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• W2030376296 abstract "A highly sensitive screening assay based on electrochemical impedance spectroscopy (EIS) has been developed for detecting HIV-1 protease (PR) and subsequent evaluation of its corresponding inhibitors at picomolar levels. The assay format was based on the immobilization of the thiol terminated ferrocene(Fc)-pepstatin conjugate on a single-walled carbon nanotube/gold nanoparticle (SWCNT/AuNP) modified gold electrode. The alteration of the interfacial properties of electrodes upon HIV-1 PR and Fc-pepstatin conjugate interaction was traced by EIS. On the basis of the charge transfer resistance data obtained and using a mixed kinetic and diffusion model, this procedure was capable of detecting picomolar HIV-1 PR owing to the specific binding of this enzyme to Fc modified pepstatin. A competitive inhibition assay format was then performed using four potent HIV-1 PR inhibitors. The estimated inhibition constant ( K i) attested that lopinavir/ritonavir ( K i = 20 +/- 3 pM) and saquinavir ( K i = 57 +/- 8 pM) even at 10 pM competed strongly with pepstatin for effective binding to HIV-1 PR. Indinavir ( K i = 630 +/- 22 pM) only competed well with pepstatin at a much higher concentration (1 nM). No significant inhibitory effect was observed for the fosamprenavir ( K i =11 +/- 0.5 nM) as expected from this pro-drug. Such results agreed well with the values reported in the literature. This assay format is a definite asset for the expedited development of effective HIV-1 PR inhibitors with low molecular weights." @default.
• W2030376296 created "2016-06-24" @default.
• W2030376296 creator A5005028846 @default.
• W2030376296 creator A5050123820 @default.
• W2030376296 date "2008-08-16" @default.
• W2030376296 modified "2023-10-01" @default.
• W2030376296 title "Impedance Method for Detecting HIV-1 Protease and Screening For Its Inhibitors Using Ferrocene−Peptide Conjugate/Au Nanoparticle/Single-Walled Carbon Nanotube Modified Electrode" @default.
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• W2030376296 doi "https://doi.org/10.1021/ac801174r" @default.
• W2030376296 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/18707132" @default.
• W2030376296 hasPublicationYear "2008" @default.
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