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Platelet-derived growth factors (PDGFs) and PDGF receptors (PDGFRs) are expressed in a variety of tumors. Activation of the PDGF/PDGFR signaling pathway is associated with cancer proliferation, metastasis, invasion, and angiogenesis through modulating multiple downstream pathways, including phosphatidylinositol 3 kinase/protein kinase B pathway and mitogen-activated protein kinase/extracellular signal-regulated kinase pathway. Therefore, targeting PDGF/PDGFR signaling pathway has been demonstrated to be an effective strategy for cancer therapy, and accordingly, some great progress has been made in this field in the past few decades. This review will focus on the PDGF isoforms and their binding with the related PDGFRs, the PDGF/PDGFR signaling and regulation, and especially present strategies and inhibitors developed for cancer therapy, and the related clinical benefits and side effects. Copyright © 2022. Published by Elsevier B.V.


Xiang Zou, Xi-Yu Tang, Zhong-Yuan Qu, Zhi-Wei Sun, Chen-Feng Ji, Yan-Jie Li, Shou-Dong Guo. Targeting the PDGF/PDGFR signaling pathway for cancer therapy: A review. International journal of biological macromolecules. 2022 Mar 31;202:539-557

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PMID: 35074329

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