Sandbox 126: Difference between revisions
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==='''PBP2a and Ceftobiprole'''=== | ==='''PBP2a and Ceftobiprole'''=== | ||
MRSA becomes resistant to β-lactams by acquiring an alternative PBP, PBP2a, that is neither bound nor inhibited by β-lactams. Ceftobiprole (PDB:<scene name='37/372726/4dki/1'>4DKI</scene>) is able to inhibit PBP2a because additional chemical groups at the <scene name='37/372726/ | MRSA becomes resistant to β-lactams by acquiring an alternative PBP, PBP2a, that is neither bound nor inhibited by β-lactams. Ceftobiprole (PDB:<scene name='37/372726/4dki/1'>4DKI</scene>) is able to inhibit PBP2a because additional chemical groups at the <scene name='37/372726/Tyr446_and_met641/4'>R2</scene> position of the cephalosporin backbone are able to interact with additional amino acid residues in PBP2a; specifically | ||
<scene name='37/372726/Tyr446_and_met641/3'>Tyr446 and Met641</scene>. As a result of tighter binding to PBP2a, ceftobiprole is able to more efficiently react with the serine active site residue and therefore inhibit the activity of PBP2a. | |||
