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Biological and Environmental Research Ontology
| Id | http://purl.obolibrary.org/obo/NCIT_C156729
http://purl.obolibrary.org/obo/NCIT_C156729
|
|---|---|
| Preferred Name | Itacnosertib |
| Definitions |
An orally bioavailable inhibitor of activin A receptor type 1 (activin receptor-like kinase 2; ALK2; ALK-2; ACRV1), with potential antineoplastic activity. Upon oral administration,itacnosertib targets, binds to and inhibits the activity of ALK-2. This prevents ALK-2-mediated signaling and inhibits cell growth in ALK-2-overexpressing tumor cells. In addition, in cancer and inflammatory conditions, ALK-2 is upregulated in response to increased signaling of pro-inflammatory cytokines, especially interleukin-6 (IL-6), and enhances the secretion of hepcidin, a peptide liver hormone and a key modulator of iron homeostasis. Blocking ALK-2-mediated pathways in inflammation and cancer leads to a decrease of hepcidin expression and restores plasma iron levels, thereby preventing low serum iron levels and anemia of chronic disease (ACD). ALK-2, a serine/threonine receptor kinase, is constitutively activated due to activating mutations or upregulated upstream signaling pathways in inflammatory conditions and certain types of cancer.
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| Type | http://www.w3.org/2002/07/owl#Class |
All Properties
| definition | An orally bioavailable inhibitor of activin A receptor type 1 (activin receptor-like kinase 2; ALK2; ALK-2; ACRV1), with potential antineoplastic activity. Upon oral administration,itacnosertib targets, binds to and inhibits the activity of ALK-2. This prevents ALK-2-mediated signaling and inhibits cell growth in ALK-2-overexpressing tumor cells. In addition, in cancer and inflammatory conditions, ALK-2 is upregulated in response to increased signaling of pro-inflammatory cytokines, especially interleukin-6 (IL-6), and enhances the secretion of hepcidin, a peptide liver hormone and a key modulator of iron homeostasis. Blocking ALK-2-mediated pathways in inflammation and cancer leads to a decrease of hepcidin expression and restores plasma iron levels, thereby preventing low serum iron levels and anemia of chronic disease (ACD). ALK-2, a serine/threonine receptor kinase, is constitutively activated due to activating mutations or upregulated upstream signaling pathways in inflammatory conditions and certain types of cancer. |
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| prefLabel | Itacnosertib
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| label | Itacnosertib
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| NCI_META_CUI | CL935854
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| PDQ_Closed_Trial_Search_ID | 795585
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| code | C156729
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| Has_Target | |
| prefixIRI | NCIT:C156729
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| in_subset |
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| Display_Name | Itacnosertib
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| Preferred_Name | Itacnosertib
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| FDA_UNII_Code | 22Z53X5LHF
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| Contributing_Source |
CTRP
FDA
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| Maps_To | ALK-2 Inhibitor TP-0184
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| CAS_Registry | 1628870-27-8
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| NCI_Drug_Dictionary_ID | 795585
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| type | |
| Is_Value_For_GDC_Property | |
| subClassOf | |
| PDQ_Open_Trial_Search_ID | 795585
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| Semantic_Type | Pharmacologic Substance
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