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https://www.readbyqxmd.com/read/28438542/identification-of-low-micromolar-dual-inhibitors-for-aldose-reductase-alr2-and-poly-adp-ribose-polymerase-parp-1-using-structure-based-design-approach
#1
Navriti Chadha, Om Silakari
Clinical studies have revealed that diabetic retinopathy is a multifactorial disorder. Moreover, studies also suggest that ALR2 and PARP-1 co-occur in retinal cells, making them appropriate targets for the treatment of diabetic retinopathy. To find the dual inhibitors of ALR2 and PARP-1, the structure based design was carried out in parallel for both the target proteins. A series of novel thiazolidine-2,4-dione (TZD) derivatives were therefore rationally designed, synthesized and their in vitro inhibitory activities against ALR2 and PARP-1 were evaluated...
April 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28431224/adp-ribosylation-goes-normal-serine-as-the-major-site-of-the-modification
#2
Qiang Liu, Bogdan I Florea, Dmitri V Filippov
Proteins containing adenosine diphosphate ribosylserine as a posttranslational modification are widespread and formed via HPF1-assisted, PARP-1-mediated PARylation as Bonfiglio et al. (2017) report in a recent issue of Molecular Cell.
April 20, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/28426879/acute-exposure-to-dehp-metabolite-mehp-cause-genotoxicity-mutagenesis-and-carcinogenicity-in-mammalian-chinese-hamster-ovary-cells
#3
Yu-Jung Chang, Chia-Yi Tseng, Pei-Ying Lin, Yu-Chen Chuang, Ming-Wei Chao
Di-(2-ethylhexyl) phthalate (DEHP), the common plasticizer used in the production of polyvinyl chloride, can be converted to the more potent metabolite mono-ethylhexyl phthalate (MEHP). Epidemiological studies have shown an association with elevated induction of rat hepatic cancer and reproductive toxicity in response to MEHP exposure. However, the mechanism of genotoxicity and carcinogenicity induced by MEHP treatment remains unclear. As a means to elucidate the mechanisms of action, lethality and mutagenicity in the adenine phosphoribosyltransferase (aprt+/-) gene induced in several CHO cell types by MEHP were assessed...
March 1, 2017: Carcinogenesis
https://www.readbyqxmd.com/read/28422286/isorhapontigenin-induced-cell-growth-inhibition-and-apoptosis-by-targeting-egfr-related-pathways-in-prostate-cancer
#4
Cuicui Zhu, Qingyi Zhu, Zhaomeng Wu, Yingying Yin, Dan Kang, Shan Lu, Ping Liu
Isorhapontigenin (ISO), a naturally phytopolyphenol compound existing in Chinese herb, apples and various vegetables, has attracted extensive interest in recent years for its diverse pharmacological characteristics. Increasing evidences reveal that ISO can inhibit cancer cell growth by induced apoptosis, however the molecular mechanisms is not fully understood. In this study, we found for the first time that ISO apparently induced cell growth inhibition and apoptosis by targeting EGFR and its downstream signal pathways in prostate cancer (PCa) cells both in vitro and in vivo, whereas no obviously effect on normal prostate cells...
April 19, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/28415784/misregulation-of-dna-damage-repair-pathways-in-hpv-positive-head-and-neck-squamous-cell-carcinoma-contributes-to-cellular-radiosensitivity
#5
Catherine M Nickson, Parisa Moori, Rachel J Carter, Carlos P Rubbi, Jason L Parsons
Patients with human papillomavirus type 16 (HPV)-associated oropharyngeal squamous cell carcinomas (OPSCC) display increased sensitivity to radiotherapy and improved survival rates in comparison to HPV-negative forms of the disease. However the cellular mechanisms responsible for this characteristic difference are unclear. Here, we have investigated the contribution of DNA damage repair pathways to the in vitro radiosensitivity of OPSCC cell lines. We demonstrate that two HPV-positive OPSCC cells are indeed more radiosensitive than two HPV-negative OPSCC cells, which correlates with reduced efficiency for the repair of ionising radiation (IR)-induced DNA double strand breaks (DSB)...
March 16, 2017: Oncotarget
https://www.readbyqxmd.com/read/28399901/activity-of-trabectedin-and-the-parp-inhibitor-rucaparib-in-soft-tissue-sarcomas
#6
Audrey Laroche, Vanessa Chaire, François Le Loarer, Marie-Paule Algéo, Christophe Rey, Kevin Tran, Carlo Lucchesi, Antoine Italiano
BACKGROUND: Trabectedin has recently been approved in the USA and in Europe for advanced soft-tissue sarcoma patients who have been treated with anthracycline-based chemotherapy without success. The mechanism of action of trabectedin depends on the status of both the nucleotide excision repair (NER) and homologous recombination (HR) DNA repair pathways. Trabectedin results in DNA double-strand breaks. We hypothesized that PARP-1 inhibition is able to perpetuate trabectedin-induced DNA damage...
April 11, 2017: Journal of Hematology & Oncology
https://www.readbyqxmd.com/read/28398610/flavonoids-of-rosa-roxburghii-tratt-exhibit-anti-apoptosis-properties-by-regulating-parp-1-aif
#7
REVIEW
Ping Xu, Xingxia Liu, Xiwen Xiong, Wenbo Zhang, Xinhua Cai, Peiyong Qiu, Minghua Hao, Lijuan Wang, Dandan Lu, Xiuhua Zhang, Wancai Yang
Radioprotection is an important approach to reduce the side-effects of radiotherapy. The radioprotective effect of the flavonoids of Rosa roxburghii Tratt (FRT) has been confirmed, and the mechanism has been identified as theBcl-2/caspase-3/PARP-1 signaling pathway. In this study, we investigated the effects of FRT on the intercellular adhesion molecule (ICAM), and vascular cell adhesion protein (VCAM) in addition to apoptosis-related proteins such as Bax/Bcl-2, p-ERK/ERK, p-p53/p53, and p-p38/p38. In the present study, we focused on the effect of FRT on PARP-1/AIF...
April 11, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28388401/parp-inhibitors-for-cancer-therapy
#8
Ken Y Lin, W Lee Kraus
Rucaparib is an inhibitor of nuclear poly (ADP-ribose) polymerases (inhibition of PARP-1 > PARP-2 > PARP-3), following a similar drug, Olaparib. It disrupts DNA repair and replication pathways (and possibly transcription), leading to selective killing of cancer cells with BRCA1/2 mutations. Rucaparib is approved for recurrent ovarian cancers with germline or somatic mutations in BRCA1/2.
April 6, 2017: Cell
https://www.readbyqxmd.com/read/28384634/poly-adp-ribose-polymerase-1-promotes-prothrombin-gene-transcription-and-produces-des-gamma-carboxy-prothrombin-in-hepatocellular-carcinoma
#9
Tatsuya Taniguchi, Kazuhiro Kishi, Tadahiko Nakagawa, Hironori Tanaka, Takahiro Tanaka, Tetsu Tomonari, Koichi Okamoto, Masahiro Sogabe, Hiroshi Miyamoto, Toshiya Okahisa, Naoki Muguruma, Mayumi Kajimoto, Ikuko Sagawa, Tetsuji Takayama
BACKGROUND AND AIM: Although des-gamma-carboxy prothrombin (DCP) is a well-known tumor marker for hepatocellular carcinoma (HCC), the mechanism of DCP production is unclear. This study aimed to investigate the mechanism how DCP is produced in HCC cells. METHODS: Levels of mRNA and DCP were analyzed by real-time polymerase chain reaction and electro-chemiluminescence immunoassay respectively. Secreted alkaline phosphatase (SEAP) expression vectors including deletion mutants of the prothrombin gene promoter were constructed for reporter gene assay...
April 7, 2017: Digestion
https://www.readbyqxmd.com/read/28373419/antitumor-activities-of-the-novel-isosteviol-derivative-10c-against-liver-cancer
#10
Ahmed Malki, Ahmed El-Sharkawy, Mohamed El Syaed, Stephen Bergmeier
BACKGROUND/AIM: Hepatocellular carcinoma (HCC) is the most common type of liver cancer and the fifth most common primary malignancy with worldwide increasing incidence. The current study aimed to investigate the anticancer activities of novel isosteviol derivatives towards human HepG2 hepatocellular cancer cells and in an animal model of hepatocellular carcinoma. MATERIALS AND METHODS: Twelve isosteviol derivatives were screened for their anti-proliferative activities against HepG2 and IC50 was calculated for all designed derivatives...
April 2017: Anticancer Research
https://www.readbyqxmd.com/read/28370165/neuroprotective-effects-of-a-novel-poly-adp-ribose-polymerase-1-inhibitor-jpi-289-in-hypoxic-rat-cortical-neurons
#11
Youngchul Kim, Young Seo Kim, Min-Young Noh, Hanchang Lee, Boyoung Joe, Hyun Young Kim, Jeongmin Kim, Seung Hyun Kim, Jiseon Park
Excessive activation of Poly (ADP-ribose) polymerase-1 (PARP-1) is known to develop neuronal apoptosis, necrosis and inflammation after ischemic brain injury. Therefore, PARP-1 inhibition after ischemic stroke has been attemptedin successful animal studies. The purpose of present work was to develop a novel water soluble PARP-1 inhibitor (JPI-289) and explore its neuroprotective effect on ischemic injury in an in vitro model. The half-life of JPI-289 after Intravenous or oral administration in rats was relatively long (1...
April 2, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/28356011/thymol-elicits-hct-116-colorectal-carcinoma-cell-death-through-induction-of-oxidative-stress
#12
Anil Kumar Chauhan, Ashutosh Bahuguna, Souren Paul, Sun Chul Kang
Colon cancer is one of the most deadly and common carcinomas occurring worldwide, and there have been many attempts to treat this cancer. The present work was designed in order to evaluate thymol as a potent drug against colon cancer. Cytotoxicity of thymol at different concentrations was evaluated against a human colon carcinoma cell line (HCT-116 cells). Fluorescent staining was carried out to evaluate the level of ROS as well as mitochondrial and DNA fragmentation and immunoblot analysis were performed to confirm apoptosis and mitoptosis...
March 27, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28350112/contribution-of-caspase-independent-pathway-to-apoptosis-in-malignant-glioma-induced-by-carbon-ion-beams
#13
Luwei Zhang, Jiawei Yan, Yang Liu, Qiuyue Zhao, Cuixia Di, Sun Chao, Li Jie, Yuanyuan Liu, Hong Zhang
High linear energy transfer (LET) carbon ion beam (CIB) is becoming the best tool for external radiotherapy of inoperable tumors because of its greater cell killing than conventional low LET gamma or X-rays. In the present study, whether the caspase-independent pathway exerts the important contribution in CIB-induced cell apoptosis was explored. Herein we showed, despite the absence of caspase activity using a pan caspase inhibitor Z-VAD-FMK, that apoptosis induced by high LET CIB were clearly observed in the glioma cells...
March 24, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28348416/cannabinoid-cb2-receptors-are-involved-in-the-protection-of-raw264-7-macrophages-against-the-oxidative-stress-an-in-vitro-study
#14
Sabrina Giacoppo, Agnese Gugliandolo, Oriana Trubiani, Federica Pollastro, Gianpaolo Grassi, Placido Bramanti, Emanuela Mazzon
Research in the last decades has widely investigated the anti-oxidant properties of natural products as a therapeutic approach for the prevention and the treatment of oxidative-stress related disorders. In this context, several studies were aimed to evaluate the therapeutic potential of phytocannabinoids, the bioactive compounds of Cannabis sativa. Here, we examined the anti-oxidant ability of Cannabigerol (CBG), a non-psychotropic cannabinoid, still little known, into counteracting the hydrogen peroxide (H2O2)-induced oxidative stress in murine RAW264...
January 23, 2017: European Journal of Histochemistry: EJH
https://www.readbyqxmd.com/read/28341135/methamphetamine-induces-hepatotoxicity-via-inhibiting-cell-division-arresting-cell-cycle-and-activating-apoptosis-in%C3%A2-vivo-and-in%C3%A2-vitro-studies
#15
Qi Wang, Li-Wen Wei, Huan-Qin Xiao, Ye Xue, Si-Hao Du, Yun-Gang Liu, Xiao-Li Xie
Methamphetamine (METH) resulted in acute hepatic injury. However, the underlying mechanisms have not been fully clarified. In the present study, rats were treated with METH (15 mg/kg B.W.) for 8 injections (i.p.), and the levels of alanine transaminase, asparatate transaminase and ammonia in serum were significantly elevated over those in the control group, suggesting hepatic injury, which was evidenced by histopathological observation. Analysis of the liver tissues with microarray revealed differential expressions of a total of 332 genes in METH-treated rats...
March 21, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28340412/discovery-of-2-substituted-1h-benzo-d-immidazole-4-carboxamide-derivatives-as-novel-poly-adp-ribose-polymerase-1-inhibitors-with-in%C3%A2-vivo-anti-tumor-activity
#16
Jie Zhou, Ming Ji, Zhixiang Zhu, Ran Cao, Xiaoguang Chen, Bailing Xu
Novel 1H-benzo[d]immidazole-4-carboxamide derivatives bearing five-membered or six-membered N-heterocyclic moieties at the 2-position were designed and synthesized as PARP-1 inhibitors. Structure-activity relationships were conducted and led to a number of potent PARP-1 inhibitors having IC50 values in the single or double digit nanomolar level. Some potent PARP-1 inhibitors also had similar inhibitory activities against PARP-2. Among all the synthesized compounds, compound 10a and 11e displayed strong potentiation effects on temozolomide (TMZ) in MX-1 cells (PF50 = 7...
March 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28339485/chronic-parp-1-inhibition-reduces-carotid-vessel-remodeling-and-oxidative-damage-of-the-dorsal-hippocampus-in-spontaneously-hypertensive-rats
#17
Krisztian Eros, Klara Magyar, Laszlo Deres, Arpad Skazel, Adam Riba, Zoltan Vamos, Tamas Kalai, Ferenc Gallyas, Balazs Sumegi, Kalman Toth, Robert Halmosi
Vascular remodeling during chronic hypertension may impair the supply of tissues with oxygen, glucose and other compounds, potentially unleashing deleterious effects. In this study, we used Spontaneously Hypertensive Rats and normotensive Wistar-Kyoto rats with or without pharmacological inhibition of poly(ADP-ribose)polymerase-1 by an experimental compound L-2286, to evaluate carotid artery remodeling and consequent damage of neuronal tissue during hypertension. We observed elevated oxidative stress and profound thickening of the vascular wall with fibrotic tissue accumulation induced by elevated blood pressure...
2017: PloS One
https://www.readbyqxmd.com/read/28322842/simultaneous-blockade-of-nmda-receptors-and-parp-1-activity-synergistically-alleviate-immunoexcitotoxicity-and-bioenergetics-in-3-nitropropionic-acid-intoxicated-mice-evidences-from-memantine-and-3-aminobenzamide-interventions
#18
Saravana Babu Chidambaram, Ranju Vijayan, Sathiya Sekar, Sugumar Mani, Barathidsan Rajamani, Ramakrishnan Ganapathy
Interlink between excitotoxicity and cellular bioenergetics depletion is implicated as one of the central deteriorative pathways in many neurodegenerative diseases including Huntington's disease (HD). Chronic administration of 3-nitropropionic acid (3-NP) depletes ATP and NAD(+;) and increases TNFα, IL-6 and glutamate content resulting in "immunoexcitotoxicity". Present study was designed to determine whether the combination of memantine (MN) and 3-aminobenzamide (3-AB), PARP inhibitor, can ameliorate immunoexcitotoxicity and improve bioenergetics in a better manner than individual administration against 3-NP intoxication in mice...
May 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28322340/signalling-mechanisms-mediating-zn-2-induced-trpm2-channel-activation-and-cell-death-in-microglial-cells
#19
Sharifah Syed Mortadza, Joan A Sim, Martin Stacey, Lin-Hua Jiang
Excessive Zn(2+) causes brain damage via promoting ROS generation. Here we investigated the role of ROS-sensitive TRPM2 channel in H2O2/Zn(2+)-induced Ca(2+) signalling and cell death in microglial cells. H2O2/Zn(2+) induced concentration-dependent increases in cytosolic Ca(2+) concentration ([Ca(2+)]c), which was inhibited by PJ34, a PARP inhibitor, and abolished by TRPM2 knockout (TRPM2-KO). Pathological concentrations of H2O2/Zn(2+) induced substantial cell death that was inhibited by PJ34 and DPQ, PARP inhibitors, 2-APB, a TRPM2 channel inhibitor, and prevented by TRPM2-KO...
March 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28321485/initial-autophagic-protection-switches-to-disruption-of-autophagic-flux-by-lysosomal-instability-during-cadmium-stress-accrual-in-renal-nrk-52e-cells
#20
W-K Lee, S Probst, M P Santoyo-Sánchez, W Al-Hamdani, I Diebels, J-K von Sivers, E Kerek, E J Prenner, F Thévenod
The renal proximal tubule (PT) is the major target of cadmium (Cd(2+)) toxicity where Cd(2+) causes stress and apoptosis. Autophagy is induced by cell stress, e.g., endoplasmic reticulum (ER) stress, and may contribute to cell survival or death. The role of autophagy in Cd(2+)-induced nephrotoxicity remains unsettled due to contradictory results and lack of evidence for autophagic machinery damage by Cd(2+). Cd(2+)-induced autophagy in rat kidney PT cell line NRK-52E and its role in cell death was investigated...
March 20, 2017: Archives of Toxicology
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