Sandbox 128: Difference between revisions
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==='''B-Lactams that Inhibit PBP2a'''=== | ==='''B-Lactams that Inhibit PBP2a'''=== | ||
MRSA becomes resistant to almost all B-Lactams by acquiring an alternative TP, PBP2a, that is neither bound nor inhibited by B-Lactams. Recently, two cephlosporins- <scene name='37/372728/Ceftobiprole/3'>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='37/372728/R2_group/7'>R2</scene> position of ceftobiprole are able to interact with additional amino acid residues in PBP2a; specifically <scene name='37/372728/Tyr446_met641_interaction/ | MRSA becomes resistant to almost all B-Lactams by acquiring an alternative TP, PBP2a, that is neither bound nor inhibited by B-Lactams. Recently, two cephlosporins- <scene name='37/372728/Ceftobiprole/3'>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='37/372728/R2_group/7'>R2</scene> position of ceftobiprole are able to interact with additional amino acid residues in PBP2a; specifically | ||
<scene name='37/372728/Tyr446_met641_interaction/4'>Tyr446 and Met641, and increase the association of ceftobiprole with PBP2a</scene>. | |||
As such, ceftobiprole is (shown as colors of the atom types [[CPK]]) is able to more efficiently react with Ser403 and therefore inhibit the activity of PBP2a. | As such, ceftobiprole is (shown as colors of the atom types [[CPK]]) is able to more efficiently react with Ser403 and therefore inhibit the activity of PBP2a. | ||