PARP-1 inhibitorsCancerStructural typesCharacteristicsBiological activityPOLY(ADP-RIBOSE) POLYMERASE INHIBITORIN-VIVOMAMMARY-TUMORSHIGHLY POTENTCOMBINATIONPoly (ADP-ribose) Polymerase-1 (PARP-1) is a member of 17 membered PARP family having diversified biological functions such as synthetic lethality, DNA ...
Among the compounds that have been developed for PARP inhibition, only those bearing pyrazole or indazole scaffolds will be discussed in this review, following the interest of our research group in this type of heterocyclic compounds. It is important to note that the binding of the inhibitor to ...
This compound is a dual PARP-1 and PARP-2 inhibitor, displaying PARP-2 IC50 = 1 nM, and significantly weaker tankyrase activity IC50 = 1.5 μM. In monotherapy, 7 was shown to selectively inhibit the growth of BRCA-1-deficient MDA-MB-436 and HCC1937 cells. In a SW620 xenograft, the ...
PARP inhibitor combination therapy - ScienceDirect In 2014, olaparib (Lynparza) became the first PARP (Poly(ADP-ribose) polymerase) inhibitor to be approved for the treatment of cancer. When used as single ... Amy Dréan a,Christopher J. Lord a,Alan Ashworth b - 《Critical Reviews in Onco...
cancer cell lines and found that in HRD cell lines, PARPi therapy reduced non-homologous end joining (NHEJ)-mediated repair, specifically due to decreased theta-mediated end-joining. The combination of PARPi with ATM serine/threonine kinase inhibitor (ATMi) suppressed both NHEJ and HR pathways ...
Metabolism‐focused CRISPR screen unveils mitochondrial pyruvate carrier 1 as a critical driver for PARP inhibitor resistance in lung cancer Homologous recombination (HR) and poly ADP‐ribosylation are partially redundant pathways for the repair of DNA damage in normal and cancer cells. In cell ... ...
Thus, we investigated whether p53 was involved in mediating DOX-induced DNA damage, cell cycle arrest, and oxidative stress by using the pharmaco- logical p53 inhibitor pifithrin-α (PFT-α ) at 72 h after DOX stimulation. We specifically examined the dose-dependent effects of PFT-α...
we investigated the use of the fluorescent Poly (ADP-ribose) Polymerase 1 (PARP1)-inhibitor PARPi-FL for early detection of dysplastic lesions in patient-derived organoids and transgenic mouse models, which closely mimic the transformation from non-malignant Barrett’s Esophagus (BE) to invasive ...
Modulation of Inflammasome and Pyroptosis by Olaparib, a PARP-1 Inhibitor, in the R6/2 Mouse Model of Huntington's Disease Pyroptosis is a type of cell death that is caspase-1 (Casp-1) dependent, which leads to a rapid cell lysis, and it is linked to the inflammasome. We recent... ...
Synthetic lethality between PARP inhibitors and defects in BRCA1/2 is the rationale underlying PARP inhibitor use as a cancer treatment: persistent SSB formation caused by PARP inhibition (PARPi) promotes the collapse of replication forks, which triggers HR for repair; but in cancers with ...