Qin Xin, Wan Yi, Li Meng, Xue Xiaochang, Wu Shouzhen, Zhang Cun, You Yanjie, Wang Weihua, Jiang Changli, Liu Yan, Zhu Wenhua, Ran Yonggang, Zhang Zhen, Han Wei, Zhang Yingqi
Biotechnology Center of The Fourth Military Medical University, and State Key Laboratory of Cancer Biology, 17 Chang'le West Road, 710032 Xi'an, People's Republic of China.
J Biochem. 2007 Jul;142(1):79-85. doi: 10.1093/jb/mvm109. Epub 2007 May 21.
Human vascular endothelia growth factor receptor 3 (VEGFR-3) is up-regulated in a variety of human cancers. It is a potentially rational target for drug delivery. To identify novel ligands with specific binding capabilities to VEGFR-3, we screened a phage display peptide library and found a consensus motif of the peptides which is displayed by the positive phages CSDxxHxWC (x is any amino acid). The phage displaying peptide CSDSWHYWC (designated as P1) exhibited the highest affinity to VEGFR-3 in phage ELISA and the chemically synthesized P1 could bind to VEGFR-3 specifically in a dose-dependent manner. In addition, the flow cytometry assay and immunofluorescence showed that the FITC labelled P1 could bind to VEGFR-3 positive carcinoma cells with specificity. Our study suggests that P1 may be a homing peptide for treatment of tumours.
人血管内皮生长因子受体3（VEGFR - 3）在多种人类癌症中上调。它是药物递送的一个潜在合理靶点。为了鉴定对VEGFR - 3具有特异性结合能力的新型配体，我们筛选了一个噬菌体展示肽库，并发现了由阳性噬菌体CSDxxHxWC（x为任意氨基酸）展示的肽的共有基序。展示肽CSDSWHYWC（命名为P1）在噬菌体酶联免疫吸附测定中对VEGFR - 3表现出最高亲和力，并且化学合成的P1能够以剂量依赖方式特异性结合VEGFR - 3。此外，流式细胞术检测和免疫荧光显示，异硫氰酸荧光素标记的P1能够特异性结合VEGFR - 3阳性癌细胞。我们的研究表明，P1可能是一种用于肿瘤治疗的归巢肽。
