蛋白酶激活受体在肿瘤血管生成中的作用及其靶向抗肿瘤药物研究进展

doi:10.3969/j.issn.2095-1264.2021.05.01

首页 > 过刊浏览>2021年第5期 >519-523. DOI:10.3969/j.issn.2095-1264.2021.05.01

蛋白酶激活受体在肿瘤血管生成中的作用及其靶向抗肿瘤药物研究进展
DOI:
                        10.3969/j.issn.2095-1264.2021.05.01
                    
作者:
                        
                        
                    
作者单位:1.南开大学药学院，天津，300350;2.南开大学附属第一中心医院 胸外科，天津，300192
作者简介:王明，女，硕士研究生，研究方向：靶向PARs的抗肿瘤血管生成药物。
通讯作者:杨诚，男，教授，研究方向：结构辅助药物设计及新药开发
中图分类号:R979.1
基金项目:★国家自然科学基金（81871972）。

Research progress on the role of protease-activated receptors in tumor angiogenesis and its targeted antineoplastic drugs^★

Author:

Affiliation:

1.College of Pharmacy, Nankai University, Tianjin, 300350, China;2.Department of Thoracic Surgery, the First Central Hospital Affiliated to Nankai University, Tianjin, 300192, China

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摘要:

肿瘤血管生成是肿瘤生长过程中一个重要的步骤，可以为肿瘤细胞提供氧气和营养物质，也与肿瘤细胞转移有关。目前，抗血管生成被认为是肿瘤治疗的一个重要靶点。蛋白酶激活受体（PAR）是G蛋白偶联受体家族成员之一，已被证明可以作为癌基因，在多种肿瘤细胞中高表达。研究发现，PARs可被凝血酶激活，诱导血管内皮生长因子（VEGF）表达，参与肿瘤血管生成，可作为抗肿瘤血管生成的靶点。本文主要介绍了PARs的活化机制及其在肿瘤血管生成中的作用，并对近年来靶向PARs抑制肿瘤血管生成的抗肿瘤药物的结构、药理活性的研究进展进行总结。

Abstract:

Tumor angiogenesis is an important step in the process of tumor growth, for it can provide oxygen and nutrients for tumor cells, and is also related to the metastatic ability of tumor cells. At present, anti-angiogenesis is regarded as an important target for cancer therapy. Protease-activated receptor (PAR) is a member of G-protein coupled receptor family. It has been proved to be an oncogene and highly expressed in a variety of tumor cells. Studies have found that PARs can induce the expression of vascular endothelial growth factor (VEGF) through thrombin activation, which is involved in the process of tumor angiogenesis. Therefore, PARs can be used as a drug target for anti-tumor angiogenesis. This paper mainly introduces the activation mechanism of PARs and its role in tumor angiogenesis, and summarizes the research progress in the structure and pharmacological activity of anti-tumor drugs targeting PARs to inhibit tumor angiogenesis in recent years.