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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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Current Breast Cancer Reports, 2011
Poly (ADP-ribose) polymerase (PARP) is a novel therapeutic target in cancer. Preclinical studies demonstrate that PARP inhibitors selectively kill BRCA-deficient cells and potentiate the effects of DNA-damaging agents. There are several PARP inhibitors in clinical development, including olaparib, iniparib, veliparib, PF-01367338, and MK-4827.
Hongyan Liang, Antoinette R. Tan
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Poly (ADP-ribose) polymerase (PARP) is a novel therapeutic target in cancer. Preclinical studies demonstrate that PARP inhibitors selectively kill BRCA-deficient cells and potentiate the effects of DNA-damaging agents. There are several PARP inhibitors in clinical development, including olaparib, iniparib, veliparib, PF-01367338, and MK-4827.
Hongyan Liang, Antoinette R. Tan
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2014
© Springer Science+Business Media New York 2017. All rights reserved. PARP enzymes synthese poly(ADP-ribose) (PAR) using nicotinamide adenine dinucleotide (NAD+) as a substrate. PARP-1 is the most extensively studied of a family of PARP enzymes. It is a highly abundant nuclear protein that is activated by DNA breaks and facilitates their repair.
Patterson MJ, Drew Y, Curtin NJ
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© Springer Science+Business Media New York 2017. All rights reserved. PARP enzymes synthese poly(ADP-ribose) (PAR) using nicotinamide adenine dinucleotide (NAD+) as a substrate. PARP-1 is the most extensively studied of a family of PARP enzymes. It is a highly abundant nuclear protein that is activated by DNA breaks and facilitates their repair.
Patterson MJ, Drew Y, Curtin NJ
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PARP inhibitor combination therapy
Critical Reviews in Oncology/Hematology, 2016In 2014, olaparib (Lynparza) became the first PARP (Poly(ADP-ribose) polymerase) inhibitor to be approved for the treatment of cancer. When used as single agents, PARP inhibitors can selectively target tumour cells with BRCA1 or BRCA2 tumour suppressor gene mutations through synthetic lethality.
Dréan, A, Lord, CJ, Ashworth, A
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Poly (ADP-Ribose) Polymerases (PARPs) and PARP Inhibitor-Targeted Therapeutics
Anti-Cancer Agents in Medicinal Chemistry, 2019Background:Poly-ADP-ribosylation, that is, adding ADP-ribose moieties to a protein, is a unique type of protein post-translational modification that regulates various cellular processes such as DNA repair, mitosis, transcription, and cell growth. Small-molecule inhibitors of poly-ADP-ribose polymerase 1 (PARP1) have been developed as anticancer agents ...
Nan, Li +3 more
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2018This Master thesis research was conducted at the Laboratory of Organic Chemistry, at the Department of Chemistry of Aristotle University of Thessaloniki. Main goal of this scientific research was the design and study of potential inhibitors of PARP-1, through 1,3-dipolar cycloaddition.
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Poly(ADP-ribose) polymerase (PARP) and PARP inhibitors
Drug Discovery Today: Disease Models, 2012PARP-1 protects cells from endogenous and therapeutically inflicted DNA damage. PARP inhibitors have been under development since 1980 and first entered clinical trial in 2003. They are an exciting new class of drugs that have the potential to increase the efficacy of anticancer DNA damaging agents and to selectively target cells that have defects in ...
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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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Pharmacological Research, 2005
The activation of poly(ADP-ribose) polymerase (PARP) is well considered to play an important role in various patho-physiological conditions like inflammation and shock. A vast amount of circumstantial evidence implicates oxygen-derived free radicals (especially, superoxide and hydroxyl radical) and high-energy oxidants (such as peroxynitrite) as ...
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The activation of poly(ADP-ribose) polymerase (PARP) is well considered to play an important role in various patho-physiological conditions like inflammation and shock. A vast amount of circumstantial evidence implicates oxygen-derived free radicals (especially, superoxide and hydroxyl radical) and high-energy oxidants (such as peroxynitrite) as ...
openaire +2 more sources