Sandbox 126: Difference between revisions
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==='''Mechanism of Action of Beta-Lactam Antibiotics'''=== | ==='''Mechanism of Action of Beta-Lactam Antibiotics'''=== | ||
The beta-lactam antibiotics irreversibly bind to and inhibit TPs. This results in the disruption of peptidoglycan synthesis and ultimately cell growth. Specifically, beta-lactams, such as penicillin and the anti-MRSA cephalosporins, ceftobiprole and ceftaroline, are molecular mimics of the peptidoglycan D-Ala-D-Ala moiety; the normal TP substrate (Figure 3; Tipper and Strominger, 1965). Therefore, they “trick” the TP active site serine residue to react with them, resulting in the irreversible inhibition of TP activity and of cell wall synthesis. | The beta-lactam antibiotics irreversibly bind to and inhibit TPs. This results in the disruption of peptidoglycan synthesis and ultimately cell growth. Specifically, beta-lactams, such as penicillin and the anti-MRSA cephalosporins, ceftobiprole and ceftaroline, are molecular mimics of the peptidoglycan D-Ala-D-Ala moiety; the normal TP substrate (Figure 3; Tipper and Strominger, 1965). Therefore, they “trick” the TP active site serine residue to react with them, resulting in the irreversible inhibition of TP activity and of cell wall synthesis. | ||
Figure 3. Mechanism of action of beta-lactams. A. Chemical structure of penicillin, a beta-lactam antibiotic. B. Chemical structure of the peptidoglycan D-Ala-D-Ala moiety, the normal TP substrate. C. Superimposition of the D-Ala-D-Ala moiety (red) with penicillin (black). The beta-lactams mimic the structure of the D-Ala-D-Ala moiety of peptidoglycan. This ensures TPs react with beta-lactams. | [[Image:DalMimic.jpg|thumb|alt= Alt text| Figure 3. Mechanism of action of beta-lactams. A. Chemical structure of penicillin, a beta-lactam antibiotic. B. Chemical structure of the peptidoglycan D-Ala-D-Ala moiety, the normal TP substrate. C. Superimposition of the D-Ala-D-Ala moiety (red) with penicillin (black). The beta-lactams mimic the structure of the D-Ala-D-Ala moiety of peptidoglycan. This ensures TPs react with beta-lactams.|550px]] | ||
