甲酰基色酮衍生物作为人蛋白酪氨酸磷酸酶1B的不可逆和选择性抑制剂。动力学和建模研究。
Formylchromone derivatives as irreversible and selective inhibitors of human protein tyrosine phosphatase 1B. Kinetic and modeling studies.
作者信息
Shim Yi Sup, Kim Ki Chul, Lee Kyung A, Shrestha Suja, Lee Keun-Hyeung, Kim Chan Kyung, Cho Hyeongjin
机构信息
Department of Chemistry and Institute of Molecular Cell Biology, Inha University, Yonghyun-dong, Nam-ku, Incheon 402-751, Republic of Korea.
出版信息
Bioorg Med Chem. 2005 Feb 15;13(4):1325-32. doi: 10.1016/j.bmc.2004.11.006.
A series of formylchromone derivatives were synthesized as PTP1B inhibitors and some of them were potent against PTP1B with IC50 values as low as 1.0 microM. They exhibited remarkable selectivity for PTP1B over other human PTPases. Kinetic studies revealed that formylchromone derivatives are irreversible and active site-directed inhibitors. Molecular modeling study identified the orientation of the inhibitor bound at the active site of PTP1B.
合成了一系列苯甲酰色酮衍生物作为蛋白酪氨酸磷酸酶1B（PTP1B）抑制剂，其中一些对PTP1B具有强效抑制作用，IC50值低至1.0微摩尔。它们对PTP1B的选择性显著高于其他人类蛋白酪氨酸磷酸酶。动力学研究表明，苯甲酰色酮衍生物是不可逆的活性位点导向抑制剂。分子模拟研究确定了抑制剂在PTP1B活性位点的结合方向。
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