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The Therapeutic Potential of Poly(ADP-Ribose) Polymerase Inhibitors
Pharmacological Reviews, 2002Poly(ADP-ribose) polymerase-1 (PARP-1) is a member of the PARP enzyme family consisting of PARP-1 and several recently identified novel poly(ADP-ribosylating) enzymes. PARP-1 is an abundant nuclear protein functioning as a DNA nick-sensor enzyme. Upon binding to DNA breaks, activated PARP cleaves NAD(+) into nicotinamide and ADP-ribose and polymerizes ...
László, Virág, Csaba, Szabó
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Poly(ADP-Ribose) Polymerase Inhibitor Combination Therapy
The Cancer Journal, 2021Abstract The introduction of poly(ADP-ribose) polymerase (PARP) inhibitors has led to significant improvements in outcome for several cancer types, most notably high-grade serous ovarian cancer. However, in general, benefit is restricted to tumors characterized by either BRCA1/2 mutation or homologous recombination deficiency.
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Structural requirements for inhibitors of poly(ADP-ribose) Polymerase
Journal of Cancer Research and Clinical Oncology, 1990The purpose of this study was to examine the structure/activity relationships of a series of substituted benzamides as poly(ADP-ribose) polymerase inhibitors. The experimental approach has involved the use of in vitro and in vivo assays in order to gather information either on the intrinsic activity of the benzamides or on the effect of various ...
SESTILI, PIERO +8 more
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Novel poly(ADP-ribose) polymerase-1 inhibitors
Bioorganic & Medicinal Chemistry Letters, 2007Synthesis and activity of a series of 3-aroyl-derived analogs of novel pyrrolocarbazole 1 as poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors are disclosed.
Derek, Dunn +3 more
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Some protease inhibitors are also inhibitors of poly(ADP-ribose) polymerase
Carcinogenesis, 1986The low-molecular-weight peptide protease inhibitors, tosyl-lysine-chloromethyl ketone, antipain and leupeptin, inhibited poly(ADP-ribose) [poly(ADP-Rib)] polymerase in permeable cells. The concentrations required for 50% inhibition were 3.6, 5 and 29 mM, respectively. Two peptides without protease inhibitor activity, fibrinopeptide A and phenylalanine-
J E, Cleaver +3 more
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Poly(ADP-ribose) polymerase and the therapeutic effects of its inhibitors
Nature Reviews Drug Discovery, 2005Poly(ADP-ribose) polymerases (PARPs) are involved in the regulation of many cellular functions. Three consequences of the activation of PARP1, which is the main isoform of the PARP family, are particularly important for drug development: first, its role in DNA repair; second, its capacity to deplete cellular energetic pools, which culminates in cell ...
Prakash, Jagtap, Csaba, Szabó
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Poly(ADP-ribose) polymerase inhibitors as potential chemotherapeutic agents
Biochemical Society Transactions, 2004PARP [poly(ADP-ribose) polymerase] activity is up-regulated by binding to DNA strand breaks and its association with DNA repair is well documented. Many anticancer therapies work by inducing breaks in DNA, if unrepaired these can lead to cell death. As PARP promotes DNA repair there is a strong rational to suggest that its inhibition may increase the ...
H E, Bryant, T, Helleday
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A Review on Poly (ADP-ribose) Polymerase (PARP) Inhibitors and Synthetic Methodologies
Current Medicinal Chemistry, 2021Ying Li, , Guo-Wu Rao
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