3q82

Meropenem acylated BlaR1 sensor domain from Staphylococcus aureus

spinqualitylabelsall models 3q82, resolution 2.10Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3q82 is a 2 chain structure with sequence from Staphylococcus aureus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 2.1Å Ligands: GOL, MER Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function BLAR_STAAU BlaR1 is a potential penicillin-binding protein required for induction of beta-lactamase. Publication Abstract from PubMed The integral membrane protein BlaR1 of methicillin-resistant Staphylococcus aureus senses the presence of beta-lactam antibiotics in the milieu and transduces the information to the cytoplasm, where the biochemical events that unleash induction of antibiotic resistance mechanisms take place. We report herein by two-dimensional and three-dimensional NMR experiments of the sensor domain of BlaR1 in solution and by determination of an x-ray structure for the apo protein that Lys-392 of the antibiotic-binding site is posttranslationally modified by N(zeta)-carboxylation. Additional crystallographic and NMR data reveal that on acylation of Ser-389 by antibiotics, Lys-392 experiences N(zeta)-decarboxylation. This unique process, termed the lysine N(zeta)-decarboxylation switch, arrests the sensor domain in the activated ("on") state, necessary for signal transduction and all the subsequent biochemical processes. We present structural information on how this receptor activation process takes place, imparting longevity to the antibiotic-receptor complex that is needed for the induction of the antibiotic-resistant phenotype in methicillin-resistant S. aureus. Lysine Nzeta-decarboxylation switch and activation of the beta-lactam sensor domain of BlaR1 protein of methicillin-resistant Staphylococcus aureus.,Borbulevych O, Kumarasiri M, Wilson B, Llarrull LI, Lee M, Hesek D, Shi Q, Peng J, Baker BM, Mobashery S J Biol Chem. 2011 Sep 9;286(36):31466-72. Epub 2011 Jul 20. PMID:21775440 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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