Preferred Label : Rucaparib Phosphate;
NCIt synonyms : PARP1 Inhibitor PF-01367338;
NCIt related terms : AG014699; PARP-1 inhibitor AG014699;
NCIt 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.;
Alternative definition : NCI-GLOSS: 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.;
UNII : H3M9955244;
InChIKey : FCCGJTKEKXUBFZ-UHFFFAOYSA-N;
CAS number : 459868-92-9;
Molecule name : PF-01367338; AG-014699; AG 014699;
Chemical formula : C19H18FN3O.H3O4P;
Codes from synonyms : CDR0000630958; CDR0000630955;
Origin ID : C78186;
UMLS CUI : C3642418;
Currated CISMeF NLP mapping
- Semantic type(s)
- chemical_or_drug_affects_gene_product
- concept_is_in_subset
- has_free_acid_or_base_form
- has_target
- is_salt_form_of
