Cisplatin-induced kidney dysfunction was prevented by another PARP inhibitor, BGP-15. The cisplatin-caused edema formation was reversed as showed by MRI analysis. High-energy phosphate intermediate levels were reestablished by BGP-15 treatment demonstrated in vivo by localized NMR spectroscopy, which ...
PARP inhibitor is a cancer therapy that targets Poly ADP-ribose Polymerase. It is the first anti-cancer drug that has successfully used the concept of Synthetic Lethality and has been approved for clinical use. Its principle is not difficult to understand: cancer patients with BRCA1 or BRCA2 g...
The clinical application of PARPi is becoming increasingly widespread, not only in the treatment of ovarian cancer but also in other BRCA1/2-related cancers. While their therapeutic effects are significant, their safety and tolerability are also a major concern. The most common adverse events assoc...
Keywords PARP inhibitor, Ovarian cancer, BRCA, Synthetic lethality, Homologous recombination repair, Chemotherapy resistance, Biomarkers, Side effect Introduction As a common gynecological tumor, ovarian cancer has many different tissue types. 90% of them are epithelial cell type, and the rest ...
MINIREVIEW British Journal of Cancer (2015) 113, S10–S16 | doi: 10.1038/bjc.2015.395 Keywords: olaparib; ovarian cancer; BRCA; PARP inhibitor; PFS; TFST; TSST PARP inhibitors in ovarian cancer: Clinical evidence for informed treatment decisions Jonathan A Ledermann*,1 and Fatima El-Khouly1 ...
The ability of different PARPi to inhibit the catalytic activity of PARP family members does not directly correlate with cytotoxic potential. All PARPi contain a benzamide moiety, which is a key feature for binding to PARP-1, but each inhibitor differs in size and flexibility, accounting for di...
While reports of radiotherapy and PARP inhibitor combination studies have been limited, there are multiple ongoing clinical trials of PARP inhibitors in combination with radiotherapy. Talazoparib has been shown to potentiate the effects of radiation and chemotherapy in vivo in a variety of cancers ...
Parp-inhibitorNiraparibOlaparibRucaparibVeliparibBACKGROUND :The second decade of 2000s is witnessing a new ovarian cancer (OC) paradigm shift thanks to the results recently obtained by a new class of targeted agents: the Poly(ADP-ribose)polymerase (PARP)-Inhibitors (PARPi). Aim of this meta...
Learn more about LYNPARZA® (olaparib) as a PARP inhibitor for certain patients with certain types of Ovarian, Breast, Prostate or Pancreatic Cancer.
We then tested whether other PTMs — such as SUMOylation or PARylation — could be involved in DPC repair. To this end, we supplemented egg extracts with an E1 ubiquitin-activating enzyme inhibitor (Ub.E1i), SUMO E1 inhibitor (SUMOi), or the PARP1 inhibitor talazoparib (PARPi) (Fig....