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PARP inhibitors are a call of drugs that are a group of pharmacological inhibitors of the enzyme poly ADP ribose polymerase (PARP), which plays a role in repairing DNA in damaged cells. Medical uses of these drugs include the treatment of heritable cancers . [ 1 ]
Thus, PARP inhibitors of various types (e.g. olaparib) for BRCA mutant breast and ovarian cancers can extend beyond these tumors if appropriate biomarkers can be developed to identify HRR defects. There are several additional classes of novel PARP inhibitors that are in various stages of clinical development. [21]
Olaparib, sold under the brand name Lynparza, is a medication for the maintenance treatment of BRCA-mutated advanced ovarian cancer in adults.It is a PARP inhibitor, inhibiting poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.
Pages in category "PARP inhibitors" The following 10 pages are in this category, out of 10 total. This list may not reflect recent changes. ...
PARP inhibitors (e.g. FDA approved olaparib, rucaparib, niraparib and talazoparib) PI3K inhibitors (e.g. perifosine in a phase III trial) Apatinib is a selective VEGF Receptor 2 inhibitor which has shown encouraging anti-tumor activity in a broad range of malignancies in clinical trials. [16]
Poly(ADP-ribose) polymerase-1 is a nuclear enzyme that is found universally in all eukaryotes and is encoded by the PARP-1 gene.It belongs to the PARP family, which is a group of catalysts that transfer ADP-ribose units from NAD (nicotinamide dinucleotide) to protein targets, thus creating branched or linear polymers. [4]
This gene encodes poly(ADP-ribosyl)transferase-like 2 protein, which contains a catalytic domain and is capable of catalyzing a poly(ADP-ribosyl)ation reaction. This protein has a catalytic domain which is homologous to that of poly (ADP-ribosyl) transferase, but lacks an N-terminal DNA binding domain which activates the C-terminal catalytic domain of poly (ADP-ribosyl) transferase.
Rucaparib, sold under the brand name Rubraca, is a PARP inhibitor used as an anti-cancer agent. [2] Rucaparib is a first-in-class pharmaceutical drug targeting the DNA repair enzyme poly-ADP ribose polymerase-1 (PARP-1).