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Peptide inhibitors of Dengue virus NS3 protease. Part 1: Warhead.
Yin, Zheng; Patel, Sejal J; Wang, Wei-Ling; Wang, Gang; Chan, Wai-Ling; Rao, K R Ranga; Alam, Jenefer; Jeyaraj, Duraiswamy A; Ngew, Xinyi; Patel, Viral; Beer, David; Lim, Siew Pheng; Vasudevan, Subhash G; Keller, Thomas H.
Affiliation
  • Yin Z; Novartis Institute for Tropical Diseases, 10 Biopolis Road, 05-01 Chromos, Singapore 138670, Singapore. zheng.yin@novartis.com
Bioorg Med Chem Lett ; 16(1): 36-9, 2006 Jan 01.
Article in En | MEDLINE | ID: mdl-16246553
ABSTRACT
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.
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Collection: 01-internacional Database: MEDLINE Main subject: Peptides / Protease Inhibitors / Drug Design / Chemistry, Pharmaceutical / Viral Nonstructural Proteins / Dengue Virus Type of study: Prognostic_studies Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2006 Document type: Article Affiliation country: Singapore
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PubMed Links

Collection: 01-internacional Database: MEDLINE Main subject: Peptides / Protease Inhibitors / Drug Design / Chemistry, Pharmaceutical / Viral Nonstructural Proteins / Dengue Virus Type of study: Prognostic_studies Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2006 Document type: Article Affiliation country: Singapore