ID 111905
著者
Morishita, Ko The University of Tokushima
Yamaguchi, Keiko The University of Tokushima
Ding, Hao The University of Tokushima
Ebisuno, Koji The University of Tokushima
Sato, Kohei The University of Tokushima
Yamamoto, Jun The University of Tokushima
Akaji, Kenichi Kyoto Pharmaceutical University
キーワード
Aromatization
Caged compound
Cysteine protease
Protective Group
UV-responsive
資料タイプ
学術雑誌論文
抄録
Cysteine proteases are attractive drug targets due to their involvement in a wide variety of diseases. To evaluate the potential of a particular protease as a drug target, use of a reagent that controls activity of the protease is indispensable. In this context, we have developed a catch-and-release reagent that first forms a covalent bond with the active center thiol of a cysteine protease to suppress its activity and then is removed by UV-irradiation to release the parent active protease. In this paper, the design and synthesis of a catch-and-release reagent of thiols are described. Its application to caging (catch) and UV-induced uncaging (release) of a model peptide derived from an active site of caspase-9 and introduction of a recognition moiety on the reagent are also reported.
掲載誌名
Tetrahedron
ISSN
00404020
cat書誌ID
AA00861787
AA11539786
出版者
Elsevier Ltd.
67
46
開始ページ
8879
終了ページ
8886
発行日
2011-09-21
権利情報
© 2011. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/
EDB ID
出版社版DOI
出版社版URL
フルテキストファイル
言語
eng
著者版フラグ
著者版
部局
薬学系