Bioorganic & medicinal chemistry letters, 2006, Vol.16 (1), p.36-39
2006
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Details
- Autor(en) / Beteiligte
- Titel
- Peptide inhibitors of dengue virus NS3 protease. Part 1: Warhead
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2006, Vol.16 (1), p.36-39
- Ort / Verlag
- Oxford: Elsevier Ltd
- Erscheinungsjahr
- 2006
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Substrate-based tetrapeptide inhibitors with various warheads were designed, synthesized, and evaluated against the Dengue virus NS3 protease. Effective inhibition was achieved by peptide inhibitors with electrophilic warheads such as aldehyde, trifluoromethyl ketone, and boronic acid. A boronic acid has the highest affinity, exhibiting a K i of 43 nM. Substrate-based tetrapeptide inhibitors with various warheads were designed, synthesized, and evaluated against the Dengue virus NS3 protease. Effective inhibition was achieved by peptide inhibitors with electrophilic warheads such as aldehyde, trifluoromethyl ketone, and boronic acid. A boronic acid has the highest affinity, exhibiting a K i of 43 nM.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2005.09.062Titel-ID: cdi_proquest_miscellaneous_70196464
- Format
- –
- Schlagworte
- Antibiotics. Antiinfectious agents. Antiparasitic agents, Antiviral agents, Biological and medical sciences, Boronic Acids - chemistry, Chemistry, Pharmaceutical - methods, Dengue Virus - enzymology, Dengue virus NS3 protease, Dose-Response Relationship, Drug, Drug Design, Enzyme Inhibitors - pharmacology, Ketones - chemistry, Kinetics, Medical sciences, Models, Chemical, Peptide inhibitors, Peptides - chemistry, Peptides - pharmacology, Pharmacology. Drug treatments, Protease Inhibitors - chemistry, Protease Inhibitors - pharmacology, RNA Helicases - antagonists & inhibitors, RNA Helicases - chemistry, Serine Endopeptidases - chemistry, Substrate Specificity, Time Factors, Viral Nonstructural Proteins - antagonists & inhibitors, Viral Nonstructural Proteins - chemistry