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首页> 外文期刊>Anticancer Research: International Journal of Cancer Research and Treatment >Antiangiogenesis and anticancer efficacy of TA138, a novel alphavbeta3 antagonist.
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Antiangiogenesis and anticancer efficacy of TA138, a novel alphavbeta3 antagonist.

机译：新型alphavbeta3拮抗剂TA138的抗血管生成和抗癌功效。

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摘要

BACKGROUND: Angiogenesis is a complex process involving endothelial cell migration, proliferation, invasion, and tube formation. Inhibition of these processes might have implications in various angiogenesis-mediated disorders. MATERIALS AND METHODS: The antiangiogenic efficacy of the novel alphavbeta3 antagonist TA138 was examined using in vivo and in vitro model systems. RESULTS: The in vitro studies demonstrated the ability of TA138 and RP747 (conjugated TA138) to inhibit endothelial cell migration toward vitronectin, with an IC50=0.04 and 0.045 microM, respectively. Furthermore, utilizing the chick chorioallantoic membrane models, TA138 inhibited basic fibroblast growth factor-induced neovascularization. CONCLUSION: TA138 might be a useful tool for the inhibition of angiogenesis associated with human tumor growth, or other pathological neovascularization processes. RP747 demonstrated antitumor efficacy in 1 spontaneous tumor model (c-neu oncomouse model, alphavbeta3 positive cells) and in 1 xenograft model (HCT116 human tumor colon carcinoma, alphavbeta3 negative cells) injected subcutaneously into nude mice.
机译：背景：血管生成是一个复杂的过程，涉及内皮细胞迁移，增殖，侵袭和管形成。这些过程的抑制可能对各种血管新生介导的疾病有影响。材料与方法：使用体内和体外模型系统检查了新型alphavbeta3拮抗剂TA138的抗血管生成功效。结果：体外研究表明TA138和RP747（结合TA138）抑制内皮细胞向玻连蛋白迁移的能力，IC50分别为0.04和0.045 microM。此外，利用鸡绒膜尿囊膜模型，TA138抑制了碱性成纤维细胞生长因子诱导的新血管形成。结论：TA138可能是抑制与人类肿瘤生长或其他病理性新血管形成过程相关的血管生成的有用工具。 RP747在1种自发肿瘤模型（c-neu oncomouse模型，alphavbeta3阳性细胞）和1种异种移植模型（HCT116人肿瘤结肠癌，alphavbeta3阴性细胞）中显示了抗肿瘤功效。

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