Dixit Manish, Tripathi Brajendra K, Tamrakar Akhilesh K, Srivastava Arvind K, Kumar Brijesh, Goel Atul
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.
Bioorg Med Chem. 2007 Jan 15;15(2):727-34. doi: 10.1016/j.bmc.2006.10.053. Epub 2006 Oct 27.
Protein tyrosine phosphatase 1B (PTP-1B) is an enzyme that plays a critical role in down-regulating insulin signaling through dephosphorylation of the insulin receptor. Studies have shown that PTP-1B knockout mice showed increased insulin sensitivity in muscle and liver as well as resistance to obesity. A series of hydroxy benzofuran methyl ketones and their naturally mimicking dimers and linear and angular furanochalcones and flavones have been evaluated as PTP-1B inhibitors. Screened compounds displayed good inhibitory activity.
蛋白酪氨酸磷酸酶1B（PTP - 1B）是一种通过使胰岛素受体去磷酸化来下调胰岛素信号传导的关键酶。研究表明，PTP - 1B基因敲除小鼠在肌肉和肝脏中表现出更高的胰岛素敏感性以及对肥胖的抵抗力。一系列羟基苯并呋喃甲基酮及其天然模拟二聚体、线性和角型呋喃查耳酮和黄酮已被评估为PTP - 1B抑制剂。筛选出的化合物显示出良好的抑制活性。
