Sandbox 127: Difference between revisions
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efficiently react with the serine active site residue and therefore inhibit the activity of | efficiently react with the serine active site residue and therefore inhibit the activity of | ||
PBP2a. | PBP2a. | ||
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/7'>R2</scene> | |||
position of the cephalosporin backbone are able to interact with additional amino acid | |||
residues in PBP2a; specifically | |||
<scene name='37/372724/Tyr446_and_met641_label/2'>Tyr446 and Met641</scene>. | |||
As a result of ceftobiprole <scene name='37/372724/R2_interaction/4⅝'>tighter binding</scene> to PBP2a as highlighted in green , <scene name='37/372724/Ceftobiprole_in_cpk/1'>the medicine</scene>, shown as colors of the atom types ([[CPK]]), is able to more efficiently react with the serine active site residue and therefore inhibit the activity of PBP2a. | |||
<scene name='37/372724/R2_interaction/6'>tighter binding</scene> | |||
