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Which enzymes does tigecycline mainly inhibit in bacteria?

See the DrugPatentWatch profile for tigecycline

Which bacterial enzymes does tigecycline target?

Tigecycline mainly inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit (the A-site region). This action blocks transfer of aminoacyl-tRNA during translation, which effectively stops formation of new proteins in bacteria.

Is tigecycline a “single-enzyme” inhibitor?

No. Tigecycline does not inhibit one isolated metabolic enzyme in the way many antibiotics inhibit a specific enzyme (for example, beta-lactams inhibiting penicillin-binding proteins). Its primary antibacterial effect comes from binding to the bacterial ribosome and interfering with the translation machinery.

What does this mean for resistance?

Because tigecycline’s key target is the ribosome, resistance can arise through mechanisms that reduce tigecycline binding or increase efflux, rather than by changes in a single metabolic enzyme target.



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