《生命科学》 2006, 18(3):

血小板源生长因子受体与肿瘤

张秀华^1,2，林莉萍²，丁 健1^1*

（1中国科学院上海生命科学研究院药物研究所新药研究国家重点实验室，上海 201203；2中国科学院研究生院，北京100049

摘　要：摘　要：血小板源生长因子(platelet-derived growth factor, PDGF)经由其受体(platelet-derived growth factor receptor, PDGFR)表现细胞效应。PDGF和PDGFR涉及多种肿瘤的发病机制并在血管生成中起重要作用。PDGF在肿瘤中的自分泌刺激、PDGFR的过表达或过度活化或者刺激肿瘤内血管生成都会促进肿瘤生长；PDGFR的阻断可以降低实体瘤中组织间质液压而增强药物传送。这些机制可能提示在肿瘤治疗中PDGFR抑制剂单用、与化疗药物或者和其他靶点药物联合用药的可能性和可行性。随着PDGFR拮抗剂，如imatinib的上市，PDGFR作为抗肿瘤药物的靶点备受瞩目。
关键词：血小板源生长因子；血小板源生长因子受体；肿瘤治疗；酪氨酸激酶抑制剂

Platelet-derived growth factor receptor and cancer

Zhang Xiu-Hua^1,2, Lin Li-Ping¹, Ding Jian^1*

1 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China; 2 Graduate School of CAS, Beijing 100049, China

Abstract: Abstract: Platelet-derived growth factors (PDGFs) exert their cellular effects through their receptors (PDGFRs). PDGF and PDGFR have been implicated in the pathogenesis of a number of tumor types and play important roles in angiogenesis. Tumor growth can be promoted by PDGF via autocrine stimulation of malignant cells, overexpression or overactivation of PDGFRs, or stimulation of angiogenesis within the tumor. PDGFR blockade may also lower the interstitial fluid pressure within solid tumors and enhance drug delivery. These mechanisms suggest that PDGFR antagonists play possible and feasible therapeutic roles in the treatment of cancer, alone and in combination with chemotherapy or other targeting agents. Due to the success of PDGFR antagonist imatinib developments during the last years, the interests for PDGFRs as cancer drug targets will be dramatically improved.
Key words: platelet-derived growth factor; platelet-derived growth factor receptor; cancer therapy; tyrosine kinase inhibitor