Sandbox 124: Difference between revisions
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==='''How does Ceftobiprole work?'''=== | ==='''How does Ceftobiprole work?'''=== | ||
MRSA becomes resistant to β-lactams by acquiring an alternative PBP, PBP2a, that is neither bound nor inhibited by β-lactams. Recently, two cephalosporins – <scene name='37/372724/Ceftobiprole/1'>ceftobiprole</scene> and ceftaroline – that have anti-MRSA activity have been developed. Ceftobiprole is able to inhibit PBP2a because additional chemical groups at the <scene name='37/372724/ | MRSA becomes resistant to β-lactams by acquiring an alternative PBP, PBP2a, that is neither bound nor inhibited by β-lactams. Recently, two cephalosporins – <scene name='37/372724/Ceftobiprole/1'>ceftobiprole</scene> and ceftaroline – that have anti-MRSA activity have been developed. Ceftobiprole is able to inhibit PBP2a because additional chemical groups at the <scene name='37/372724/Ceftobiprole/2'>R2</scene> position of the cephalosporin backbone are able to interact with additional amino acid residues in PBP2a; specifically <scene name='37/372724/Met641_and_tyr446_labeled/1'>Tyr446 and Met641</scene>. As a result of its tighter binding to PBP2a, | ||
<scene name='37/372724/Rb6_interactions/1'>ceftobiprole</scene> is able to more efficiently react with the serine active site residue and therefore inhibit the activity of PBP2a. | <scene name='37/372724/Rb6_interactions/1'>ceftobiprole</scene> is able to more efficiently react with the serine active site residue and therefore inhibit the activity of PBP2a. | ||