Targeting Delivery of Platelets Inhibitor to Prevent Tumor Metastasis

Marzieh Geranpayehvaghei, Quanwei Shi, Baochang Zhao, Suping Li, Junchao Xu, Mohammad Taleb, Hao Qin, Yinlong Zhang, Khosro Khajeh, Guangjun Nie

Research output: Contribution to journalArticlepeer-review


Activated platelets have a high affinity for tumor cells, and consequently, they can protect tumor cells from environmental stress and immune attacks. Therefore, preventing platelet–tumor cell interaction can lead to the elimination of circulating tumor cells via natural killer cells and finally metastasis inhibition. It is also shown that CREKA (Cys-Arg-Glu-Lys-Ala), a tumor-homing pentapeptide, targets fibrin–fibronectin complexes that are found on the tumor stroma and the vessel walls. In this study, we linked CREKA to Ticagrelor, a reversible antagonist of the P2Y12 receptor on platelets. In vitro experiments indicated that CREKA-Ticagrelor could not only inhibit the platelet-induced migration of tumor cells with an invasive phenotype but also prevent tumor–platelet interaction. In vivo antitumor and antimetastasis results of this drug showed that CREKA-Ticagrelor could specifically target the tumor tissues within 24 h post intravenous injection and suppress lung metastasis. Meanwhile, by having this antiplatelet drug targeted, its side effects were minimized, and bleeding risk was decreased. Thus, CREKA-Ticagrelor offers an efficient antimetastatic agent.
Original languageEnglish
Pages (from-to)2349-2357
Number of pages9
JournalBioconjugate Chemistry
Issue number9
Early online date20 Aug 2019
Publication statusPublished - 18 Sep 2019
Externally publishedYes

Bibliographical note

PMID: 31429535


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