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Evaluations of substrate specificity and inhibition at PR/p3 cleavage site of HTLV-1 protease
Authors:Naka Hiromi  Teruya Kenta  Bang Jeong Kyu  Aimoto Saburo  Tatsumi Tadashi  Konno Hiroyuki  Nosaka Kazuto  Akaji Kenichi
Institution:Institute for Protein Research, Osaka University, Osaka 565-0871, Japan.
Abstract:Core sequences necessary for substrate recognition and its inhibition at the PR/p3 site of HTLV-1 protease were clarified for the first time. From the cleavage rates of peptides containing a part of the PR/p3 site, a heptapeptide was found to be the minimal sequence required for substrate recognition. The use of synthetic inhibitors containing hydroxyethylamine dipeptide isostere indicated that a tetrapeptide sequence was necessary to achieve potent inhibition.
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