Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2006 Jan 1;16(1):36-9. Epub 2005 Oct 21.

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

Author information

1
Novartis Institute for Tropical Diseases, 10 Biopolis Road, 05-01 Chromos, Singapore 138670, Singapore. zheng.yin@novartis.com

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.

PMID:
16246553
DOI:
10.1016/j.bmcl.2005.09.062
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center