Abstract

The platelet-derived growth factor receptors (PDGFRs), including the PDGFRα and PDGFRβ, are typical class III receptor tyrosine kinases. They regulate important physiopathylogical processes, including angiogenesis, wound healing, and tumor cell proliferation, migration and survival. Overexpression of platelet-derived growth factors (PDGFs) and their receptors or activating mutations of PDGF receptors had been linked to a series of diseases, such as tumorigenesis, fibrosis and cardiovascular diseases. Therefore, PDGFs/PDGFRs had been validated as important therapeutic targets in the treatment of these diseases. Herein, we reviewed the progress in the structural and functional studies of PDGFR signaling, their regulation, and their association with human diseases. In addition, we discussed the therapeutic strategies undertaken on targeting dysregulated PDGF/PDGFR signaling. Moreover, we provided our perspectives on future research directions.

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