2008
DOI: 10.1128/aac.00961-07
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NS3 Peptide, a Novel Potent Hepatitis C Virus NS3 Helicase Inhibitor: Its Mechanism of Action and Antiviral Activity in the Replicon System

Abstract: Hepatitis C virus (HCV) chronic infections represent one of the major and still unresolved health problems because of low efficiency and high cost of current therapy. Therefore, our studies centered on a viral protein, the NS3 helicase, whose activity is indispensable for replication of the viral RNA, and on its peptide inhibitor that corresponds to a highly conserved arginine-rich sequence of domain 2 of the helicase. The NS3 peptide (p14) was expressed in bacteria. Its 50% inhibitory activity in a fluorometr… Show more

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Cited by 33 publications
(30 citation statements)
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References 48 publications
(55 reference statements)
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“…212 HCV helicase activity is inhibited in vitro by recombinant antibodies, 213,214 by RNA aptamers 215,216 and by peptides. 217,218 Targeting the nucleotide binding site of HCV-NS3 has proven exceedingly difficult, 219 although nucleotide-mimicking competitive inhibitors have been identified. 220,221 Ring-expanded nucleoside and nucleotide analogs have been shown to selectively inhibit HCV, West Nile Virus, and Japanese encephalitis virus NS3 helicases in vitro without affecting the activity of a control host helicase.…”
Section: Rna Helicases As Drug Targetsmentioning
confidence: 99%
“…212 HCV helicase activity is inhibited in vitro by recombinant antibodies, 213,214 by RNA aptamers 215,216 and by peptides. 217,218 Targeting the nucleotide binding site of HCV-NS3 has proven exceedingly difficult, 219 although nucleotide-mimicking competitive inhibitors have been identified. 220,221 Ring-expanded nucleoside and nucleotide analogs have been shown to selectively inhibit HCV, West Nile Virus, and Japanese encephalitis virus NS3 helicases in vitro without affecting the activity of a control host helicase.…”
Section: Rna Helicases As Drug Targetsmentioning
confidence: 99%
“…49 Helicase activity has been exploited therapeutically, with drug candidates in preclinical development for both HCV and herpes simplex virus (HSV). 50,51 Helicase ALPHAVIRUS ANTIVIRAL DRUG DEVELOPMENT activity of nsP2 may be amenable to HTS, as fluorometric assays have been developed for the HCV NS3 helicase. 51 Nonstructural protein 3 (nsP3) is a phosphoprotein that is essential for virus replication.…”
Section: Viral-directed Therapeutic Targetsmentioning
confidence: 99%
“…To some proteins, thermal unfolding follow partially [12] or highly [13,14] reversible steps, and the reversibility may decrease in the presence of denaturants or high pH values. To some other proteins, especially the multi-domain proteins, thermal unfoldings are usually irreversible [23,24].…”
Section: Introductionmentioning
confidence: 99%