2,3-二羟喹喔啉诱导单纯疱疹病毒胸苷激酶的 ATP 酶活性。
2,3-Dihydroxy-quinoxaline induces ATPase activity of Herpes Simplex Virus thymidine kinase.
机构信息
N.D. Zelinsky Institute Of Organic Chemistry (ZIOC RAS), Leninsky prospekt, 47, 119991 Moscow, Russia.
N.D. Zelinsky Institute Of Organic Chemistry (ZIOC RAS), Leninsky prospekt, 47, 119991 Moscow, Russia.
出版信息
FEBS Lett. 2014 Jan 31;588(3):509-11. doi: 10.1016/j.febslet.2013.12.017. Epub 2013 Dec 25.
2,3-Dihydroxy-quinoxaline, a small molecule that promotes ATPase catalytic activity of Herpes Simplex Virus thymidine kinase (HSV-TK), was identified by virtual screening. This compound competitively inhibited HSV-TK catalyzed phosphorylation of acyclovir with Ki=250 μM (95% CI: 106-405 μM) and dose-dependently increased the rate of the ATP hydrolysis with KM=112 μM (95% CI: 28-195 μM). The kinetic scheme consistent with this experimental data is proposed.
2,3-二羟基喹喔啉是一种能促进单纯疱疹病毒胸苷激酶（HSV-TK）ATPase 催化活性的小分子化合物，它是通过虚拟筛选发现的。该化合物竞争性抑制 HSV-TK 催化阿昔洛韦的磷酸化，Ki 值为 250 μM（95%置信区间：106-405 μM），并呈剂量依赖性增加 ATP 水解的速度，KM 值为 112 μM（95%置信区间：28-195 μM）。提出了与实验数据一致的动力学方案。
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