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Biological and Environmental Research Ontology
| Id | http://purl.obolibrary.org/obo/NCIT_C166417
http://purl.obolibrary.org/obo/NCIT_C166417
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|---|---|
| Preferred Name | Zegocractin |
| Definitions |
A calcium (Ca2+) release-activated channel (CRAC) inhibitor, with potential anti-inflammatory and protective activities. Upon administration, zegocractin targets, binds to and inhibits the calcium release-activated calcium channel protein 1 (Orai1), which forms the pore of CRAC, and is expressed on both parenchymal cells and immune cells. This prevents the transport of extracellular Ca2+ into the cell and inhibits the subsequent activation of Ca2+-mediated signaling and transcription of target genes. This may prevent Ca2+ entry-mediated cell death. It may also inhibit the proliferation of immune cells and prevents the release of various inflammatory cytokines in immune cells, such as interleukin-2 (IL-2) and tumor necrosis factor-alpha (TNF-a). This may lead to a reduction of inflammatory responses in inflammatory-mediated diseases. CRACs, specialized plasma membrane Ca2+ ion channels composed of the plasma membrane based Orai channels and the endoplasmic reticulum (ER) stromal interaction molecules (STIMs), mediate store operated Ca2+ entry (SOCE) and play a key role in calcium homeostasis. CRACs are overactivated in a variety of cell types, especially certain immune cells during inflammation, including T-lymphocytes, neutrophils and macrophages.
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| Type | http://www.w3.org/2002/07/owl#Class |
All Properties
| definition | A calcium (Ca2+) release-activated channel (CRAC) inhibitor, with potential anti-inflammatory and protective activities. Upon administration, zegocractin targets, binds to and inhibits the calcium release-activated calcium channel protein 1 (Orai1), which forms the pore of CRAC, and is expressed on both parenchymal cells and immune cells. This prevents the transport of extracellular Ca2+ into the cell and inhibits the subsequent activation of Ca2+-mediated signaling and transcription of target genes. This may prevent Ca2+ entry-mediated cell death. It may also inhibit the proliferation of immune cells and prevents the release of various inflammatory cytokines in immune cells, such as interleukin-2 (IL-2) and tumor necrosis factor-alpha (TNF-a). This may lead to a reduction of inflammatory responses in inflammatory-mediated diseases. CRACs, specialized plasma membrane Ca2+ ion channels composed of the plasma membrane based Orai channels and the endoplasmic reticulum (ER) stromal interaction molecules (STIMs), mediate store operated Ca2+ entry (SOCE) and play a key role in calcium homeostasis. CRACs are overactivated in a variety of cell types, especially certain immune cells during inflammation, including T-lymphocytes, neutrophils and macrophages. |
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| prefLabel | Zegocractin
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| label | Zegocractin
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| NCI_META_CUI | CL971668
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| PDQ_Closed_Trial_Search_ID | 800239
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| code | C166417
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| prefixIRI | NCIT:C166417
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| in_subset |
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| Display_Name | Zegocractin
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| Preferred_Name | Zegocractin
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| FDA_UNII_Code | 564AW1RR37
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| Contributing_Source |
CTRP
FDA
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| Maps_To | Calcium Release-activated Channel Inhibitor CM4620
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| CAS_Registry | 1713240-67-5
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| NCI_Drug_Dictionary_ID | 800239
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| type | |
| Is_Value_For_GDC_Property | |
| subClassOf | |
| PDQ_Open_Trial_Search_ID | 800239
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| Semantic_Type | Pharmacologic Substance
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