Results 161 to 170 of about 80,955 (206)
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Expanding biomarkers for PARP inhibitors
Nature Cancer, 2022International audience ; The efficacy of talazoparib and other PARP inhibitors has been primarily reported in germline BRCA mutation carriers. New results establish germline mutations in PALB2, but not in other homologous recombination (HR) genes, as targets for PARP inhibitors in breast cancer, whereas the added predictive value of HR signatures ...
Florence Coussy, Francois-Clement Bidard
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Development of PARP inhibitors in oncology
Expert Opinion on Investigational Drugs, 2008Poly (ADP-ribose) polymerase (PARP) plays a key role in DNA repair mechanisms by detecting and initiating repair after DNA strand breaks. Inhibition of PARP in DNA repair-defective tumors (like those with BRCA1 or BRCA2 mutations) can lead to gross genomic instability and cell death.
Jordi, Rodon +2 more
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The Vasoactivity of PARP Inhibitors
2015PARP-inhibition has proven to be an attractive therapeutic approach in cancer whereby the effectiveness of DNA-damaging therapy can be enhanced by inhibiting the PARP-mediated DNA-repair process. Generally there is good concordance between enhanced therapeutic efficacy in vitro and that observed in vivo.
Williams, Kaye J., McCrudden, Cian M.
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Tackling PARP inhibitor resistance
Trends in Cancer, 2021Homologous recombination-deficient (HRD) tumours, including those harbouring mutations in the BRCA genes, are hypersensitive to treatment with inhibitors of poly(ADP-ribose) polymerase (PARPis). Despite high response rates, most HRD cancers ultimately develop resistance to PARPi treatment through reversion mutations or genetic/epigenetic alterations to
Fugger, Kasper +3 more
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Mechanisms of PARP Inhibitor Resistance
2023Poly(ADP-ribose) polymerase (PARP) inhibitors (PARPi) represent the first medicines based on the targeting of the DNA damage response (DDR). PARPi have become standard of care for first-line maintenance treatment in ovarian cancer and have also been approved in other cancer indications including breast, pancreatic and prostate.
Mark J, O'Connor, Josep V, Forment
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Nature Reviews Clinical Oncology, 2020
The much anticipated results from two phase III studies evaluating the clinical efficacy of poly(ADP-ribose) polymerase (PARP) inhibition in patients with advanced-stage breast cancer harbouring a germline mutation in BRCA1/2 have established new therapeutic opportunities and yet, have left us with several ongoing questions.
Shani Paluch-Shimon, Fatima Cardoso
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The much anticipated results from two phase III studies evaluating the clinical efficacy of poly(ADP-ribose) polymerase (PARP) inhibition in patients with advanced-stage breast cancer harbouring a germline mutation in BRCA1/2 have established new therapeutic opportunities and yet, have left us with several ongoing questions.
Shani Paluch-Shimon, Fatima Cardoso
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Adverse events of PARP inhibitors
Česká gynekologie, 2021An evaluation of the safety of poly-ADP-ribose-polymerase inhibitors (PARPi) in ovarian cancer treatment.An analysis of the studies on PARP inhibitors, a summary of the most common and serious adverse events.According to the studies, the most common adverse events of PARPi include hematotoxicity, nausea and vomiting.
Martina, Romanová, Jaroslav, Klát
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PARP inhibitor resistance mechanisms and PARP inhibitor derived imaging probes
Expert Review of Anticancer TherapyPoly(ADP-ribose) polymerase 1 (PARP1) inhibition has become a major target in anticancer therapy. While PARP inhibitors (PARPi) are approved for homologous recombination (HR) deficient cancers, therapeutic resistance is a challenge and PARPi are now being investigated in cancers lacking HR deficiencies.
Tony, Yu, Benjamin H, Lok
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Evolution of the Development of PARP Inhibitors
2023PARP inhibitors first entered the clinic in 2003 in combination with DNA damaging agents in an attempt to overcome treatment resistance to established agents. A brief overview of ADP-ribosylator enzyme biology and the early preclinical development of the class is discussed, illustrating the multiple biological activities of these enzymes and potential ...
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IDrugs : the investigational drugs journal, 2005
Poly(ADP-ribose) polymerase (PARP) catalyzes the biochemical conversion of nicotinamide adenine dinucleotide (NAD+) to poly(ADP-ribose) and nicotinamide, which is a weak feedback inhibitor of the enzyme. Early designs of PARP inhibitors were primarily based on mimicking the structure of nicotinamide and resulted in the identification and widespread use
J H, Li, J, Zhang
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Poly(ADP-ribose) polymerase (PARP) catalyzes the biochemical conversion of nicotinamide adenine dinucleotide (NAD+) to poly(ADP-ribose) and nicotinamide, which is a weak feedback inhibitor of the enzyme. Early designs of PARP inhibitors were primarily based on mimicking the structure of nicotinamide and resulted in the identification and widespread use
J H, Li, J, Zhang
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