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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

The Development of PDGF Receptor Inhibitors for the Treatment of Glioma: A Review

Author(s): Michael A. Badruddoja, Emad Elquza, James Welsh, Laurence Cooke, Abhay Sanan, Baldassrre Stea and Daruka Mahadavan

Volume 7, Issue 4, 2010

Page: [290 - 299] Pages: 10

DOI: 10.2174/157018010790945887

Price: $65


The platelet-derived growth factor (PDGF-A, PDGF-B, PDGF-C, PDGF-D) family is composed of homo- and hetero-dimers that are potent mitogens for a wide variety of cell types. They exert their biological effects by binding to two receptor tyrosine kinases (α- and β-PDGFR). PDGF-AA, -AB, -BB and -CC dimers bind to the α-PDGFR with high affinity, whereas PDGF-BB and -DD dimers bind to β-PDGFR. Aberrant PDGF signaling leads to increased interstitial fluid pressure, stromal cell recruitment and neo-angiogenesis in glioblastoma multiforme (GBM) due to deregulated autocrine/paracrine signaling. Therefore, targeting the PDGFR tyrosine kinase domain with small molecule tyrosine kinase inhibitors (TKIs) alone or in combination with chemotherapy may provide therapeutic benefit in GBM. Here we review PDGFR antagonists in clinical development including novel multi-targeted TKIs.

Keywords: Platelet derived growth factor receptor, Tyrosine Kinase Inhibitors, Glioblastoma Multiforme, Clinical trials

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