Sandbox 127: 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 | MRSA becomes resistant to β-lactams by acquiring an alternative PBP, PBP2a, that is | ||
neither bound nor inhibited by β-lactams. Recently, two cephalosporins – | neither bound nor inhibited by β-lactams. Recently, two cephalosporins – | ||
<scene name='37/372724/ | <scene name='37/372724/Medicine_interaction/4'>cefobiprole</scene> and | ||
ceftaroline – that have anti-MRSA activity have been developed. Ceftobiprole is able to | ceftaroline – that have anti-MRSA activity have been developed. Ceftobiprole is able to | ||
inhibit PBP2a because additional chemical groups at the | inhibit PBP2a because additional chemical groups at the | ||
<scene name='37/372724/ | <scene name='37/372724/Medicine_interaction/3'>R2</scene> | ||
position of the cephalosporin backbone are able to interact with additional amino acid | position of the cephalosporin backbone are able to interact with additional amino acid | ||
residues in PBP2a; specifically | residues in PBP2a; specifically | ||
<scene name='37/372724/ | <scene name='37/372724/Medicine_interaction/2'>Tyr446 and Met641</scene>. | ||
<scene name='37/372724/Medicine_interaction/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 as a result of ceftobiprole <scene name='37/372724/R2_interaction/6'>tighter binding</scene> to pbp2a. unlike penicillin, this results in inhibition of pbp2a | |||
<scene name='37/372724/R2_interaction/6'>tighter binding</scene> | |||
