Peptide inhibitors of Dengue virus NS3 protease. Part 1: Warhead.

ID: ALA1147780

Journal: Bioorg Med Chem Lett

Title: Peptide inhibitors of Dengue virus NS3 protease. Part 1: Warhead.

Authors: Yin Z, Patel SJ, Wang WL, Wang G, Chan WL, Rao KR, Alam J, Jeyaraj DA, Ngew X, Patel V, Beer D, Lim SP, Vasudevan SG, Keller TH.

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.

CiteXplore: 16246553

DOI: 10.1016/j.bmcl.2005.09.062

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