Results 221 to 230 of about 105,598 (267)
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Poly(ADP-Ribose) Polymerase Inhibitors
Current Medicinal Chemistry, 2003Poly(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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Trapping Poly(ADP-Ribose) Polymerase
The Journal of Pharmacology and Experimental Therapeutics, 2015Recent findings indicate that a major mechanism by which poly(ADP-ribose) polymerase (PARP) inhibitors kill cancer cells is by trapping PARP1 and PARP2 to the sites of DNA damage. The PARP enzyme-inhibitor complex "locks" onto damaged DNA and prevents DNA repair, replication, and transcription, leading to cell death.
Yuqiao, Shen +2 more
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Poly (ADP-ribose) polymerase 1
2022Poly (ADP-ribose) polymerase 1 is a key player in DNA repair and transcription regulation. The role of PARP1 in DNA damage recognition and protein signaling in response make it integral to genome stability. Beyond this, it regulates gene expression through chromatin remodeling and transcription factor binding.
Fletcher E Bain +6 more
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Poly(ADP‐ribose) polymerase: Molecular biological aspects
BioEssays, 1991AbstractA number of roles have been ascribed to poly(ADP‐ribose) polymerase* including involvement in DNA repair, cell proliferation, differentiation and transformation. Cloning of the gene has allowed the development of molecular biological approaches to elucidate the structure and the function(s) of this highly conserved enzyme.
G, de Murcia +2 more
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Purification of Recombinant Poly(ADP-Ribose) Polymerases
2011The purification of Poly(ADP-ribose) polymerases from overexpressing cells (Sf9 insect cells, Escherichia coli) has been updated to a fast and reproducible three chromatographic steps protocol. After cell lysis, proteins from the crude extract are separated on a Heparine Sepharose™ column. The PARP-containing fractions are then affinity purified on a 3-
Amé, Jean-Christophe +3 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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Poly(ADP-ribose) polymerase: Structure-function relationship
Biochimie, 1995Dissection of the human poly(ADP-ribose) polymerase (PARP) molecule in terms of its structure-function relationship has proved to be an essential step towards understanding the biological role of poly(ADP-ribosylation) as a cellular response to DNA damage in eukaryotes.
M. Masson +14 more
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Poly(ADP-ribose)polymerase Inhibition - Where Now?
Current Medicinal Chemistry, 2005The poly(ADP-ribose)polymerases (PARPs) catalyse the transfer of ADP-ribose units from the substrate NAD+ to acceptor proteins, biosynthesising polyanionic poly(ADP-ribose) polymers. A major isoform, PARP-1, has been the target for design of inhibitors for over twenty-five years.
Esther C Y, Woon, Michael D, Threadgill
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Regulatory mechanisms of poly(ADP-ribose) polymerase
Molecular and Cellular Biochemistry, 1999Here, we describe the latest developments on the mechanistic characterization of poly(ADP-ribose) polymerase (PARP) [EC 2.4.2.30], a DNA-dependent enzyme that catalyzes the synthesis of protein-bound ADP-ribose polymers in eucaryotic chromatin. A detailed kinetic analysis of the automodification reaction of PARP in the presence of nicked dsDNA ...
R, Alvarez-Gonzalez +4 more
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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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