Different inhibition characteristics of intracellular transglutaminase activity by cystamine and cysteamine

Ju Hong Jeon; Hye Jin Lee; Gi Yong Jang; Chai Wan Kim; Dong Myung Shin; Sung Yup Cho; Eui Ju Yeo; Sang Chul Park; In Gyu Kim

doi:10.1038/emm.2004.74

Different inhibition characteristics of intracellular transglutaminase activity by cystamine and cysteamine

Ju Hong Jeon, Hye Jin Lee, Gi Yong Jang, Chai Wan Kim, Dong Myung Shin, Sung Yup Cho, Eui Ju Yeo, Sang Chul Park, In Gyu Kim

Research output: Contribution to journal › Article › peer-review

34 Scopus citations

Abstract

The treatment of cystamine, a transglutaminase (TGase) inhibitor, has beneficial effects in several diseases including CAG-expansion disorders and cataract. We compared the inhibition characteristics of cystamine with those of cysteamine, a reduced form of cystamine expected to be present inside cells. Cystamine is a more potent inhibitor for TGase than cysteamine with different kinetics pattern in a non-reducing condition. By contrast, under reducing conditions, the inhibitory effect of cystamine was comparable with that of cysteamine. However, cystamine inhibited intracellular TGase activity more strongly than cysteamine despite of cytoplasmic reducing environment, suggesting that cystamine itself inhibits in situ TGase activity by forming mixed disulfides.

Original language	English (US)
Pages (from-to)	576-581
Number of pages	6
Journal	Experimental and Molecular Medicine
Volume	36
Issue number	6
DOIs	https://doi.org/10.1038/emm.2004.74
State	Published - Dec 31 2004

Keywords

Cystamine
Cysteamine
Inhibitor
Polyamine
Transglutaminase

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Clinical Biochemistry

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10.1038/emm.2004.74

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abstract = "The treatment of cystamine, a transglutaminase (TGase) inhibitor, has beneficial effects in several diseases including CAG-expansion disorders and cataract. We compared the inhibition characteristics of cystamine with those of cysteamine, a reduced form of cystamine expected to be present inside cells. Cystamine is a more potent inhibitor for TGase than cysteamine with different kinetics pattern in a non-reducing condition. By contrast, under reducing conditions, the inhibitory effect of cystamine was comparable with that of cysteamine. However, cystamine inhibited intracellular TGase activity more strongly than cysteamine despite of cytoplasmic reducing environment, suggesting that cystamine itself inhibits in situ TGase activity by forming mixed disulfides.",

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AU - Jeon, Ju Hong

AU - Lee, Hye Jin

AU - Jang, Gi Yong

AU - Kim, Chai Wan

AU - Shin, Dong Myung

AU - Cho, Sung Yup

AU - Yeo, Eui Ju

AU - Park, Sang Chul

AU - Kim, In Gyu

PY - 2004/12/31

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AB - The treatment of cystamine, a transglutaminase (TGase) inhibitor, has beneficial effects in several diseases including CAG-expansion disorders and cataract. We compared the inhibition characteristics of cystamine with those of cysteamine, a reduced form of cystamine expected to be present inside cells. Cystamine is a more potent inhibitor for TGase than cysteamine with different kinetics pattern in a non-reducing condition. By contrast, under reducing conditions, the inhibitory effect of cystamine was comparable with that of cysteamine. However, cystamine inhibited intracellular TGase activity more strongly than cysteamine despite of cytoplasmic reducing environment, suggesting that cystamine itself inhibits in situ TGase activity by forming mixed disulfides.

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KW - Transglutaminase

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Different inhibition characteristics of intracellular transglutaminase activity by cystamine and cysteamine

Abstract

Keywords

ASJC Scopus subject areas

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