A novel FGFR1-binding peptide exhibits anti-tumor effect on lung cancer by inhibiting proliferation and angiogenesis.
A novel FGFR1-binding peptide exhibits anti-tumor effect on lung cancer by inhibiting proliferation and angiogenesis.
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一种新型 FGFR1 结合肽通过抑制增殖和血管生成对肺癌发挥抗肿瘤作用
DOI：
10.7150/ijbs.24739
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发表时间：
2018
影响因子：
9.2
通讯作者：
Chen L
中科院分区：
文献类型：
--
作者：
Tan Q;Wang Z;Wang Q;Wang Y;Huang Z;Su N;Jin M;Kuang L;Qi H;Ni Z;Li C;Zhu Y;Jiang W;Chen H;Deng C;Du X;Xie Y;Chen L
据报道，成纤维细胞生长因子受体1（FGFR 1）的过度活化是大多数非小细胞肺癌（NSCLC）样本中发现的重要特征。本研究鉴定了FGFR 1抑制肽R1-P2，并研究了其对肺癌细胞生长和血管生成的影响。我们的结果表明，R1-P2结合到人FGFR 1蛋白，并有效地阻断了A549和NCI-H460细胞中FGF 2与FGFR 1的结合。此外，该肽在两种细胞系中显著降低增殖、迁移和侵袭，但促进凋亡。此外，R1-P2能有效抑制A549裸鼠移植瘤的生长和血管生成，R1-P2还能显著抑制血管形成实验和CAM模型中FGF 2诱导的血管生成。我们进一步证明R1-P2通过抗血管生成和抗增殖活性抑制肺肿瘤生长。我们的数据可能提供一种新的先导分子，在治疗FGFR 1活化相关的肺癌中具有潜在的应用。
It has been reported that overactivation of fibroblast growth factor receptor 1 (FGFR1) is an important characteristic found in most non-small cell lung cancer (NSCLC) samples. Here, we identified a FGFR1 inhibitory peptide R1-P2 and investigated its effects on the lung cancer cells growth and angiogenesis in vitro and in vivo. Our results demonstrate that R1-P2 bound to human FGFR1 protein, and efficiently blocked the binding of FGF2 to FGFR1 in A549 and NCI-H460 cells. Moreover, this peptide significantly decreased the proliferation, migration and invasion, but promoted the apoptosis in both cell lines. In addition, R1-P2 treatment effectively inhibited the tumor growth and neovascularization in nude mice with xenografted A549 cells, and R1-P2 also significantly inhibited the FGF2-induced angiogenesis in tube formation experiment and CAM model. We further demonstrated that R1-P2 suppressed lung tumor growth through anti-angiogenic and anti-proliferative activity. Our data may provide a novle leading molecule with potential application in the treatment of FGFR1 activation related lung cancers.
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影响因子：
5.6
作者：
Yang GW;Jiang JS;Lu WQ
通讯作者：
Lu WQ
DOI：
10.1152/ajpendo.00089.2006
发表时间：
2007-03-01
影响因子：
5.1
作者：
Sun, Haijun D.;Malabunga, Maria;Kussie, Paul
通讯作者：
Kussie, Paul
影响因子：
5.3
作者：
Preusser, Matthias;Berghoff, Anna S.;Birner, Peter
通讯作者：
Birner, Peter
影响因子：
7.3
作者：
Safieh-Garabedian, B;Dardenne, M;Saadé, NE
通讯作者：
Saadé, NE
影响因子：
2.8
作者：
Liang, Yang-Hung;Chang, Chia-Chen;Lin, Chii-Wann
通讯作者：
Lin, Chii-Wann