loading...| Preferred Name |
Rucaparib |
|
| Synonyms |
|
|
| Definitions |
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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| ID |
http://purl.obolibrary.org/obo/NCIT_C137800 |
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| Accepted_Therapeutic_Use_For |
ecurrent ovarian, fallopian tube, or primary peritoneal cancer |
|
| CAS_Registry |
283173-50-2 |
|
| code |
C137800 |
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| Contributing_Source |
CTRP FDA |
|
| definition |
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. |
|
| Display_Name |
Rucaparib |
|
| FDA_UNII_Code |
8237F3U7EH |
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| Has_Salt_Form | ||
| in_subset |
http://purl.obolibrary.org/obo/NCIT_C63923 http://purl.obolibrary.org/obo/NCIT_C177537 http://purl.obolibrary.org/obo/NCIT_C116977 http://purl.obolibrary.org/obo/NCIT_C128784 http://purl.obolibrary.org/obo/NCIT_C118169 |
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| Is_Value_For_GDC_Property | ||
| label |
Rucaparib |
|
| Maps_To |
Rucaparib |
|
| Preferred_Name |
Rucaparib |
|
| prefixIRI |
NCIT:C137800 |
|
| prefLabel |
Rucaparib |
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| Semantic_Type |
Pharmacologic Substance |
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| UMLS_CUI |
C3661315 |
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| subClassOf |