[3 h]乙酰唑胺结合碳酸酐酶在正常和转化细胞。

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Meyerson LR,内斯塔D

[3 h]乙酰唑胺结合碳酸酐酶在正常和转化细胞。

生物化学杂志。1991年3月15-Apr 1; 41 (6): 995 - 1000。

PubMed ID

1901209 (在PubMed

]

文摘

的绑定[3 h]乙酰唑胺(AZ),一个碳酸酐酶(CA)抑制剂,可溶性和颗粒形式的CA进行了研究。来源分析纯化CA II,成年鼠大脑皮层,少突细胞和神经丰富的准备工作;其他培养小鼠神经胶质细胞鼠神经胶质瘤,鼠肝癌和人类胶质母细胞瘤细胞。CA酶活性在相同的准备也化验孵化期间遵循pH值的变化。凝胶渗透色谱方法开发评估[3 h] AZ绑定可溶性钙、玻璃纤维过滤器真空过滤时用于微粒CA绑定。饱和的特定绑定[3 h] AZ鼠皮质可溶性和颗粒CA准备了。计算机辅助数据分析估计的绑定参数[3 h] AZ可溶性鼠皮质CA Bmax = 0.38 + / - 0.13 pmol /毫克蛋白和Kd = 34.7 + / - 17.5海里。大鼠皮质颗粒分数Bmax是2.05 + / - 0.28 pmol / mg Kd的蛋白107.1 + / - 24.2海里。纯化牛CA-II绑定1.15 + / - 0.19 pmol [3 h]阿兹/ mg Kd的蛋白54.0 + / - 3.4海里。pH值最适条件[3 h] AZ绑定可溶性和微粒CA在6.5和7.5之间。 Binding was linear with respect to protein up to 1.0 mg/mL. The particulate fraction bound 3-4 times more [3H]ligand per unit protein than the soluble fraction. Interestingly, no detectable CA enzyme activity or [3H]AZ binding was observed in the soluble or particulate fractions of human glioblastoma, rat C-6 glioma or rat hepatoma cells. Binding of [3H]AZ to other soluble enzymes or proteins was negligible. In competition binding experiments, a rank order of inhibition of [3H]AZ binding to rat cortical CA by established CA inhibitors was: dichlorphenamide greater than acetazolamide greater than or equal to benzolamide greater than methazolamide greater than hydrochlorothiazide greater than or equal to sulfanilamide. [3H]AZ binding was not affected by other classes of pharmacologic characterizing agents. The binding of [3H]AZ to the CA enzyme molecule is highly specific and sensitive and may prove useful in vitro or in situ as a probe for this enzyme.

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药物靶点

药物	目标	类	生物	药理作用	行动
Methyclothiazide	碳酸酐酶2	蛋白质	人类	未知的	抑制剂	细节