Navigation überspringen
Universitätsbibliothek Heidelberg
Status: Bibliographieeintrag

Verfügbarkeit
Standort: ---
Exemplare: ---
heiBIB
 Online-Ressource
Verfasst von:Nitsche, Christoph [VerfasserIn]   i
 Behnam, Mira A. M. [VerfasserIn]   i
 Steuer, Christian [VerfasserIn]   i
 Klein, Christian D. [VerfasserIn]   i
Titel:Retro peptide-hybrids as selective inhibitors of the Dengue virus NS2B-NS3 protease
Verf.angabe:Christoph Nitsche, Mira A.M. Behnam, Christian Steuer, Christian D. Klein
E-Jahr:2012
Jahr:26 February 2012
Umfang:8 S.
Fussnoten:Gesehen am 11.06.2018
Titel Quelle:Enthalten in: Antiviral research
Ort Quelle:Amsterdam [u.a.] : Elsevier Science, 1981
Jahr Quelle:2012
Band/Heft Quelle:94(2012), 1, Seite 72-79
ISSN Quelle:1872-9096
Abstract:New chemotherapeutics against Dengue virus and related flaviviruses are of growing interest in antiviral drug discovery. The viral serine protease NS2B-NS3 is a promising target for the development of such agents. Drug-like inhibitors of this protease with high affinity to the target are not available at the moment. The present work describes the discovery of new retro di- and tripeptide hybrids that do not necessarily require an electrophilic “warhead” to achieve affinities in the low micromolar range. The most active sequence in this series is the tripeptide R-Arg-Lys-Nle-NH2. By variation of the N-terminal groups (R) it could be shown that the previously described arylcyanoacrylamide moiety is a preferable group in this position. Retro tripeptide hybrids were found to be more active and more selective than retro dipeptide hybrids. A significant selectivity towards the Dengue virus protease could be shown in a counterscreen with thrombin and the West Nile virus protease. Alternative sequences to R-Arg-Lys-Nle-NH2 did not have higher affinities towards the Dengue virus protease, similar to retro-inverse sequences with d-lysine and d-arginine residues. The results of a competition assay with the known inhibitor aprotinin indicate that the N-terminal arylcyanoacrylamide residue of this compound class binds near the catalytic center of the enzyme.
DOI:doi:10.1016/j.antiviral.2012.02.008
URL:Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.

Volltext: http://dx.doi.org/10.1016/j.antiviral.2012.02.008
 Volltext: http://www.sciencedirect.com/science/article/pii/S0166354212000411
 DOI: https://doi.org/10.1016/j.antiviral.2012.02.008
Datenträger:Online-Ressource
Sprache:eng
Sach-SW:Dengue virus
 Hybrid retro peptides
 NS2B-NS3 protease
 Thrombin
 West Nile virus
K10plus-PPN:1576212165
Verknüpfungen:→ Zeitschrift

Permanenter Link auf diesen Titel (bookmarkfähig):  https://katalog.ub.uni-heidelberg.de/titel/68259868   QR-Code
zum Seitenanfang