Results 1 to 10 of about 54,968 (233)

Selective PARP1 inhibitors, PARP1-based dual-target inhibitors, PROTAC PARP1 degraders, and prodrugs of PARP1 inhibitors for cancer therapy

open access: yesPharmacological Research, 2022
Poly ADP-ribose polymerase (PARP) plays a critical role in many cellular processes such as DNA damage repair, gene transcription and cell apoptosis. Therefore, targeting PARP represents a promising strategy for cancer therapy. To date, numerous small molecule PARP1 inhibitors have been identified, but many of them suffer from limited clinical efficacy ...
Xiaopeng Peng   +2 more
exaly   +3 more sources

Interactions of PARP1 Inhibitors with PARP1-Nucleosome Complexes

open access: yesCells, 2022
Inhibitors (PARPi) of poly(ADP-ribose-)polymerase-1 (PARP1) are used in antitumor therapy; their cytotoxicity correlates with the efficiency of PARP1 trapping in cell chromatin.
Natalya Maluchenko   +4 more
doaj   +3 more sources

PARP1 in Carcinomas and PARP1 Inhibitors as Antineoplastic Drugs [PDF]

open access: yesInternational Journal of Molecular Sciences, 2017
Poly (ADP-ribose) polymerase 1 (PARP1), the best-studied isoform of the nuclear enzyme PARP family, plays a pivotal role in cellular biological processes, such as DNA repair, gene transcription, and so on. PARP1 has been found to be overexpressed in various carcinomas.
Chao Liang, Fangfei Li, Daogang Guan
exaly   +3 more sources

TIMELESS Forms a Complex with PARP1 Distinct from Its Complex with TIPIN and Plays a Role in the DNA Damage Response [PDF]

open access: yesCell Reports, 2015
PARP1 is the main sensor of single- and double-strand breaks in DNA and, in building chains of poly(ADP-ribose), promotes the recruitment of many downstream signaling and effector proteins involved in the DNA damage response (DDR).
Lauren M. Young   +9 more
doaj   +25 more sources

Increased PARP1‐DNA binding due to autoPARylation inhibition of PARP1 on DNA rather than PARP1‐DNA trapping is correlated with PARP1 inhibitor's cytotoxicity [PDF]

open access: yesInternational Journal of Cancer, 2019
PARP1 inhibitors (PARPis) are used clinically during cancer therapy and are thought to exert their cytotoxicity through PARP1 polymerase inhibition and PARP1‐DNA trapping. Here, we showed no significant correlation between PARP1‐DNA trapping and cytotoxicity induced by PARPis.
Hua-Dong Chen, Yu-Ting Wang, Ne Guo
exaly   +4 more sources

Deacetylation-dependent regulation of PARP1 by SIRT2 dictates ubiquitination of PARP1 in oxidative stress-induced vascular injury

open access: yesRedox Biology, 2021
Poly(ADP-ribose) polymerase 1 (PARP1) has a major regulatory role in cardiovascular disease. However, inhibiting PARP1 activity does not significantly improve clinical outcomes of cardiovascular disease, which suggests that the regulatory mechanism of ...
Jingwei Liu, Liu Cao, Yingxian Sun
exaly   +3 more sources

The multifaceted roles of PARP1 in DNA repair and chromatin remodelling

open access: yesNature Reviews Molecular Cell Biology, 2017
Cells are exposed to various endogenous and exogenous insults that induce DNA damage, which, if unrepaired, impairs genome integrity and leads to the development of various diseases, including cancer.
Arnab Ray Chaudhuri
exaly   +2 more sources

Therapeutic Potentials of Poly (ADP‐Ribose) Polymerase 1 (PARP1) Inhibition in Multiple Sclerosis and Animal Models: Concept Revisiting

open access: yesAdvanced Science, 2022
Poly (ADP‐ribose) polymerase 1 (PARP1) plays a fundamental role in DNA repair and gene expression. Excessive PARP1 hyperactivation, however, has been associated with cell death. PARP1 and/or its activity are dysregulated in the immune and central nervous
David Pleasure, Fuzheng Guo
exaly   +2 more sources

Vascular Protection of Poly(ADP-ribose) Polymerase Inhibitors in the Combination Therapy With Vascular Endothelial Growth Factor Signaling Pathway Inhibitors [PDF]

open access: yesReviews in Cardiovascular Medicine
The Poly(ADP-ribose) polymerase (PARP) family comprises seventeen members that catalyze poly- or mono- adenosine diphosphate (ADP)-ribosylation, a pivotal post-translational modification regulating a wide array of cellular processes, including ...
Jie Ma   +8 more
doaj   +2 more sources

PARP1-DNA co-condensation drives DNA repair site assembly to prevent disjunction of broken DNA ends

open access: yesCell
DNA double-strand breaks (DSBs) are repaired at DSB sites. How DSB sites assemble and how broken DNA is prevented from separating is not understood. Here we uncover that the synapsis of broken DNA is mediated by the DSB sensor protein poly(ADP-ribose ...
Simon Alberti   +2 more
exaly   +2 more sources

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