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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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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 Inhibitor Inhibition in Ovarian Cancer
The Cancer Journal, 2021Abstract The emergence of clinical trial data for poly(ADP-ribose) polymerase inhibitors (PARPi), in BRCA-associated ovarian cancer (epithelial ovarian cancer [EOC]) in 2009 (Lancet 2010;376:245–251) unleashed a rapid series of additional asset development and clinical trial activation across all lines of EOC treatment, ultimately leading to ...
Kathleen N, Moore, Bhavana, Pothuri
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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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Tricyclic Benzimidazoles as Potent Poly(ADP-ribose) Polymerase-1 Inhibitors
Journal of Medicinal Chemistry, 2002Novel tricyclic benzimidazole carboxamide poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors have been synthesized. Several compounds were found to be powerful chemopotentiators of temozolomide and topotecan in both A549 and LoVo cell lines. In vitro inhibition of PARP-1 was confirmed by direct measurement of NAD+ depletion and ADP-ribose polymer ...
Skalitzky +28 more
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Triple-negative Breast Cancer and Poly(ADP-ribose) Polymerase Inhibitors
Anti-Cancer Agents in Medicinal Chemistry, 2012Recent gene profiling studies have identified at least 5 major subtypes of breast cancer, including normal type, luminal A type, luminal B type, human epidermal growth factor receptor (HER)-2 positive type, and basal-like type. Triple-negative breast cancer (TNBC), showing no or low expressions of estrogen receptor (ER), progesterone receptor (PgR ...
Youngjin, Park +5 more
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Potential clinical applications of poly(ADP-ribose) polymerase (PARP) inhibitors
Pharmacological Research, 2002Poly(ADP-ribose) polymerases (PARPs) are defined as cell signaling enzymes that catalyze the transfer of ADP-ribose units from NAD(+)to a number of acceptor proteins. PARP-1, the best characterized member of the PARP family, that presently includes six members, is an abundant nuclear enzyme implicated in cellular responses to DNA injury provoked by ...
TENTORI, LUCIO +2 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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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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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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