The discovery of potent and stable short peptide FGFR1 antagonist for cancer therapy.

Fibroblast growth factor receptor 1 (FGFR1) is one of the attractive pharmaceutical targets for cancer therapy. The FGFR1 targeting antagonist peptides, especially of the short peptides harbouring only coding amino acid might highlights promising aspects for their higher affinity, specificity and lower adverse reactions. However, most of peptides inhibitors remain in preclinical research, likely associating with their instability and short half-life. In this study, we found a stable short peptide inhibitor P48 and speculated that its stability might be related to its non-linear spatial structure. In addition, P48 could target the extracellular immunoglobulin domain of FGFR1, and effectively block the particular signaling pathways of FGFR1, which lead to the inhibition of cancer proliferation, invasion in vitro and restraint of tumor growth in vivo. Together, this study provided a promising FGFR1 inhibitor with the potential to be developed as an antitumor drug. Copyright © 2019 Elsevier B.V. All rights reserved.

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Jianzhang Wu, Lingzi Chen, Liping Chen, Lei Fan, Zhe Wang, Zhaojun Dong, Qian Chen, Tao Wei, Yuepiao Cai, Wulan Li. The discovery of potent and stable short peptide FGFR1 antagonist for cancer therapy. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2020 Feb 15;143:105179

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PMID: 31841696

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