Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377817 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
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 Ki of 43 nM.
Graphical abstractSubstrate-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 Ki of 43 nM.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Zheng Yin, Sejal J. Patel, Wei-Ling Wang, Gang Wang, Wai-Ling Chan, K.R. Ranga Rao, Jenefer Alam, Duraiswamy A. Jeyaraj, Xinyi Ngew, Viral Patel, David Beer, Siew Pheng Lim, Subhash G. Vasudevan, Thomas H. Keller,