Results 191 to 200 of about 70,337 (231)

Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase

Bioorganic & Medicinal Chemistry Letters, 2008
We have previously described poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors based on a substituted benzyl-phthalazinone scaffold. As an alternative chemical template, a novel series of alkoxybenzamides were developed with restricted conformation through intramolecular hydrogen bond formation; the compounds exhibit low nM enzyme and cellular activity
Keith A, Menear, Claire, Adcock, Francisco Cuenca, Alonso, Kristel, Blackburn, Louise, Copsey, Jan, Drzewiecki, Alexandra, Fundo, Armelle, Le Gall, Sylvie, Gomez, Hashim, Javaid, Carlos Fenandez, Lence, Niall M B, Martin, Chris, Mydlowski, Graeme C M, Smith   +13 more
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‘PARP’ing fibrosis: repurposing poly (ADP ribose) polymerase (PARP) inhibitors

Drug Discovery Today, 2020
Fibrosis is a wound-healing process that results in tissue scarring and organ dysfunction. Several novel mechanisms of fibrogenesis have been discovered recently. In this review, we focus on the role of poly-ADP ribose polymerase (PARP) in major organ fibrosis, such as lungs, heart, liver, and kidneys.
Pooja Dhileepkumar Rao, Himanshu Sankrityayan, Anjali Srivastava, Yogesh A. Kulkarni, Shrikant R. Mulay, Anil Bhanudas Gaikwad   +5 more
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Poly(ADP-ribose) polymerase inhibitors as potential chemotherapeutic agents

Biochemical Society Transactions, 2004
PARP [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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The Therapeutic Potential of Poly(ADP-Ribose) Polymerase Inhibitors

Pharmacological Reviews, 2002
Poly(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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Structural requirements for inhibitors of poly(ADP-ribose) Polymerase

Journal of Cancer Research and Clinical Oncology, 1990
The 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, SPADONI, GILBERTO, BALSAMINI, CESARINO, SCOVASSI I, CATTABENI F, DURANTI E, CANTONI, ORAZIO, HIGGINS D, THOMSON C.   +8 more
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Poly(ADP-ribose) polymerase inhibitors in prostate and urothelial cancer

Current Opinion in Urology, 2020
Purpose 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, Ursula, Lemberger, Andreas, Bruchbacher, Shahrokh F, Shariat, Melanie R, Hassler   +4 more
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Some protease inhibitors are also inhibitors of poly(ADP-ribose) polymerase

Carcinogenesis, 1986
The 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, M J, Banda, W, Troll, C, Borek   +3 more
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Poly(ADP-Ribose) Polymerase Inhibitor Inhibition in Ovarian Cancer

The Cancer Journal, 2021
Abstract 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, 2004
Poly(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, 2002
Novel 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, D., Marakovits, J., Maegley, K., Ekker, A., Yu, X., Hostomsky, Z., Webber, S., Eastman, B., Almassy, R., Li, Curtin, N. J., Newell, D. R., Calvert, A. H., Griffin, R. J., Golding, B. T.   +28 more
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