D-ASPARTIC ACID-CONTAINING PROTEIN-SPLITTING ENZYME INHIBITOR
|Posted date||Jun 8, 2011|
|Date of filing||Mar 30, 2001|
|Date of publication of application||Oct 9, 2002|
|Date of registration||Feb 8, 2008|
|Title||D-ASPARTIC ACID-CONTAINING PROTEIN-SPLITTING ENZYME INHIBITOR|
PROBLEM TO BE SOLVED: To provide an inhibitor for an aspartic acid-containing protein-splitting enzyme, particularly for D-aspartic acid endopeptidase(DAEP), in view of the fact that the existing inhibitor is only lactacystine known as a proteasome inhibitor however, it is poor in sensitivity, and its drawback being that it also acts on proteasome.
SOLUTION: This inhibitor, i-DAEP, is obtained by paying attention to that DAEP specifically splits a substrate including D-Asp and by designing such a compound as to inhibit DAEP activity by blocking the active center of DAEP by the analog. This inhibitor thus obtained is composed of an amino acid sequence including D-asp-CH2Cl or a derivative thereof, preferably of benzoyl- Arg-His-D-Asp-CH2Cl, biotinyl-Arg-His-D-Asp-CH2Cl or biotinyl-Gly-Gly-D-Asp- CH2Cl.
|Outline of related art and contending technology||
|Field of industrial application||
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|State of application right||Registered|
Contact Information for " D-ASPARTIC ACID-CONTAINING PROTEIN-SPLITTING ENZYME INHIBITOR"
- Japan Science and Technology Agency Department of Intellectual Property Management
- URL: http://www.jst.go.jp/chizai/
- Address: 5-3, Yonbancho, Chiyoda-ku, Tokyo, Japan , 102-8666
- Fax: 81-3-5214-8476