Micro-PET imaging of hepatitis C virus NS3/4A protease activity using a protease-activatable retention probe.

ABSTRACT: Hepatitis C virus (HCV) NS3/4A protease is an attractive target for direct-acting antiviral agents. Real-time tracking of the NS3/4A protease distribution and activity is useful for clinical diagnosis and disease management. However, no approach has been developed that can systemically detect NS3/4A protease activity or distribution. We designed a protease-activatable retention probe for tracking HCV NS3/4A protease activity via positron emission topography (PET) imaging. A cell-penetrating probe was designed that consisted of a cell-penetrating Tat peptide, HCV NS3/4A protease substrate, and a hydrophilic domain. The probe was labeled by fluorescein isothiocyanate (FITC) and ¹²⁴I in the hydrophilic domain to form a TAT-ΔNS3/4A-¹²⁴I-FITC probe. Upon cleavage at

SUBMITTER: Chuang CH 

PROVIDER: S-EPMC9672079 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature