Recent advances in antiangiogenic agents with VEGFR as target.
Recent advances in antiangiogenic agents with VEGFR as target.
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DOI：
10.2174/138955711797068355
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发表时间：
2011-09
期刊：
影响因子：
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通讯作者：
J. Zhang;Y. Shan;X. Pan;L. He
中科院分区：
文献类型：
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作者：
J. Zhang;Y. Shan;X. Pan;L. He
血管生成是侵袭性肿瘤生长和转移所必需的，并且构成控制癌症进展的重要点。它的抑制可能是一种有价值的癌症治疗方法。抗血管生成剂被设计为攻击肿瘤血管系统并切断肿瘤的营养供应。血管生成的全身性阻断最近已被批准用于治疗几种类型的人类癌症。与常规治疗相比，抗血管生成治疗具有多种优势。血管内皮生长因子（VEGF）是血管生成的重要调节因子，也是抗肿瘤治疗的重要靶点。VEGF与其受体（VEGFR）的结合通过酪氨酸激酶（TK）途径导致细胞增殖和新血管形成。VEGF/VEGFR通路成为抗肿瘤药物设计的重要靶点。据信它在控制血管生成方面很重要。据报道，基于VEGFR抑制的抗血管生成治疗是有效的临床策略。在这篇综述中，作者描述了过去几年中关于VEGFR抑制剂的现有文献。我们试图涵盖药物化学的化学结构，药理学概况和结构-活性关系方面的所有重要出版物。
Angiogenesis is required for invasive tumor growth and metastasis and constitutes an important point in the control of cancer progression. Its inhibition may be a valuable approach to cancer therapy. Antiangiogenic agents are designed to attack the tumor vasculature and cut off the tumor's supply of nutrients. Systemic blockade of angiogenesis has been recently approved for the treatment of several types of human cancers. Antiangiogenic therapy presents various advantages as compared to conventional treatment. Vascular endothelial growth factor (VEGF) is considered to be one of the most important regulators of angiogenesis and a key target in anticancer treatment. VEGF binding to its receptor (VEGFR) leads to cell proliferation and new vascular formation by tyrosine kinase (TK) pathway. VEGF/VEGFR pathway is becoming attractive target for anticancer drug design. It is believed to be important in the control of angiogenesis. Antiangiogenic therapy based on inhibition of VEGFR was reported to be powerful clinical strategies. In this review, the authors describe the existing literature regarding VEGFR inhibitors in the last few years. We attempt to cover all essential publications on the medicinal chemistry in terms of chemical structure, pharmacological profile and structure-activity relationships.