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
Otaka, Akira
The University of Tokushima
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Keywords | Aromatization
Caged compound
Cysteine protease
Protective Group
UV-responsive
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Content Type |
Journal Article
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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.
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Journal Title |
Tetrahedron
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ISSN | 00404020
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NCID | AA00861787
AA11539786
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Publisher | Elsevier Ltd.
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Volume | 67
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Issue | 46
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Start Page | 8879
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End Page | 8886
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Published Date | 2011-09-21
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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/
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EDB ID | |
DOI (Published Version) | |
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language |
eng
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TextVersion |
Author
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departments |
Pharmaceutical Sciences
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