Tripeptide inhibitors of dengue and West Nile virus NS2B-NS3 protease

Simple item page
dc.catalogadoraba
dc.contributor.authorSchüller, Andreas
dc.contributor.authorYin, Z.
dc.contributor.authorChia, C. S. B.
dc.contributor.authorDoan, D. N. P.
dc.contributor.authorKim, H.
dc.contributor.authorShang, L.
dc.contributor.authorLoh, T. P.
dc.contributor.authorHill, J.
dc.contributor.authorVasudevan, S. G.
dc.date.accessioned2025-02-06T18:46:51Z
dc.date.available2025-02-06T18:46:51Z
dc.date.issued2011
dc.description.abstractA series of tripeptide aldehyde inhibitors were synthesized and their inhibitory effect against dengue virus type 2 (DENV2) and West Nile virus (WNV) NS3 protease was evaluated side by side with the aim to discover potent flaviviral protease inhibitors and to examine differences in specificity of the two proteases. The synthesized inhibitors feature a varied N-terminal cap group and side chain modifications of a P2-lysine residue. In general a much stronger inhibitory effect of the tripeptide inhibitors was observed toward WNV protease. The inhibitory concentrations against DENV2 protease were in the micromolar range while they were submicromolar against WNV. The data suggest that a P2-arginine shifts the specificity toward DENV2 protease while WNV protease favors a lysine in the P2 position. Peptides with an extended P2-lysine failed to inhibit DENV2 protease suggesting a size-constrained S2 pocket. Our results generally encourage the investigation of di- and tripeptide aldehydes as inhibitors of DENV and WNV protease.
dc.fuente.origenSIPA
dc.identifier.doi10.1016/j.antiviral.2011.07.002
dc.identifier.issn0166-3542
dc.identifier.urihttps://doi.org/10.1016/j.antiviral.2011.07.002
dc.identifier.urihttps://doi.org/10.1016/j.antiviral.2011.07.002
dc.identifier.urihttps://repositorio.uc.cl/handle/11534/102168
dc.identifier.wosidWOS:000295860800012
dc.information.autorucFacultad de Ciencias Biológicas; Schüller, Andreas; 0000-0002-4443-4279; 207692
dc.issue.numero1
dc.language.isoen
dc.nota.accesocontenido parcial
dc.pagina.final101
dc.pagina.inicio96
dc.revistaANTIVIRAL RESEARCH
dc.rightsacceso restringido
dc.subjectDengue virus
dc.subjectWest Nile virus
dc.subjectNS2B–NS3 protease
dc.subjectPeptide inhibitor
dc.subject.ddc570
dc.subject.deweyBiologíaes_ES
dc.titleTripeptide inhibitors of dengue and West Nile virus NS2B-NS3 protease
dc.typeartículo
dc.volumen92
sipa.codpersvinculados207692
Files
Collections
Artículos de revistas