Angiogenesis has become an attractive target for drug therapy because of its key role in tumor growth. An extensive array of compounds is currently in preclinical development, with many now entering the clinic and/or achieving approval from the US Food and Drug Administration. Several regulatory and signaling molecules governing angiogenesis are of interest, including growth factors (eg, vascular endothelial growth factor, platelet‐derived growth factor, fibroblast growth factor, and epidermal growth factor), receptor tyrosine kinases, and transcription factors such as hypoxia inducible factor, as well as molecules involved in mitogen‐activated protein kinase (MAPK) and phosphoinositide 3‐kinase (PI3K) signaling. Pharmacologic agents have been identified that target these pathways, yet for some agents (notably thalidomide), an understanding of the specific mechanisms of antitumor action has proved elusive. The following review describes key molecular mechanisms and novel therapies that are on the horizon for antiangiogenic tumor therapy. CA Cancer J Clin 2010. © 2010 American Cancer Society, Inc.

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血管生成抑制剂：当前策略和未来前景

由于其在肿瘤生长中的关键作用，血管生成已成为药物治疗的一个有吸引力的目标。大量化合物目前正处于临床前开发阶段，其中许多已进入临床和/或获得美国食品和药物管理局的批准。几个控制血管生成的调节和信号分子是令人感兴趣的，包括生长因子（例如，血管内皮生长因子、血小板衍生生长因子、成纤维细胞生长因子和表皮生长因子）、受体酪氨酸激酶和转录因子，如缺氧诱导因子以及参与丝裂原活化蛋白激酶 (MAPK) 和磷酸肌醇 3-激酶 (PI3K) 信号传导的分子。已经确定了靶向这些途径的药物制剂，但对于某些药物（特别是沙利度胺），对抗肿瘤作用的具体机制的理解被证明是难以捉摸的。以下综述描述了即将出现的抗血管生成肿瘤治疗的关键分子机制和新疗法。CA Cancer J Clin 2010。© 2010 美国癌症协会，Inc。