Sandbox 124: Difference between revisions
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==='''How does Ceftobiprole work?'''=== | ==='''How does Ceftobiprole work?'''=== | ||
PBP2a and Ceftobiprole2 | PBP2a and Ceftobiprole2 | ||
MRSA becomes resistant to β-lactams by acquiring an alternative PBP, PBP2a, that is neither bound nor inhibited by β-lactams. Recently, two cephalosporins – ceftobiprole and ceftaroline – that have anti-MRSA activity have been developed. Ceftobiprole is able to inhibit PBP2a because additional chemical groups at the R2 position of the cephalosporin backbone are able to interact with additional amino acid residues in PBP2a; specifically <scene name='37/372724/Tyr446labeled/ | MRSA becomes resistant to β-lactams by acquiring an alternative PBP, PBP2a, that is neither bound nor inhibited by β-lactams. Recently, two cephalosporins – ceftobiprole and ceftaroline – that have anti-MRSA activity have been developed. Ceftobiprole is able to inhibit PBP2a because additional chemical groups at the R2 position of the cephalosporin backbone are able to interact with additional amino acid residues in PBP2a; specifically <scene name='37/372724/Tyr446labeled/3'>Tyr446</scene> and Met641. As a result of its tighter binding to PBP2a, ceftobiprole is able to more efficiently react with the serine active site residue and therefore inhibit the activity of PBP2a. |