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Biological and Environmental Research Ontology
| Id | http://purl.obolibrary.org/obo/NCIT_C88324
http://purl.obolibrary.org/obo/NCIT_C88324
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|---|---|
| Preferred Name | Factor VIIa Inhibitor PCI-27483 |
| Definitions |
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.
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| Type | http://www.w3.org/2002/07/owl#Class |
All Properties
| 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. |
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| prefLabel | Factor VIIa Inhibitor PCI-27483
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| label | Factor VIIa Inhibitor PCI-27483
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| NCI_META_CUI | CL413585
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| PDQ_Closed_Trial_Search_ID | 661024
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| code | C88324
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| prefixIRI | NCIT:C88324
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| in_subset | |
| Preferred_Name | Factor VIIa Inhibitor PCI-27483
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| FDA_UNII_Code | 6073LCU8U9
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| Contributing_Source | FDA
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| Maps_To | Factor VIIa Inhibitor PCI-27483
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| CAS_Registry | 871266-63-6
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| NCI_Drug_Dictionary_ID | 661024
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| type | |
| Is_Value_For_GDC_Property | |
| subClassOf | |
| PDQ_Open_Trial_Search_ID | 661024
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| Semantic_Type | Pharmacologic Substance
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