Results 251 to 260 of about 71,002 (280)
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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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Poly(ADP-ribose) polymerase inhibitors in prostate and urothelial cancer
Current Opinion in Urology, 2020Purpose of review The aim of this article is to give an overview of poly(ADP-ribose) polymerase inhibitors (PARPis) trials in prostate cancer and to discuss emerging approaches with potential future clinical implementation in both prostate and urothelial cancer.
Stephan, Brönimann +4 more
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Relevance of poly (ADP-ribose) polymerase inhibitors in prostate cancer
Current Opinion in Supportive & Palliative Care, 2018Purpose of review Poly (ADP-ribose) polymerase inhibitors (PARPi) are approved drugs for the treatment of ovarian and breast cancer and currently under investigation for the treatment of prostate cancer and other malignancies with aberrations in homologous recombination DNA repair.
Pasquale, Rescigno +2 more
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The poly (ADP ribose) polymerase inhibitor niraparib: Management of toxicities
Gynecologic Oncology, 2018Niraparib is an oral poly(ADP ribose) polymerase (PARP) inhibitor that is currently approved by the United States Food and Drug Administration (US FDA) as well as recently approved by the European Medicines Agency (EMA) for the maintenance treatment of women with recurrent ovarian cancer who are in complete or partial response to platinum-based ...
Kathleen N, Moore +2 more
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New inhibitors of poly(ADP-ribose) polymerase (PARP)
Expert Opinion on Therapeutic Patents, 2004Poly(ADP-ribose) polymerase-1 (PARP-1), the most prominent member of the PARP family, is a DNA-binding protein that is activated by nicks in DNA occurring during inflammation, ischaemia, neurodegeneration or cancer therapy. Activated PARP-1 consumes NAD+ that is cleaved into nicotinamide and ADP-ribose and polymerises the latter onto nuclear acceptor ...
Stefan Peukert, Uwe Schwahn
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2,5-Diketopiperazines: A New Class of Poly(ADP-ribose)polymerase Inhibitors
Biochemistry (Moscow), 2018We show for the first time that natural 2,5-diketopiperazines (cyclic dipeptides) can suppress the activity of the important anticancer target poly(ADP-ribose)polymerase (PARP). Cyclo(L-Ala-L-Ala) and cyclo(L-Ala-D-Ala) can interact with the key residues of the PARP-1 active site, as demonstrated using docking and molecular dynamics simulations. One of
D K, Nilov +6 more
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Poly (ADP-ribose) polymerase inhibitor efficacy in head and neck cancer
Oral Oncology, 2014Poly (ADP-ribose) polymerase inhibitors (PARPi) have shown single agent activity against tumors with deficiencies in the DNA repair mechanism homologous recombination including, but not limited to those harboring BRCA mutations. We hypothesized that, in the context of homologous recombination deficiency (HRD), PARPi could have an effect in head and ...
Jana Heitmann +6 more
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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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Targeting angiogenesis with poly(ADP-ribose) polymerase inhibitors
2007The process of angiogenesis is mediated by a wide range of factors, including pro-inflammatory cytokines. On the basis of the involvement of inflammation in tumor development and of the dual role of PARP inhibitor as enhancer of chemotherapy or as anti-inflammatory agent we have investigated the ability of PARP inhibitors to affect endothelial ...
MUZI, ALESSIA +9 more
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