Inhibition of human epidermal transglutaminases in vitro and in vivo by tyrosinamidomethyl dihydrohaloisoxazoles.
Inhibition of human epidermal transglutaminases in vitro and in vivo by tyrosinamidomethyl dihydrohaloisoxazoles.
复制标题
酪氨酸酰胺甲基二氢卤代异恶唑在体外和体内抑制人表皮转谷氨酰胺酶。
DOI：
10.1111/1523-1747.ep12479331
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发表时间：
1991
期刊：
影响因子：
--
通讯作者：
Akers,W
中科院分区：
文献类型：
--
作者：
Goldsmith,LA;DeYoung,LM;Falciano,V;Ballaron,SJ;Akers,W
酪氨酸酰胺甲基二氢卤代异恶唑（THX）不可逆地抑制分离的表皮转氨酶和离子载体诱导的恶性人角质形成细胞的细胞被膜形成。在10- 5 M THX中培养5天的培养的人包皮角质形成细胞中，可溶性和颗粒性转氨酶分别被抑制90%和44- 51%。自发细胞包膜形成被抑制高达54%。当THX处理的角质形成细胞与10- 5 M视黄酸（RA）同时孵育时，与单独使用任何一种药物相比，细胞包膜形成的抑制作用增强。抑制剂在与胎牛血清或脱脂血清孵育的角质形成细胞中同样有效。THX作用于正常人胸部皮肤9 d后，从负压疱表皮分离的可溶性和颗粒性转氨酶分别被抑制30%和40%。THX可有效抑制转氨酶活性增加的疾病中的可溶性和颗粒性转氨酶活性。
Tyrosinamidomethyl dihydrohaloisoxazoles (THX) irreversibly inhibit isolated epidermal transglutaminases and ionophore-induced cell envelope formation in malignant human keratinocytes. In cultured human foreskin keratinocytes cultured in 10-5M THX for 5 days, soluble and particulate transglutaminases were inhibited by 90% and 44-51%, respectively. Spontaneous cell envelope formation was inhibited up to 54%. When THX-treated keratinocytes were simultaneously incubated with 10-5M retinoic acid (RA), there was enhanced inhibition of cell envelope formation compared to either agent alone. The inhibitors were equally effective in keratinocytes incubated with fetal calf serum or delipidized serum. After THX was applied to normal human thoracic skin in vivo for 9 d, the soluble and particulate transglutaminases isolated from suction blister epidermis were inhibited 30% and 40%, respectively. THX may be effective in inhibiting both soluble and particulate transglutaminase activity in disorders with increased transglutaminase activity.