Results 281 to 290 of about 72,887 (326)

Comparative Analyses of Poly(ADP-Ribose) Polymerase Inhibitors

International Journal of Toxicology, 2022
Poly(ADP-ribose) polymerase inhibitors (PARPi) are approved as monotherapies in BRCA1/2-mutated (m BRCA1/2) metastatic breast and ovarian cancers, and in advanced pancreatic and metastatic castration-resistant prostate cancers. Differential safety profiles across PARPi necessitate improved mechanistic understanding of inhibitor differences, especially
Mausumee Guha, Zhanna Sobol, Mathew Martin, Michelle Hemkens, Tae Sung, Elizabeth Rubitski, Richard Spellman, Martin Finkelstein, Nasir Khan, Wenyue Hu   +9 more
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Poly(ADP-Ribose) Polymerase Inhibitor Combination Therapy

The Cancer Journal, 2021
Abstract 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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Poly(ADP-Ribose) Polymerase Inhibitors

Current Medicinal Chemistry, 2003
Poly(ADP-ribose) polymerase-1 (PARP-1) is the principal member of the PARP enzyme family consisting of PARP-1 and several recently identified novel poly(ADP-ribosyl)ating enzymes. PARP-1 functions as a DNA damage sensor and signalling molecule. Upon binding to DNA breaks, activated PARP cleaves NAD(+) into nicotinamide and ADP-ribose and polymerizes ...
Garry J, Southan, Csaba, Szabó
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Natural Inhibitors of Poly(ADP-ribose) Polymerase-1

Molecular Neurobiology, 2012
Poly(ADP-ribose) polymerases (PARPs) are enzymes that catalyze the transfer of ADP-ribose units from β-nicotinamide adenine dinucleotide (NAD(+)) to acceptor proteins. PARP-1 is responsible for more than 90 % of protein poly-ADP-ribosylation in the brain and may play a role as a molecular switch for cell survival and death. The functional roles of PARP-
Marek, Banasik, Todd, Stedeford, Robert P, Strosznajder   +2 more
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Poly (ADP-ribose) Polymerase Inhibitors in Cancer Treatment

American Journal of Clinical Oncology, 2014
Recent research on inhibitors of poly (ADP-ribose) polymerase (PARP) has demonstrated their potential for improving cancer therapy. They inhibit protein poly (ADP-ribosyl)ation and thus affect numerous molecular and cellular functions, including DNA repair and cell survival, that are critical for such physiological and patho-physiological states as ...
Kathryn A, Mason, Uma, Raju, Thomas A, Buchholz, Li, Wang, Zvonimir L, Milas, Luka, Milas   +5 more
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Current role of poly(ADP-ribose) polymerase inhibitors: which poly(ADP-ribose) polymerase inhibitor and when?

Current Opinion in Oncology, 2019
Purpose of review In the past few years, the advent of PARP inhibitors has been a revolution in the management of ovarian cancer. Patients harboring somatic or germ line BRCA1/2 mutations exhibit different clinical and treatment response behavior.
Hélène, Vanacker, Clémence, Romeo, Isabelle, Ray-Coquard   +2 more
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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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