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Biological and Environmental Research Ontology
| Id | http://purl.obolibrary.org/obo/NCIT_C78186
http://purl.obolibrary.org/obo/NCIT_C78186
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|---|---|
| Preferred Name | Rucaparib Phosphate |
| Definitions |
The phosphate salt form of rucaparib, an orally bioavailable tricyclic indole and inhibitor of poly(ADP-ribose) polymerases (PARPs) 1 (PARP1), 2 (PARP2) and 3 (PARP3), with potential chemo/radiosensitizing and antineoplastic activities. Upon administration, rucaparib selectively binds to PARP1, 2 and 3 and inhibits PARP-mediated DNA repair. This enhances the accumulation of DNA strand breaks, promotes genomic instability and induces cell cycle arrest and apoptosis. This may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. PARPs are enzymes activated by single-strand DNA breaks that catalyze the post-translational ADP-ribosylation of nuclear proteins, which induces signaling and the recruitment of other proteins to repair damaged DNA. The PARP-mediated repair pathway plays a key role in DNA repair and is dysregulated in a variety of cancer cell types.
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| Type | http://www.w3.org/2002/07/owl#Class |
All Properties
| definition | The phosphate salt form of rucaparib, an orally bioavailable tricyclic indole and inhibitor of poly(ADP-ribose) polymerases (PARPs) 1 (PARP1), 2 (PARP2) and 3 (PARP3), with potential chemo/radiosensitizing and antineoplastic activities. Upon administration, rucaparib selectively binds to PARP1, 2 and 3 and inhibits PARP-mediated DNA repair. This enhances the accumulation of DNA strand breaks, promotes genomic instability and induces cell cycle arrest and apoptosis. This may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. PARPs are enzymes activated by single-strand DNA breaks that catalyze the post-translational ADP-ribosylation of nuclear proteins, which induces signaling and the recruitment of other proteins to repair damaged DNA. The PARP-mediated repair pathway plays a key role in DNA repair and is dysregulated in a variety of cancer cell types. |
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| prefLabel | Rucaparib Phosphate
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| label | Rucaparib Phosphate
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| PDQ_Closed_Trial_Search_ID | 594405
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| code | C78186
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| Has_Target | |
| prefixIRI | NCIT:C78186
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| in_subset |
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| Display_Name | Rucaparib Phosphate
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| Preferred_Name | Rucaparib Phosphate
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| FDA_UNII_Code | H3M9955244
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| Contributing_Source |
CTRP
FDA
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| Chemical_Formula | C19H18FN3O.H3O4P
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| Maps_To | Rucaparib Phosphate
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| CAS_Registry | 459868-92-9
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| NCI_Drug_Dictionary_ID | 594405
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| Legacy Concept Name | PARP-1_Inhibitor_AG014699
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| type | |
| ALT_DEFINITION | A substance being studied in the treatment of breast cancers caused by mutations (changes) in the BRCA1 and BRCA2 genes. It is also being studied in the treatment of other types of cancer. It blocks an enzyme involved in many functions of the cell, including the repair of DNA damage. DNA damage may be caused by normal cell actions, UV light, some anticancer drugs, and radiation used to treat cancer. AG014699 may cause cancer cells to die. It is a type of poly(ADP-ribose) polymerase inhibitor.
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| Is_Value_For_GDC_Property | |
| subClassOf | |
| PDQ_Open_Trial_Search_ID | 594405
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| Semantic_Type |
Organic Chemical
Pharmacologic Substance
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| UMLS_CUI | C2603422
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