Recent Advances in PTP1B Inhibitor Development for the Treatment of Type 2 Diabetes and Obesity
Recent Advances in PTP1B Inhibitor Development for the Treatment of Type 2 Diabetes and Obesity
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DOI：
10.1039/9781849735322-00142
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发表时间：
2013-01-01
期刊：
影响因子：
--
通讯作者：
Zhang, Zhong-Yin
中科院分区：
文献类型：
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作者：
He, Rongjun;Zeng, Li-Fan;Zhang, Zhong-Yin
蛋白质残基的可逆磷酸化是细胞传递和传导细胞信号（例如生长、分化、迁移和凋亡）的关键策略。异常的磷酸化要么启动不适当的信号通路，要么阻断功能信号通路，从而导致各种人类疾病的发病机制，包括癌症、糖尿病/肥胖、炎症和传染病。 1 磷酸化和去磷酸化反应分别由蛋白激酶和蛋白磷酸酶催化。激酶作为蛋白质磷酸化的促进剂，是人类癌症治疗最成功的治疗靶点之一，2001年至2008年美国FDA批准了八种小分子激酶抑制剂药物，目前有大量化合物正在进行临床试验。 2 由于与激酶在控制蛋白质磷酸化水平方面的作用相反，
Reversible phosphorylation of protein residues is a key strategy for cells to convey and conduct cellular signals, such as growth, differentiation, migration, and apoptosis. Aberrant phosphorylations either initiate inappropriate or block functional signal pathways, which results in the pathogenesis of various human diseases, including cancer, diabetes/obesity, inflammation, and infectious diseases. 1 The reactions of phosphorylation and dephosphorylation are catalyzed by protein kinases and protein phosphatases respectively. Kinases as promoters of protein phosphorylation are among the most successful therapeutic targets for human cancer therapy with eight small molecule kinase inhibitor drugs approved by the US FDA from 2001 to 2008 and a large number of compounds are presently in clinical trials. 2 Due to the opposite role to kinases in controlling the level of protein phosphorylation,