Goodman Research Cancer Centre, McGill University, 1160 Pine Avenue, Room 601 Montreal, QC, Canada H3A 1A3.
Anticancer Agents Med Chem. 2012 Jan;12(1):4-18. doi: 10.2174/187152012798764741.
Protein tyrosine phosphatases (PTPs) constitute a large family of enzymes that can exert both positive and negative effects on signaling pathways. They play dominant roles in setting the levels of intracellular phosphorylation downstream of many receptors including receptor tyrosine kinases and G protein-coupled receptors. As observed with kinases, deregulation of PTP activity can also contribute to cancer. This review will examine a broad array of PTP family members that positively affect oncogenesis in human cancer tissues. We will describe the PTP family, their biological significance in oncology, and how recent progress is being made to more effectively target specific PTPs. Finally, we will discuss the therapeutic implications of targeting these oncogenic PTPs in cancer.
蛋白酪氨酸磷酸酶（PTPs）构成了一个庞大的酶家族，它们可以对信号通路产生正反两方面的影响。它们在许多受体（包括受体酪氨酸激酶和 G 蛋白偶联受体）下游的细胞内磷酸化水平的设定中发挥着主导作用。与激酶一样，PTP 活性的失调也可能导致癌症。这篇综述将研究广泛的 PTP 家族成员，这些成员在人类癌症组织中促进肿瘤发生。我们将描述 PTP 家族，它们在肿瘤学中的生物学意义，以及最近在更有效地靶向特定 PTP 方面取得的进展。最后，我们将讨论靶向这些致癌 PTP 在癌症中的治疗意义。
