Preferred Label : Factor VIIa Inhibitor PCI-27483;
NCIt related terms : PCI-27483;
NCIt definition : A reversible small-molecule inhibitor of activated factor VII (factor VIIa) with potential
antineoplastic and antithrombotic activities. FVII, a serine protease, becomes 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. In addition, this agent inhibits
both the extrinsic and intrinsic coagulation cascades, preventing blood clot formation.
TF, a blood protein overexpressed on the cell surface of a variety of tumor cell types,
may correlate with poor prognosis; PAR-2 (also known as thrombin receptor-like 1)
is a G protein-coupled receptor (GPCR) and a protease-activated receptor.;
UNII : 6073LCU8U9;
CAS number : 871266-63-6;
Molecule name : PCI-27483;
NCI Metathesaurus CUI : CL413585;
Origin ID : C88324;
UMLS CUI : C2981841;
Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
