Results 11 to 20 of about 47,778 (228)
Interactions of PARP1 Inhibitors with PARP1-Nucleosome Complexes
Cells, 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 inhibitors trigger innate immunity via PARP1 trapping-induced DNA damage response
eLife, 2020 It is being increasingly appreciated that the immunomodulatory functions of PARP1 inhibitors (PARPi) underlie their clinical activities in various BRCA-mutated tumors. PARPi possess both PARP1 inhibition and PARP1 trapping activities.
Chiho Kim, Xu-Dong Wang, Yonghao Yu
doaj +3 more sources
Pharmacological 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 +6 more
openaire +2 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]
International 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 +8 more
openaire +3 more sources
Mechanisms of Nucleosome Reorganization by PARP1 [PDF]
International Journal of Molecular Sciences, 2021 Poly(ADP-ribose) polymerase 1 (PARP1) is an enzyme involved in DNA repair, chromatin organization and transcription. During transcription initiation, PARP1 interacts with gene promoters where it binds to nucleosomes, replaces linker histone H1 and participates in gene regulation.
Natalya V. Maluchenko +10 more
openaire +2 more sources
PARP1 in Carcinomas and PARP1 Inhibitors as Antineoplastic Drugs [PDF]
International 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.
Luyao Wang +7 more
openaire +2 more sources
Uncoupling of PARP1 trapping and inhibition using selective PARP1 degradation [PDF]
Nature Chemical Biology, 2019 PARP1 inhibitors (PARPi) are known to kill tumor cells via two mechanisms (PARP1 catalytic inhibition and PARP1 trapping). The relative contribution of these two pathways in mediating the cytotoxicity of PARPi, however, is not well understood. Here we designed a series of small molecule PARP degraders.
Shuai Wang +8 more
openaire +2 more sources
PARP1 Inhibitors: Antitumor Drug Design [PDF]
Acta Naturae, 2015 The poly (ADP-ribose) polymerase 1 (PARP1) enzyme is one of the promising molecular targets for the discovery of antitumor drugs. PARP1 is a common nuclear protein (1-2 million molecules per cell) serving as a sensor for DNA strand breaks. Increased PARP1 expression is sometimes observed in melanomas, breast cancer, lung cancer, and other neoplastic ...
MALYUCHENKO N.V. +4 more
openaire +3 more sources
Advanced 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
Yan Wang +3 more
doaj +1 more source
Poly(ADP-Ribose) Polymerase-1 Lacking Enzymatic Activity Is Not Compatible with Mouse Development
Cells, 2023 Poly(ADP-ribose) polymerase-1 (PARP1) binds DNA lesions to catalyse poly(ADP-ribosyl)ation (PARylation) using NAD+ as a substrate. PARP1 plays multiple roles in cellular activities, including DNA repair, transcription, cell death, and chromatin ...
Tatiana Kamaletdinova +11 more
doaj +1 more source