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Description: PCI-27483 is a novel, potent and reversible small-molecule inhibitor of activated factor VII (factor VIIa) with potential anticancer and antithrombotic activities. Factor VII is a serine protease which can be activated (FVIIa) upon binding with TF forming the FVIIa/TF complex, which induces intracellular signaling pathways by activating protease activated receptor 2 (PAR-2). Upon subcutaneous administration, factor VIIa inhibitor PCI-27483 selectively inhibits factor FVIIa in the VIIa/TF complex, which may prevent PAR-2 activation and PAR2-mediated signal transduction pathways, thereby inhibiting tumor cell proliferation, angiogenesis, and metastasis of TF-overexpressing tumor cells.
References: Cancer Research May 2008 Volume 68, Issue 9 Supplement.; Ther Adv Cardiovasc Dis. 2011 Feb; 5(1):33-59.
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