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血管生成是肿瘤发展、转移所必需的 ,抗血管生成是目前基于生物靶点的抗肿瘤研究热点之一。血管内皮细胞生长因子 (VEGF)在肿瘤血管生成中处于核心地位 ,因此阻断VEGF的作用可以达到抗血管生成的目的。VEGF及其受体的结构特征和生物学特性 ,以及结合后产生的作用机制目前已经比较清楚 ,已有多种作用于不同环节的阻断手段在临床试验 ,但均有缺陷。计算机辅助药物设计可以根据生物靶分子的晶体结构设计出结合力高、专属性强的小分子抑制剂已有成功应用。因此 ,选择不同的部位设计作用更强更优的小分子抑制剂是新药创制的重要方向。
Angiogenesis is necessary for the development and metastasis of tumors. Antiangiogenesis is one of the hot topics in anti-tumor research based on biological targets. Vascular endothelial cell growth factor (VEGF) is at the core of tumor angiogenesis, so blocking VEGF can achieve the purpose of anti-angiogenesis. The structural and biological characteristics of VEGF and its receptors, as well as the mechanism of action resulting from the binding, have now become clearer. There are many different clinical and experimental approaches to block VEGF, but these have drawbacks. Computer-aided drug design can be designed according to the crystal structure of biological target molecules with high binding strength and specificity of small molecule inhibitors have been successfully applied. Therefore, the selection of different parts of the design role of stronger and better small molecule inhibitors is an important direction for the creation of new drugs.