摘要
纹状体富集蛋白酪氨酸磷酸酶 (STEP) 仅在中枢神经系统中表达,并通过不同底物的去磷酸化调节各种神经元信号因子。 STEP 的表达失调或无法控制的酶活性会导致神经系统疾病,例如阿尔茨海默病,这使其成为有希望的药物靶点。 在此,我们回顾了 STEP 的结构和生物学功能,以及小分子 STEP 调节剂的最新发展。 我们希望这篇综述能为进一步开发更有效和选择性的 STEP 抑制剂治疗神经系统疾病提供参考。
关键词: 纹状体富集蛋白酪氨酸磷酸酶,神经系统疾病,抑制剂,激活剂,构效关系,PTP 结构域。
Current Medicinal Chemistry
Title:Structure, Function and Modulation of Striatal-enriched Protein Tyrosine Phosphatase (STEP)
Volume: 28 Issue: 37
关键词: 纹状体富集蛋白酪氨酸磷酸酶,神经系统疾病,抑制剂,激活剂,构效关系,PTP 结构域。
摘要: Striatal-enriched protein tyrosine phosphatase (STEP) is exclusively expressed in the central nervous system and regulates various neuronal signaling factors through the dephosphorylation of different substrates. Dysregulated expression or uncontrollable enzymatic activity of STEP contributes to neurological disorders such as Alzheimer's disease, which makes it a promising pharmaceutical target. Herein, we have reviewed the structure and biological functions of STEP, as well as the recent development of smallmolecule STEP modulators. We hope this review will provide a reference for the further development of more potent and selective STEP inhibitors for the treatment of nervous system diseases.
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Cite this article as:
Structure, Function and Modulation of Striatal-enriched Protein Tyrosine Phosphatase (STEP), Current Medicinal Chemistry 2021; 28 (37) . https://dx.doi.org/10.2174/0929867328666210412123304
DOI https://dx.doi.org/10.2174/0929867328666210412123304 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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