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Platelet-derived Growth Factor (PDGF) Inhibitor

Platelet-Derived Growth Factor Receptor (PDGFR) Kinase Inhibitors

In recent years, several RTK inhibitors with in vivo activity have been developed. Most of these inhibitors have focused on targeting the signaling pathways of VEGF, but diverse chemical compounds were also developed as selective PDGFR kinase inhibitors. Many of these PDGFR kinase inhibitors, including several quinoxalines were found to be highly potent and selective toward the PDGFR and its family members, kit and Flt3.

Inhibition of Platelet-derived Growth Factor Receptor Signaling

Inhibition of the PDGF signal pathway results in loss of pericytes and a reduction in vessel density in the neovascularized cornea that correlates with reduced expression of PDGF, ang1/2, and VEGF mRNA. PI3-K is known to be involved in the regulation of VEGF, ang1, and PDGF, as the PI3-K inhibitors wortmannin or LY294002 has similar effects. Since PDGF is a known stimulus for PI3-K activation, decrease in VEGF, ang1/2, and PDGF mRNA levels on administration of the PDGF inhibitor is caused by the decreased activation of the PI3-K signaling cascade.

Platelet-derived Growth Factor (PDGF) Inhibitor Related Studies

    1. Ball SG, et al. (2012) Inhibition of platelet-derived growth factor receptor signaling regulates Oct4 and Nanog expression, cell shape, and mesenchymal stem cell potency. Stem Cells. 30(3):548-60.
    2. Abdollahi A, et al. (2005) Inhibition of platelet-derived growth factor signaling attenuates pulmonary fibrosis. J Exp Med. 201(6):925-35.
    3. Johannes Waltenberger, et al. (1999) A Dual Inhibitor of Platelet-Derived Growth Factor β-Receptor and Src Kinase Activity Potently Interferes With Motogenic and Mitogenic Responses to PDGF in Vascular Smooth Muscle Cells. Circulation Research. 85: 12-22.
    4. Shulman T, et al. (1997) An antibody reactive with domain 4 of the platelet-derived growth factor beta receptor allows BB binding while inhibiting proliferation by impairing receptor dimerization. J Biol Chem. 272(28): 17400-4.
    5. McClintock J, et al. (1992) Detection of c-sis proto-oncogene transcripts by direct enzyme-labeled cDNA probes and in situ hybridization. In Vitro Cell Dev Biol. 28A (2): 102-8.