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Bacterial Cell Wall Synthesis Enzyme (Transpeptidase) (PBP)

Target: PBP
Molecular classification: Enzyme

Overview

Transpeptidase enzymes play an indispensable role in constructing the bacterial cell wall by catalyzing the formation of peptide cross-links within the peptidogylcan layer. Their inhibition forms the basis for one of medicine’s most successful classes of antibacterial agents—the β-lactams—while changes or acquisition of alternative PBPs underlie major clinical challenges such as MRSA.

Other names: Penicillin-Binding Protein(s)PBP

Mechanism of action

Inhibition of transpeptidase activity by binding to the active site, preventing peptidoglycan cross-linking and leading to cell wall weakening and osmotic lysis.

Biological functions

Peptidoglycan synthesisCell wall biogenesisCross-linking of peptidoglycan

Disease associations

InfectionAntibiotic resistance

Safety considerations

Antibiotic resistance developmentSelection of resistant strains

Interacting drugs

Penicillins

2 more in the full profile.

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