ID 111905
Author
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
Keywords
Aromatization
Caged compound
Cysteine protease
Protective Group
UV-responsive
Content Type
Journal Article
Description
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.
Journal Title
Tetrahedron
ISSN
00404020
NCID
AA00861787
AA11539786
Publisher
Elsevier Ltd.
Volume
67
Issue
46
Start Page
8879
End Page
8886
Published Date
2011-09-21
Rights
© 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
DOI (Published Version)
URL ( Publisher's Version )
FullText File
language
eng
TextVersion
Author
departments
Pharmaceutical Sciences