Ontology highlight
ABSTRACT:
SUBMITTER: Behnam MA
PROVIDER: S-EPMC4160758 | biostudies-literature | 2014 Sep
REPOSITORIES: biostudies-literature
Behnam Mira A M MA Nitsche Christoph C Vechi Sérgio M SM Klein Christian D CD
ACS medicinal chemistry letters 20140718 9
Dengue virus protease is a promising target for the development of antiviral drugs. We describe here a two-step rational optimization that led to the discovery of the potent inhibitor 35 with nanomolar binding affinity at dengue protease serotype 2 (IC50 = 0.6 μM, K i = 0.4 μM). First, a large number of natural and non-natural amino acids were screened at the C-terminal position of the previously reported, canonical peptide sequence (Cap-Arg-Lys-Nle-NH2). Compared to the reference compound 1 (Bz ...[more]