Ferrara Napoleone, Hillan Kenneth J, Novotny William
Department of Molecular Oncology, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
Biochem Biophys Res Commun. 2005 Jul 29;333(2):328-35. doi: 10.1016/j.bbrc.2005.05.132.
Vascular endothelial growth factor (VEGF) is an endothelial cell-specific mitogen in vitro and an angiogenic inducer in vivo. The tyrosine kinases Flt-1 (VEGFR-1) and Flk-1/KDR (VEGFR-2) are high affinity VEGF receptors. VEGF plays an essential role in developmental angiogenesis and is important also for reproductive and bone angiogenesis. Substantial evidence also implicates VEGF as a mediator of pathological angiogenesis. Anti-VEGF monoclonal antibodies and other VEGF inhibitors block the growth of several tumor cell lines in nude mice. Clinical trials with VEGF inhibitors in a variety of malignancies are ongoing. Recently, a humanized anti-VEGF monoclonal antibody (bevacizumab; Avastin) has been approved by the FDA as a first-line treatment for metastatic colorectal cancer in combination with chemotherapy. Furthermore, VEGF is implicated in intraocular neovascularization associated with diabetic retinopathy and age-related macular degeneration.
血管内皮生长因子（VEGF）在体外是一种内皮细胞特异性促有丝分裂原，在体内是一种血管生成诱导剂。酪氨酸激酶Flt-1（VEGFR-1）和Flk-1/KDR（VEGFR-2）是高亲和力VEGF受体。VEGF在发育性血管生成中起重要作用，对生殖和骨血管生成也很重要。大量证据还表明VEGF是病理性血管生成的介质。抗VEGF单克隆抗体和其他VEGF抑制剂可阻断裸鼠体内多种肿瘤细胞系的生长。针对多种恶性肿瘤的VEGF抑制剂的临床试验正在进行。最近，一种人源化抗VEGF单克隆抗体（贝伐单抗；阿瓦斯汀）已被美国食品药品监督管理局批准作为转移性结直肠癌联合化疗的一线治疗药物。此外，VEGF与糖尿病视网膜病变和年龄相关性黄斑变性相关的眼内新生血管形成有关。
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