The PDGF/PDGFR pathway as a drug target.

Mol Aspects Med

Department of Pharmaceutical Biosciences, Uppsala University, Biomedical Center, Box 591, SE-751 24 Uppsala, Sweden. Electronic address:

Published: August 2018

AI Article Synopsis

  • PDGF plays a crucial role in promoting the growth, survival, and movement of mesenchymal cells, with its signaling dysfunction linked to various diseases like cancer and fibrosis.
  • Current therapies target PDGF signaling through methods like DNA aptamers, blocking antibodies, and small molecules to inhibit receptor activity.
  • The review discusses different strategies to modify PDGF signaling, evaluates existing drugs, and highlights both successful treatments and ongoing challenges in this area.

Article Abstract

Platelet-derived growth factors (PDGF) promotes cell proliferation, survival and migration, primarily of cells of mesenchymal origin. Dysfunction of PDGF signaling has been observed in a wide array of pathological conditions, such as cancer, fibrosis, neurological conditions and atherosclerosis. Reported abnormalities of the PDGF pathway include overexpression or amplification of PDGF receptors (PDGFRs), gain of function point mutations or activating chromosomal translocations. Current development of therapeutic drugs often aims at producing compounds that specifically target interaction between PDGFs and their receptors by specific DNA aptamers and ligand traps, or downregulate PDGFRs with blocking antibodies, or inhibit tyrosine kinase activity of PDGFRs with small molecules. In this review, we discuss some of the approaches taken to interfere with PDGF signaling, review a panel of existing therapeutic drugs, and consider clinically successful cases and remaining challenges.

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Source
http://dx.doi.org/10.1016/j.mam.2017.11.007DOI Listing

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