Article
Evaluation of peptide-aldehyde inhibitors using R188I mutant of SARS 3CL protease as a proteolysis-resistant mutant.
Bioorganic & medicinal chemistry - 1 Nov 2008
Akaji Kenichi, Konno Hiroyuki, Onozuka Mari, Makino Ayumi, Saito Hiroyuki, Nosaka Kazuto
Abstract excerpt
The 3C-like (3CL) protease of the severe acute respiratory syndrome (SARS) coronavirus is a key enzyme for the virus maturation. We found for the first time that the mature SARS 3CL protease is subject to degradation at 188Arg/189Gln. Replacing Arg with Ile at position 188 rendered the protease resistant to proteolysis. The R188I mutant digested a conserved undecapeptide substrate with a K(m) of 33.8 microM and...
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