Description
PF-03758309 is an ATP-competitive inhibitor of p21-activated kinase 4 (PAK4), a kinase typically upregulated in many cancers. This compound exhibits anticancer chemotherapeutic and anti-metastatic activities. Inhibition of PAK4 inhibits cell motility, proliferation, and survival in cellular models of cancer and suppresses tumor growth in animal models of cancer. PF-03758309 also inhibits fusion and migration of preosteoclasts, osteoclast differentiation, and podosome formation in cellular models of osteoclast-related disorders.
References
Choi SW, Yeon JT, Ryu BJ, et al. Repositioning Potential of PAK4 to Osteoclastic Bone Resorption. J Bone Miner Res. 2015 Jan 31. [Epub ahead of print]. PMID: 25640698.
Ryu BJ, Lee H, Kim SH, et al. PF-3758309, p21-activated kinase 4 inhibitor, suppresses migration and invasion of A549 human lung cancer cells via regulation of CREB, NF-κB, and β-catenin signalings Mol Cell Biochem. 2014 Apr;389(1-2):69-77. PMID: 24366569.
Murray BW, Guo C, Piraino J, et al. Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proc Natl Acad Sci U S A. 2010 May 18;107(20):9446-51. PMID: 20439741.
www.clinicaltrials.gov/show/NCT00932126
