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Biological and Environmental Research Ontology
| Id | http://purl.obolibrary.org/obo/NCIT_C106126
http://purl.obolibrary.org/obo/NCIT_C106126
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|---|---|
| Preferred Name | MEK/Aurora Kinase Inhibitor BI 847325 |
| Definitions |
An orally available dual inhibitor of mitogen-activated protein kinase kinase (MEK) and Aurora kinases, with potential antineoplastic activity. Upon oral administration, MEK/Aurora kinase inhibitor BI 847325 selectively binds to and inhibits the activity of MEK, which both prevents the activation of MEK-dependent effector proteins and inhibits growth factor-mediated cell signaling. BI 847325 also binds to and inhibits the activity of the Aurora kinases A, B and C which may disrupt the assembly of the mitotic spindle apparatus, prevent chromosome segregation, and inhibit both cellular division and proliferation in Aurora kinase-overexpressing tumor cells. Altogether, this leads to the inhibition of cell proliferation and tumor growth as well as the induction of tumor regression. MEK, a dual-specificity threonine/tyrosine kinase that plays a key role in the activation of the RAS/RAF/MEK/ERK signaling pathway, is frequently upregulated in a variety of tumor cell types. Aurora kinases are serine-threonine kinases that play essential roles in mitotic checkpoint control and are overexpressed by a wide variety of cancer cell types.
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| Type | http://www.w3.org/2002/07/owl#Class |
All Properties
| definition | An orally available dual inhibitor of mitogen-activated protein kinase kinase (MEK) and Aurora kinases, with potential antineoplastic activity. Upon oral administration, MEK/Aurora kinase inhibitor BI 847325 selectively binds to and inhibits the activity of MEK, which both prevents the activation of MEK-dependent effector proteins and inhibits growth factor-mediated cell signaling. BI 847325 also binds to and inhibits the activity of the Aurora kinases A, B and C which may disrupt the assembly of the mitotic spindle apparatus, prevent chromosome segregation, and inhibit both cellular division and proliferation in Aurora kinase-overexpressing tumor cells. Altogether, this leads to the inhibition of cell proliferation and tumor growth as well as the induction of tumor regression. MEK, a dual-specificity threonine/tyrosine kinase that plays a key role in the activation of the RAS/RAF/MEK/ERK signaling pathway, is frequently upregulated in a variety of tumor cell types. Aurora kinases are serine-threonine kinases that play essential roles in mitotic checkpoint control and are overexpressed by a wide variety of cancer cell types. |
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| prefLabel | MEK/Aurora Kinase Inhibitor BI 847325
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| label | MEK/Aurora Kinase Inhibitor BI 847325
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| PDQ_Closed_Trial_Search_ID | 698315
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| code | C106126
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| prefixIRI | NCIT:C106126
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| in_subset | |
| Preferred_Name | MEK/Aurora Kinase Inhibitor BI 847325
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| Maps_To | MEK/Aurora Kinase Inhibitor BI 847325
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| NCI_Drug_Dictionary_ID | 698315
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| type | |
| Is_Value_For_GDC_Property | |
| subClassOf | |
| PDQ_Open_Trial_Search_ID | 698315
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| Semantic_Type | Pharmacologic Substance
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| UMLS_CUI | C3827151
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