针对蛋白酪氨酸磷酸酶的抗癌药物发现。
Targeting protein tyrosine phosphatases for anticancer drug discovery.
机构信息
Departments of Molecular Oncology and Drug Discovery, H. Lee Moffitt Cancer Center and Research Institute, University of South Florida College of Medicine, Tampa, FL 33612, USA.
出版信息
Curr Pharm Des. 2010 Jun;16(16):1843-62. doi: 10.2174/138161210791209027.
Abstract
Protein tyrosine phosphatases (PTPs) are a diverse family of enzymes encoded by 107 genes in the human genome. Together with protein tyrosine kinases (PTKs), PTPs regulate various cellular activities essential for the initiation and maintenance of malignant phenotypes. While PTK inhibitors are now used routinely for cancer treatment, the PTP inhibitor development field is still in the discovery phase. In this article, the suitability of targeting PTPs for novel anticancer drug discovery is discussed. Examples are presented for PTPs that have been targeted for anticancer drug discovery as well as potential new PTP targets for novel anticancer drug discovery.
摘要
蛋白酪氨酸磷酸酶（PTPs）是一个由人类基因组中的 107 个基因编码的具有多样性的酶家族。PTPs 与蛋白酪氨酸激酶（PTKs）一起调节各种细胞活动，这些活动对于起始和维持恶性表型至关重要。虽然现在已经常规使用 PTK 抑制剂来治疗癌症，但 PTP 抑制剂的开发领域仍处于发现阶段。本文讨论了将 PTP 作为新型抗癌药物发现的靶标的适宜性。本文还介绍了一些已被作为抗癌药物发现的靶标的 PTP 以及一些新的潜在的用于新型抗癌药物发现的 PTP 靶标。
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