Naka Hiromi, Teruya Kenta, Bang Jeong Kyu, Aimoto Saburo, Tatsumi Tadashi, Konno Hiroyuki, Nosaka Kazuto, Akaji Kenichi
Institute for Protein Research, Osaka University, Osaka 565-0871, Japan.
Bioorg Med Chem Lett. 2006 Jul 15;16(14):3761-4. doi: 10.1016/j.bmcl.2006.04.056. Epub 2006 May 8.
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.
首次阐明了人嗜T淋巴细胞病毒1型蛋白酶PR/p3位点底物识别及其抑制所必需的核心序列。从含有PR/p3位点一部分的肽的切割速率来看，发现一种七肽是底物识别所需的最小序列。使用含有羟乙胺二肽等排体的合成抑制剂表明，一个四肽序列对于实现有效抑制是必要的。
