Results 211 to 220 of about 43,499 (244)
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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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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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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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