PARP inhibitors
Chemotherapy reduces PARP1 in cancers of the ovary: implications for future clinical trials involving PARP inhibitors
... To our knowledge, this study is the first to probe the effect of chemotherapy treatment on PARP1 protein expression in HGSC. Considering that all patients en- rolled in previous clinical trials received several cycles of ...
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LKB1 is a DNA damage response protein that regulates cellular sensitivity to PARP inhibitors
... Liver kinase B1 (LKB1) functions as a tumor suppressor encoded by STK11, a gene that mutated in Peutz-Jeghers syndrome and in sporadic cancers. Previous studies showed that LKB1 participates in IR- and ROS-induced DNA ...
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PARP inhibitors in the management of breast cancer: current data and future prospects
... kinase inhibitors targeting overexpressed or amplified HER2 ...– PARP inhibitors ...of PARP inhibitors was that they acted through synthetic lethality by targeting the base excision ...
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<p>PARP Inhibitors in Endometrial Cancer: Current Status and Perspectives</p>
... (PARP) inhibitors. This class of drugs that inhibit PARP enzymes has been investigated in many different types of tumors and its use in the treatment of gynecological malignancies has rapidly ...
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Resistance to PARP inhibitors by SLFN11 inactivation can be overcome by ATR inhibition
... to PARP inhibitors, we demonstrate that the addition of an ATR inhibitor overcomes such resistance (Figure ...under PARP inhibitor treatment. Our experiments show that ATR and PARP inhibitor ...
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Advances in using PARP inhibitors to treat cancer
... The Cancer Genome Atlas Research Project recently reported on the molecular aberrations in high grade ser- ous ovarian adenocarcinoma, demonstrating a defect in the HR pathway in half of the 489 tumors analyzed [24]. ...
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Targeting DNA Repair in Cancer: Beyond PARP Inhibitors.
... of PARP inhibitors is not restricted to patients with germline or somatic BRCA1/2 mutations however, and significant efforts are underway to determine tumors that are essentially HR deficient through other ...
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A decade of clinical development of PARP inhibitors in perspective.
... of PARP inhibitor clinical development, a work that has resulted in the registration of several PARP inhibitors in breast (olaparib and talazoparib) and ovarian cancer (olaparib, niraparib and ...
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Synthetic lethal targeting of oncogenic transcription factors in acute leukemia by PARP inhibitors
... (PARP) inhibitors (PARPi) have given renewed enthusiasm to developing anticancer treatments that can specifically target cancer cells but spare the normal 1,2 ...of PARP in a variety of DNA repair ...
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Synthetic lethal therapies for cancer: what's next after PARP inhibitors?
... The genetic concept of synthetic lethality has now been validated clinically through the demonstrated efficacy of PARP inhibitors (PARPi) for the treatment of cancers in individuals with germline mutations ...
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An update on PARP inhibitors for the treatment of cancer
... (PARP) inhibitors (PARPi) has progressed greatly over the last few years and has shown encouraging results in the BRCA1/2 mutation–related ...molecular inhibitors; future and ongoing trials will ...
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Reverse the Resistance to PARP Inhibitors
... by PARP enzymes. Many clinical trials show that PARP inhibitors are promising in treatment of ...reducing inhibitors’ affinity for PARP1, restoring HR repair pathway, and suppressing ...to ...
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Targeted therapy with Poly(ADP-ribose) polymerase (PARP) inhibitors for the treatment of solid tumours
... Abbreviated description of the state of knowledge: PARP inhibitors have been used in the standard treatment of ovarian cancer. Three of them: Olaparyb, Rucaparyb and Niraparyb have indications for ...
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New combinatorial strategies to improve the PARP inhibitors efficacy in the urothelial bladder Cancer treatment
... DDR inhibitors, as PARP inhibitors, determine an increase of DNA damage, especially in tu- mors that show a defects in DNA repair pathways, in- creasing the tumor mutational load and stimulating the ...
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Resistance relationships between platinum and parp inhibitors in ovarian cancer
... Gene expression was compared between:• Relatively Olaparib Sensitive A2780, CAOV3, ES-2, HOC-1 • Relatively Olaparib Resistant HEY, IGROV-1, OVCAR420 OVCAR432 • When comparing the relati[r] ...
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Beyond DNA repair: the novel immunological potential of PARP inhibitors.
... polymerase inhibitors (PARPi) and defects in the DNA repair tumor suppressor genes BRCA1 and BRCA2 (known as breast cancer type 1/2 susceptibility genes), has led to a more targeted approach to therapeutically ...
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Advances and perspectives of PARP inhibitors
... Fig. 1 PARP and PARPis. a The structure schematic of PARP molecule. There are six main domains of PARP1 which include three zinc finger-related domains (DNA binding domains), one BRCA1 C-terminus domain ...
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PARP inhibitors: Synthetic lethality in the clinic.
... CHEK1/2 inhibitors) has gained some traction of late, being bolstered by the recent development of drug- like WEE1 and ATR inhibitors that now make this a testable hypothesis in clinical trials ...
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The evolving landscape of predictive biomarkers of response to PARP inhibitors
... their PARP-trapping potency (Figure ...potent PARP trapper (nanomolar potency), veliparib is primarily a catalytic inhibitor with only weak PARP-trapping ability (5, ...TOP1 inhibitors (11) ...
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Novel treatment strategies in triple-negative breast cancer: specific role of poly(adenosine diphosphate-ribose) polymerase inhibition
... The high degree of genomic instability observed in TNBC without germ-line BRCA mutation has suggested the pres- ence of other germ-line or somatically acquired defects in DNA-repair proficiency, and has encouraged the ...
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