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首页> 外文期刊>Cell and Tissue Research >Anti-neoplastic effect of protein kinase CK2 inhibitor, 2-dimethylamino-4,5,6,7-tetrabromobenzimidazole (DMAT), on growth and hormonal activity of human adrenocortical carcinoma cell line (H295R) in vitro
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Anti-neoplastic effect of protein kinase CK2 inhibitor, 2-dimethylamino-4,5,6,7-tetrabromobenzimidazole (DMAT), on growth and hormonal activity of human adrenocortical carcinoma cell line (H295R) in vitro

机译:蛋白激酶CK2抑制剂2-二甲基氨基-4,5,6,7-四溴苯并咪唑(DMAT)对人肾上腺皮质癌细胞系(H295R)生长和激素活性的体外抗肿瘤作用

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摘要

Several studies indicate the involvement of protein kinases in the progression of various malignancies. Kinase inhibitors are therefore becoming important anticancer drugs. CK2 kinase (casein kinase-2) has been suggested to be a constituent of a neoplastic milleu, and its inhibition might represent a new approach to cancer therapy. Adrenocortical carcinomas (ACCs) are highly malignant neoplasms with poor overall prognosis. We have examined the effects of 2-dimethylamino-4,5,6,7-tetrabromobenzimidazole (DMAT), a potent CK2 inhibitor, on the H295R human adrenocortical cancer cell line. Treatment with DMAT decreases the secretion of aldosterone, dehydroepiandrosterone sulfate, and androstendione and results in an accumulation of 17-OH-progesterone. Cell growth as measured by the MTT and 5-bromo-2′-deoxyuridine incorporation assays is inhibited, and cell cycle analysis has revealed a slight induction of apoptosis. Thus, CK2 kinase activity is probably involved in human ACC endocrine activity and growth.
机译:几项研究表明蛋白激酶参与了各种恶性肿瘤的发展。因此,激酶抑制剂成为重要的抗癌药。 CK2激酶(酪蛋白激酶2)被认为是肿瘤的组成部分,其抑制作用可能代表了一种新的癌症治疗方法。肾上腺皮质癌(ACC)是高度恶性的肿瘤,总体预后较差。我们已经检查了有效的CK2抑制剂2-二甲基氨基-4,5,6,7-四溴苯并咪唑(DMAT)对H295R人肾上腺皮质癌细胞系的影响。 DMAT处理可减少醛固酮,硫酸脱氢表雄酮和雄烯二酮的分泌,并导致17-OH-孕酮的积累。通过MTT和5-溴-2'-脱氧尿苷掺入测定法测量的细胞生长被抑制,并且细胞周期分析显示出轻微的凋亡诱导。因此,CK2激酶活性可能与人ACC内分泌活性和生长有关。

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