Preferred Label : Rucaparib;
NCIt synonyms : 6H-Pyrrolo(4,3,2-ef)(2)benzazepin-6-one, 8-Fluoro-1,3,4,5-tetrahydro-2-(4-((methylamino)methyl)phenyl)-; 8-Fluoro-2-(4-((methylamino)methyl)phenyl)-1,3,4,5-tetrahydro-6H-azepino(5,4,3-cd)indol-6-one;
NCIt 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.;
UNII : 8237F3U7EH;
InChIKey : HMABYWSNWIZPAG-UHFFFAOYSA-N;
CAS number : 283173-50-2;
Molecule name : AG 14447; AG-14447;
Codes from synonyms : 454;
Origin ID : C137800;
UMLS CUI : C3661315;
Automatic exact mappings (from CISMeF team)
- Currated CISMeF NLP mapping
- See also inter- (CISMeF)
- Semantic type(s)
- UMLS correspondences (same concept)
- chemical_or_drug_affects_gene_product
- concept_is_in_subset
- has_salt_form
- has_target
- is_free_acid_or_base_form_of
