ACYCLOVIR: Mechanisms Step 1 Activation- conversion to Acyclovir monophosphate(Acyclovir-MP) ACYCLOVIR Binds 200x more strongly to HS virus thymidine kinase than to host TK Viral thymidine Kinase (TK) Viral Tk phosphorylates 3x106 times faster than host tK -Acyclovir-MP is primarily produced in the infected cells Acyclovir-MP (Selectivity! The overall rate of conversion in infected cells -30-20-fold fasterACYCLOVIR: Mechanisms • Activation – conversion to Acyclovir monophosphate (Acyclovir-MP) • • Binds 200x more strongly to HS virus thymidine kinase than to host TK • Viral TK phosphorylates 3x106 times faster than host TK – Acyclovir-MP is primarily produced in the infected cells (Selectivity!!!). • The overall rate of conversion in infected cells – 30-20-fold faster. ACYCLOVIR Viral thymidine Kinase (TK) Acyclovir-MP Step 1