Results 151 to 160 of about 39,225 (199)

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
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Captured snapshots of PARP1 in the active state reveal the mechanics of PARP1 allostery

Molecular Cell, 2022
PARP1 rapidly detects DNA strand break damage and allosterically signals break detection to the PARP1 catalytic domain to activate poly(ADP-ribose) production from NAD+. PARP1 activation is characterized by dynamic changes in the structure of a regulatory helical domain (HD); yet, there are limited insights into the specific contributions that the HD ...
Dragomir B Krastev   +2 more
exaly   +3 more sources

Pleiotropic role of PARP1: an overview

3 Biotech, 2021
Poly (ADP-ribose) polymerase 1 (PARP1) protein is encoded by the PARP1 gene located on chromosome 1 (1q42.12) in human cells. It plays a crucial role in post-translational modification by adding poly (ADP-ribose) (PAR) groups to various proteins and PARP1 itself by utilizing nicotinamide adenine dinucleotide (NAD +) as a substrate.
Vikas Kumar   +4 more
openaire   +2 more sources

PARP1 is required for chromosomal translocations

open access: yesBlood, 2013
Key Points Chromosomal translocations are mediated by PARP1 and can be suppressed by the clinical PARP1 inhibitors.
Justin Wray   +2 more
exaly   +4 more sources

NAD+ rescues aging-induced blood-brain barrier damage via the CX43-PARP1 axis.

Neuron, 2023
Blood-brain barrier (BBB) function deteriorates during aging, contributing to cognitive impairment and neurodegeneration. It is unclear what drives BBB leakage in aging and how it can be prevented.
Rui Zhan   +39 more
semanticscholar   +1 more source

PARP1: A Promising Target for the Development of PARP1-based Candidates for Anticancer Intervention

Current Medicinal Chemistry, 2016
Poly(ADP-ribose) polymerase 1 (PARP1) inhibition, increasing chemosensitization and conferring independent antiproliferation against defective homologous recombination cells, has provided a unique opportunity for anticancer therapeutic intervention.
Xiaolei, Zhu, Xiaodong, Ma, Yongzhou, Hu
openaire   +2 more sources

Sleep tight thanks to Parp1

Nature Reviews Molecular Cell Biology, 2021
DNA damage accumulation in zebrafish neurons during wakefulness is detected by Parp1, which induces a homeostatic drive to sleep and repair the damage.
openaire   +2 more sources

BRCA2 prevents PARPi-mediated PARP1 retention to protect RAD51 filaments

Nature
The tumour-suppressor protein BRCA2 has a central role in homology-directed DNA repair by enhancing the formation of RAD51 filaments on resected single-stranded DNA generated at double-stranded DNA breaks and stimulating RAD51 activity1,2.
Sudipta Lahiri   +6 more
semanticscholar   +1 more source

Imaging poly(ADP-ribose) polymerase-1 (PARP1) in vivo with 18F-labeled brain penetrant positron emission tomography (PET) ligand

Acta Pharmaceutica Sinica B
Poly(ADP-ribose) polymerase 1 (PARP1) is a multifunctional protein involved in diverse cellular functions, notably DNA damage repair. Pharmacological inhibition of PARP1 has therapeutic benefits for various pathologies.
Xin Zhou   +23 more
semanticscholar   +1 more source

Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor.

Journal of Medicinal Chemistry
PARP inhibitors have attracted considerable interest in drug discovery due to the clinical success of first-generation agents such as olaparib, niraparib, rucaparib, and talazoparib. Their success lies in their ability to trap PARP to DNA; however, first-
J. Johannes   +41 more
semanticscholar   +1 more source

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