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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This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/3.0/) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.
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Jeon, JH., Lee, HJ., Jang, GY. et al. Different inhibition characteristics of intracellular transglutaminase activity by cystamine and cysteamine. Exp Mol Med 36, 576–581 (2004). https://doi.org/10.1038/emm.2004.74
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DOI: https://doi.org/10.1038/emm.2004.74
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