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- ceftobiprole and ceftaroline- that have anti-MRSA activity have been developed. Ceftobiprole is able to inhibit PBP2a because additional chemical groups at the R2 position of ceftobiprole are able to interact with additional amino acid residues in PBP2a; specifically Tyr446 and Met641, and increase the association of ceftobiprole with 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. | 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- ceftobiprole and ceftaroline- that have anti-MRSA activity have been developed. Ceftobiprole is able to inhibit PBP2a because additional chemical groups at the R2 position of ceftobiprole are able to interact with additional amino acid residues in PBP2a; specifically Tyr446 and Met641, and increase the association of ceftobiprole with 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. | ||
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