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Biological and Environmental Research Ontology
| Id | http://purl.obolibrary.org/obo/NCIT_C131910
http://purl.obolibrary.org/obo/NCIT_C131910
|
|---|---|
| Preferred Name | Abequolixron |
| Definitions |
An orally bioavailable agonist of the nuclear receptor liver X receptor beta (LXRbeta; NR1H2; LXR-b), with potential immunomodulating and antineoplastic activities. Upon oral administration, abequolixron selectively targets and binds to LXRbeta, thereby activating LXRbeta-mediated signaling, leading to the transcription of certain tumor suppressor genes and the downregulation of certain tumor promoter genes. This particularly activates the expression of apolipoprotein E (ApoE), a tumor suppressor protein, in tumor cells and certain immune cells. This activates the innate immune system, resulting in depletion of immunosuppressive myeloid-derived suppressor cells (MDSCs), tumor cells and endothelial cells in the tumor microenvironment. This reverses immune evasion, enhances anti-tumor immune responses and inhibits proliferation of tumor cells. LXRbeta, a member of the oxysterol receptor family, which is in the nuclear receptor family of transcription factors, plays a key role in cholesterol transport, glucose metabolism and the modulation of inflammatory responses; activation of LXRbeta suppresses tumor cell invasion, angiogenesis, tumor progression, and metastasis in a variety of tumor cell types. The expression of the ApoE protein becomes silenced in human cancers as they grow, become invasive, and metastasize; ApoE silencing is related to reduced survival in cancer patients. The LXR-ApoE pathway regulates the ability of cancers to evade the immune system and recruit blood vessels.
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| Type | http://www.w3.org/2002/07/owl#Class |
All Properties
| definition | An orally bioavailable agonist of the nuclear receptor liver X receptor beta (LXRbeta; NR1H2; LXR-b), with potential immunomodulating and antineoplastic activities. Upon oral administration, abequolixron selectively targets and binds to LXRbeta, thereby activating LXRbeta-mediated signaling, leading to the transcription of certain tumor suppressor genes and the downregulation of certain tumor promoter genes. This particularly activates the expression of apolipoprotein E (ApoE), a tumor suppressor protein, in tumor cells and certain immune cells. This activates the innate immune system, resulting in depletion of immunosuppressive myeloid-derived suppressor cells (MDSCs), tumor cells and endothelial cells in the tumor microenvironment. This reverses immune evasion, enhances anti-tumor immune responses and inhibits proliferation of tumor cells. LXRbeta, a member of the oxysterol receptor family, which is in the nuclear receptor family of transcription factors, plays a key role in cholesterol transport, glucose metabolism and the modulation of inflammatory responses; activation of LXRbeta suppresses tumor cell invasion, angiogenesis, tumor progression, and metastasis in a variety of tumor cell types. The expression of the ApoE protein becomes silenced in human cancers as they grow, become invasive, and metastasize; ApoE silencing is related to reduced survival in cancer patients. The LXR-ApoE pathway regulates the ability of cancers to evade the immune system and recruit blood vessels. |
|---|---|
| label | Abequolixron
|
| prefLabel | Abequolixron
|
| in_subset | |
| Preferred_Name | Abequolixron
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| Is_Value_For_GDC_Property | |
| Maps_To | Liver X Receptor beta Agonist RGX-104
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| PDQ_Open_Trial_Search_ID | 786379
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| FDA_UNII_Code | Q26B92650V
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| prefixIRI | NCIT:C131910
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| NCI_Drug_Dictionary_ID | 786379
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| Contributing_Source | FDA
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| subClassOf | |
| code | C131910
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| type | |
| PDQ_Closed_Trial_Search_ID | 786379
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| Semantic_Type | Pharmacologic Substance
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| CAS_Registry | 610318-54-2
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| NCI_META_CUI | CL520758
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