Evaluations of substrate specificity and inhibition at PR/p3 cleavage site of HTLV-1 protease |
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Authors: | Naka Hiromi Teruya Kenta Bang Jeong Kyu Aimoto Saburo Tatsumi Tadashi Konno Hiroyuki Nosaka Kazuto Akaji Kenichi |
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Affiliation: | Institute for Protein Research, Osaka University, Osaka 565-0871, Japan. |
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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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