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Identification of potential inhibitory peptide drugs for vascular endothelial growth factor receptor 2 (VEGFR2, KDR) using bacteria display methods

机译:使用细菌显示方法鉴定血管内皮生长因子受体2(VEGFR2,KDR)的潜在抑制肽药物

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Vascular endothelial growth factor receptor 2 (VEGFR2) plays a very important role on the generation and development of newly-formed tumor vessels. Many antibodies and small molecules have been designed or discovered to target it, which can be used as powerful drugs for tumor patients. However, those molecules have very limited effect or strong malignant side effect, which limits their approval by FDA. In our project, we used bacteria display methods to screen and select highly specific peptides with high affinity which can interact with the outer membrane domain of VEGFR2, furthermore, can inhibit the binding ability between VEGF and VEGFR2. Through selection and evolution of peptides, some of those kinds' peptides have been identified and may work as potential drugs for tumor patients.
机译:血管内皮生长因子受体2(VEGFR2)对新形成的肿瘤血管的产生和发育起着非常重要的作用。设计或发现了许多抗体和小分子以靶向,可用作肿瘤患者的强大药物。然而,这些分子的效果非常有限或强烈的恶性副作用,这限制了其通过FDA的批准。在我们的项目中,我们使用细菌显示方法来筛选并选择具有高亲和力的高特异性肽,其可以与VEGFR2的外膜结构域相互作用,可以抑制VEGF和VEGFR2之间的结合能力。通过肽的选择和演化,已经鉴定了一些这些种类的肽,可以作为肿瘤患者的潜在药物。

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