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NOVEL TUMOR-TARGETED PEPTIDE-CAMPTOTHECIN CONJUGATES; SYNTHESIS AND BIOLOGICAL EVALUATION

机译:新型肿瘤靶向肽 - 喜树蛋白缀合物;合成与生物学评价

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摘要

Small peptides have been used in literature, for targeting antitumoral drugs to specific membrane receptors over-expressed by tumor cells, such as somatostatin, bombesin, RGD peptide analogues and peptidomimetics. RGD peptides, that selectively recognize α_vβ3 and α_vβ5 integrin receptors, appear attractive candidates. Due to the role of integrins in the angiogenesis and tumor growing , tumor-targeted RGD peptide-cytotoxic drug conjugates are likely to exhibit a dual antitumor and antiangiogenic effect.
机译:在文献中使用的小肽,用于靶向抗肿瘤药物,以肿瘤细胞(如生长抑制菌素,Bombesin,RGD肽类似物和拟肽剂)过度表达的特异性膜受体。选择性地识别α_Vβ3和α_Vβ5整联蛋白受体的RGD肽似乎有吸引力。由于整联蛋白在血管生成和肿瘤生长中的作用,肿瘤靶向的RGD肽 - 细胞毒性药物缀合物可能表现出双抗肿瘤和抗血管生成效果。

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