase A(2) (PLA(2)) of the Indian cobra (Naja naja naja) is the first example of nonantibiotic tetracycline interactions with a protein. MinoTc interferes with the conformation of the active-site Ca(2+)-binding loop, preventing Ca(2)(+) binding, and shields the active site from substrate entrance, resulting in inhibition of the enzyme. MinoTc binding to PLA(2) is dominated by hydrophobic interactions quite different from antibiotic recognition of tetracyclines by proteins or the ribosome. The affinity of minoTc for PLA(2) was determined by surface plasmon resonance, resulting in a dissociation constant K(d)=1.8 x 10(-)(4) M. Nonantibiotic properties of tetracyclines: structural basis for inhibition of secretory phospholipase A2.,Dalm D, Palm GJ, Aleksandrov A, Simonson T, Hinrichs W J Mol Biol. 2010 Apr 23;398(1):83-96. Epub 2010 Mar 6. PMID:20211188 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Phospholipase A2

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