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ツゲ ヒデアキ
TSUGE HIDEAKI
津下 英明 所属 京都産業大学 生命科学部 先端生命科学科 職種 教授 |
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| 言語種別 | 英語 |
| 発行・発表の年月 | 1999/09 |
| 形態種別 | 研究論文 |
| 査読 | 査読あり |
| 標題 | Structure based development of novel specific inhibitors for cathepsin L and cathepsin S in vitro and in vivo |
| 執筆形態 | その他 |
| 掲載誌名 | FEBS LETTERS |
| 出版社・発行元 | ELSEVIER SCIENCE BV |
| 巻・号・頁 | 458(1),pp.6-10 |
| 著者・共著者 | N Katunuma,E Murata,H Kakegawa,A Matsui,H Tsuzuki,H Tsuge,D Turk,Turk, V,M Fukushima,Y Tada,T Asao |
| 概要 | Specific inhibitors for cathepsin L and cathepsin S have been developed with the help of computer-graphic modeling based on the stereo-structure, The common fragment, N-(L- trans-carbamoyloxyrane-2-carbonyl)-phenylalanine-dimethyl-amide, is required for specific inhibition of cathepsin L, Seven novel inhibitors of the cathepsin L inhibitor Katunuma(CLIK) specifically inhibited cathepsin L at a concentration of 10(-7) M in vitro, while almost no inhibition of cathepsins B, C, S and IC was observed Four of the CLIKs are stable, and showed highly selective inhibition for hepatic cathepsin L in vivo. One of the CLIK inhibitors contains an aldehyde group, and specifically Inhibits cathepsin S at 10(-7) M in vitro. (C) 1999 Federation of European Biochemical Societies. |
| DOI | 10.1016/S0014-5793(99)01107-2 |
| ISSN | 0014-5793 |