Different inhibition characteristics of intracellular transglutaminase activity by cystamine and cysteamine
Different inhibition characteristics of intracellular transglutaminase activity by cystamine and cysteamine
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DOI：
10.1038/emm.2004.74
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发表时间：
2004-12-31
影响因子：
12.8
通讯作者：
Kim, IG
中科院分区：
文献类型：
--
作者：
Jeon, JH;Lee, HJ;Kim, IG
胱胺（一种转谷氨酰胺酶 (TGase) 抑制剂）的治疗对多种疾病（包括 CAG 扩张障碍和白内障）具有有益作用。我们将胱胺的抑制特性与半胱胺的抑制特性进行了比较，半胱胺是一种预计存在于细胞内的胱胺的还原形式。胱胺是比半胱胺更有效的 TGase 抑制剂，在非还原条件下具有不同的动力学模式。相比之下，在还原条件下，胱胺的抑制效果与半胱胺相当。然而，尽管存在细胞质还原环境，胱胺对细胞内TGase活性的抑制作用比半胱胺更强，这表明胱胺本身通过形成混合二硫化物来抑制原位TGase活性。
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 nonreducing 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.