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https://www.readbyqxmd.com/read/29664094/analysis-of-poly-adp-ribose-polymerase-1-by-enzyme-initiated-auto-parylation-controlled-aggregation-of-hemin-graphene-nanocomposites
#1
Yong Liu, Xiaolin Xu, Haitang Yang, Ensheng Xu, Shuangshuang Wu, Wei Wei, Jin Chen
Poly(ADP-ribose) polymerase-1 (PARP-1) is a highly conserved nuclear enzyme, which binds tightly to damaged DNA and plays a key role in DNA repair, recombination, proliferation, and genomic stability. However, due to the poor electrochemical and optical activity of PARP-1 and its product PAR, only a few studies on its activity detection method have been reported. Herein, we report a simple and sensitive colorimetric strategy to monitor PARP-1 activity based on enzyme-initiated auto-PARylation-controlled aggregation of hemin-graphene nanocomposites (H-GNs)...
April 17, 2018: Analyst
https://www.readbyqxmd.com/read/29664016/the-evolving-landscape-of-predictive-biomarkers-of-response-to-parp-inhibitors
#2
Anish Thomas, Junko Murai, Yves Pommier
Poly(ADP-ribose) polymerase inhibitors (PARPis) are DNA-damaging agents that trap PARP-DNA complexes and interfere with DNA replication. Three PARPis - olaparib, niraparib, and rucaparib - were recently approved by the FDA for the treatment of breast and ovarian cancers. These PARPis, along with 2 others (talazoparib and veliparib), are being evaluated for their potential to treat additional malignancies, including prostate cancers. While lack of PARP-1 confers high resistance to PARPis, it has not been established whether or not the levels of PARP-1 directly correlate with tumor response...
April 16, 2018: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/29648554/discovery-of-quinazoline-2-4-1h-3h-dione-derivatives-as-novel-parp-1-2-inhibitors-design-synthesis-and-their-antitumor-activity
#3
Jie Zhou, Ming Ji, Haiping Yao, Ran Cao, Hailong Zhao, Xiaoyu Wang, Xiaoguang Chen, Bailing Xu
Novel quinazoline-2,4(1H,3H)-dione derivatives bearing a 3-amino pyrrolidine moiety were designed and synthesized as PARP-1/2 inhibitors. Structure-activity relationships were examined which revealed a number of potent PARP-1/2 inhibitors with moderate selectivity toward PARP-1 over PARP-2. These compounds had IC50 values against PARP-1 at the 10-9 M level and against PARP-2 at the 10-8 M level. Among all the synthesized compounds, compounds 10 and 11 displayed strong cytotoxicities which are either used as a single agent or in combination with temozolomide (TMZ) in MX-1 cells (10, IC50 < 3...
April 12, 2018: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/29620161/biotinylation-enhances-the-anticancer-effects-of-15d%C3%A2-pgj2-against-breast-cancer-cells
#4
Christelle Colin, Maxime Meyer, Claudia Cerella, Alexandra Kleinclauss, Gérald Monard, Michel Boisbrun, Marc Diederich, Stéphane Flament, Isabelle Grillier-Vuissoz, Sandra Kuntz
15-Deoxy-∆12,14-prostaglandin J2 (15d‑PGJ2) is a natural agonist of peroxisome proliferator-activated receptor γ (PPARγ) that displays anticancer activity. Various studies have indicated that the effects of 15d‑PGJ2 are due to both PPARγ-dependent and -independent mechanisms. In the present study, we examined the effects of a biotinylated form of 15d‑PGJ2 (b‑15d‑PGJ2) on hormone-dependent MCF‑7 and triple‑negative MDA‑MB‑231 breast cancer cell lines. b‑15d‑PGJ2 inhibited cell proliferation more efficiently than 15d‑PGJ2 or the synthetic PPARγ agonist, efatutazone...
March 28, 2018: International Journal of Oncology
https://www.readbyqxmd.com/read/29618301/2-5-diketopiperazines-a-new-class-of-poly-adp-ribose-polymerase-inhibitors
#5
D K Nilov, K I Yashina, I V Gushchina, A L Zakharenko, M V Sukhanova, O I Lavrik, V K Švedas
We show for the first time that natural 2,5-diketopiperazines (cyclic dipeptides) can suppress the activity of the important anticancer target poly(ADP-ribose)polymerase (PARP). Cyclo(L-Ala-L-Ala) and cyclo(L-Ala-D-Ala) can interact with the key residues of the PARP-1 active site, as demonstrated using docking and molecular dynamics simulations. One of the amide groups of cyclo(L-Ala-L-Ala) and cyclo(L-Ala-D-Ala) forms hydrogen bonds with the Gly863 residue, while the second amide group can form a hydrogen bond with the catalytic residue Glu988, and the side chain can make a hydrophobic contact with Ala898...
February 2018: Biochemistry. Biokhimii︠a︡
https://www.readbyqxmd.com/read/29608885/microrna-223-protects-neonatal-rat-cardiomyocytes-and-h9c2-cells-from-hypoxia-induced-apoptosis-and-excessive-autophagy-via-the-akt-mtor-pathway-by-targeting-parp-1
#6
Xiaoxiao Liu, Yunfei Deng, Yifeng Xu, Wei Jin, Hongli Li
Myocardial infarction (MI), characterized by interruption of blood and oxygen to myocardium, is a common yet fatal cardiovascular event that causes progressive damage to myocardial tissue and eventually leads to heart failure. Previous studies have shown increased expression of microRNA-223 (miR-223) in infarcted myocardial tissues of humans and in rat models of MI. However, the role of miR-223 in cell survival during MI has not been elucidated. Thus, we aimed to investigate whether miR-223 participates in the regulation of cardiac ischemia-induced injury and to elucidate the underlying mechanisms of this process...
March 30, 2018: Journal of Molecular and Cellular Cardiology
https://www.readbyqxmd.com/read/29606854/rucaparib-a-novel-parp-inhibitor-for-brca-advanced-ovarian-cancer
#7
REVIEW
Ilaria Colombo, Stephanie Lheureux, Amit Manulal Oza
Rucaparib is a potent small-molecule inhibitor of poly (ADP-ribose) polymerase (PARP) proteins (PARP-1, PARP-2 and PARP-3) that play an important role in repairing DNA damage and maintaining genomic stability. Tumors with mutations in BRCA1/2 or other homologous recombination deficiency (HRD) genes are particularly sensitive to PARP inhibitors because of "synthetic lethality", whereby a therapeutic agent can take advantage of an intrinsic weakness in DNA repair. Rucaparib has been investigated in several preclinical and clinical studies showing promising activity in BRCA -mutant and BRCA -wild-type epithelial ovarian cancers (EOCs)...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29605737/rucaparib-an-emerging-parp-inhibitor-for-treatment-of-recurrent-ovarian-cancer
#8
REVIEW
Angela Musella, Erlisa Bardhi, Claudia Marchetti, Laura Vertechy, Giusy Santangelo, Carolina Sassu, Federica Tomao, Francesco Rech, Renzo D'Amelio, Marco Monti, Innocenza Palaia, Ludovico Muzii, Pierluigi Benedetti Panici
Recently, Poly-ADP-Ribose Polymerase (PARP) inhibitors are one of the most intensively studied group of antiblastic agents for the management of recurrent ovarian cancer. Among this family, Olaparib was the first to be approved by European Medicines Agency as maintenance therapy post-response to platinum-based chemotherapy for recurrent ovarian cancer in women with deleterious BRCA1/2 mutation. Following that, the Food and Drug Administration (FDA) approved Olaparib monotherapy as fourth or later line of treatment in advanced ovarian cancer with deleterious germ-line BRCA1/2 mutation...
March 23, 2018: Cancer Treatment Reviews
https://www.readbyqxmd.com/read/29605020/targeting-intestinal-epithelial-cell-programmed-necrosis-alleviates-tissue-injury-after-intestinal-ischemia-reperfusion-in-rats
#9
Xiang Li, Yihong Ling, Zhongming Cao, Jiantong Shen, Shaoqian Chen, Weifeng Liu, Baolong Yuan, Shihong Wen
BACKGROUND: Intestinal dysfunction, especially acute pathologies linked to intestinal ischemia/reperfusion (I/R) injury, is profoundly affected by inflammation and improper execution of cell death. Few studies have examined the efficacy of combined strategies in regulated intestinal epithelial necrosis after intestinal I/R. Here, we evaluated the functional interaction between poly (adenosine diphosphate-ribose) polymerase 1 (PARP-1)-induced parthanatos and receptor-interacting protein 1/3 (RIP1/3) kinase-induced necroptosis in the pathophysiological course of acute ischemic intestinal injury...
May 2018: Journal of Surgical Research
https://www.readbyqxmd.com/read/29602037/synthesis-and-anti-mitotic-activity-of-2-4-or-2-6-disubstituted-and-2-4-6-trisubstituted-2h-pyrazolo-4-3-c-pyridines
#10
Vaida Milišiūnaitė, Eglė Arbačiauskienė, Eva Řezníčková, Radek Jorda, Veronika Malínková, Asta Žukauskaitė, Wolfgang Holzer, Algirdas Šačkus, Vladimír Kryštof
An efficient synthetic route for the synthesis of 2H-pyrazolo[4,3-c]pyridines, primarily varying by the substituents at the 2-, 4- and 6-positions, is described here. A Sonogashira-type cross-coupling reaction was employed to yield 3-alkynyl-1H-pyrazole-4-carbaldehydes, ethanones and propanones from the corresponding 1H-pyrazol-3-yl trifluoromethanesulfonates. Subsequent treatment of the coupling products with dry ammonia afforded a versatile library of 2H-pyrazolo[4,3-c]pyridines, which were then evaluated for their cytotoxicity against K562 and MCF-7 cancer cell lines...
March 16, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29592880/trastuzumab-resistant-her2-breast-cancer-cells-retain-sensitivity-to-poly-adp-ribose-polymerase-parp-inhibition
#11
Monica E Wielgos, Zhuo Zhang, Rajani Rajbhandari, Tiffiny S Cooper, Ling Zeng, Andres Forero, Francisco J Esteva, C Kent Osborne, Rachel Schiff, Albert F LoBuglio, Susan E Nozell, Eddy S Yang
HER2-targeted therapies, such as trastuzumab, have increased the survival rates of HER2+ breast cancer patients. However, despite these therapies, many tumors eventually develop resistance to these therapies. Our lab previously reported an unexpected sensitivity of HER2+ breast cancer cells to poly (ADP-Ribose) polymerase inhibitors (PARPi), agents that target homologous recombination (HR) deficient tumors, independent of a DNA repair deficiency. In this study, we investigated whether HER2+ trastuzumab resistant (TR) breast cancer cells were susceptible to PARPi and the mechanism behind PARPi induced cytotoxicity...
March 28, 2018: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/29570944/anticancer-gold-iii-peptidomimetics-from-synthesis-to-in-vitro-and-ex-vivo-biological-evaluation
#12
Giulia Boscutti, Chiara Nardon, Luciano Marchiò, Marco Crisma, Barbara Biondi, Daniele Dalzoppo, Lisa Dalla Via, Fernando Formaggio, Angela Casini, Dolores Fregona
Five new Au(III)-peptidodithiocarbamato complexes of the type [AuIIIBr2(dtc-AA1-AA2-OR] (AA1=Sar, L/D-Pro; AA2=L/D-Ala, Aib; R=OtBu, TEG), differing in the amino acidic sequence and/or the chiral amino acid configuration, were designed to enhance the tumor selectivity and bioavailability. The gold(III)-based moiety was functionalized to exploit the targeting properties of the peptidomimetic ligand towards two peptide transporters (namely, PEPT1 and PEPT2), up-regulated in several tumor cells. The compounds were synthesized and fully characterized, mainly by means of elemental analysis, mono- and bidimensional NMR spectroscopy, FT-IR and UV-Vis spectrophotometries...
March 23, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29548826/bigelovin-a-sesquiterpene-lactone-suppresses-tumor-growth-through-inducing-apoptosis-and-autophagy-via-the-inhibition-of-mtor-pathway-regulated-by-ros-generation-in-liver-cancer
#13
Bei Wang, Shu-Sen Zheng, Tan-Yang Zhou, Chun-Hui Nie, Da-Long Wan
Bigelovin (BigV) is a sesquiterpene lactone, isolated from Inula helianthus aquatica, which has been reported to induce apoptosis and show anti-inflammatory and anti-angiogenic activities. Nevertheless, the effects of BigV on liver cancer and the underlying mechanisms have not been investigated. In the study, we found that BigV exhibited potential anti-tumor activities against human liver cancer in vitro and in vivo. BigV reduced the cell proliferation and colony formation. BigV induced apoptosis through improving the cleavage of Caspase-3 and poly (ADP-ribose) polymerase 1 (PARP-1)...
March 13, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29546393/bufalin-inhibits-human-breast-cancer-tumorigenesis-by-inducing-cell-death-through-the-ros-mediated-rip1-rip3-parp-1-pathways
#14
Yanlan Li, Xiaodan Liu, Pengchao Gong, Xin Tian
Bufalin, a key active ingredient of the Chinese medicine Chan Su, inhibits breast cancer tumorigenesis in vitro and in vivo. Here we found that the pan-caspase inhibitor zVAD-fmk failed to inhibit bufalin-induced cell death in MCF-7 and MDA-MB-231 human breast cancer cells, confirming that the cell death induced by bufalin is caspase-independent. Instead, bufalin increased the expression of the necroptosis mediators RIP1 and RIP3. Bufalin-induced cell death was prevented by small molecule inhibitors of RIP1 and poly (ADP-ribose) polymerase-1 (PARP-1) or genetic knockdown of RIP3 by shRNA transfection...
March 13, 2018: Carcinogenesis
https://www.readbyqxmd.com/read/29545876/jwa-deficiency-induces-malignant-transformation-of-murine-embryonic-fibroblast-cells
#15
Hong Qi, Aiping Li
The present study aimed to investigate the effects of JWA knockout (JWA-/- ) on malignant transformation of murine embryonic fibroblast (MEF) cells using a conditional JWA-/- mouse model. Once MEF cells were prepared, the potential role of JWA-/- on proliferation, migration, invasion and colony formation of MEF cells was investigated by cytological examination. The effects of JWA-/- on the regulation and protein expression levels of epithelial-mesenchymal transition (EMT)-related proteins in MEF cells, including poly(ADP-ribose) polymerase-1 (PARP-1), vimentin, β-catenin and E-cadherin, were investigated using western blot analysis...
April 2018: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/29532444/metabolic-enhancer-piracetam-attenuates-the-translocation-of-mitochondrion-specific-proteins-of-caspase-independent-pathway-poly-adp-ribose-polymerase-1-up-regulation-and-oxidative-dna-fragmentation
#16
Dinesh Kumar Verma, Sonam Gupta, Joyshree Biswas, Neeraj Joshi, K Sivarama Raju, Mu Wahajuddin, Sarika Singh
Piracetam, a nootropic drug, has been clinically used for decades; however, its mechanism of action still remains enigmatic. The present study was undertaken to evaluate the role of mitochondrion-specific factors of caspase-independent pathway like apoptotic-inducing factor (AIF) and endonuclease-G (endo-G) in piracetam-induced neuroprotection. N2A cells treated with lipopolysaccharide (LPS) exhibited significant cytotoxicity, impaired mitochondrial activity, and reactive oxygen species generation which was significantly attenuated with piracetam co-treatment...
March 12, 2018: Neurotoxicity Research
https://www.readbyqxmd.com/read/29514732/erratum
#17
Enrico Mini, Ida Landini, Laura Lucarini, Andrea Lapucci, Cristina Napoli, Gabriele Perrone, Renato Tassi, Emanuela Masini, Flavio Moroni, Stefania Nobili
The poly(ADP-ribose) polymerase (PARP) enzymes play a key role in the regulation of cellular processes (e.g., DNA damage repair, genomic stability). It has been shown that PARP inhibitors (PARPIs) are selectively cytotoxic against cells having dysfunctions in genes involved in DNA repair mechanisms (synthetic lethality). Drug-induced PARP inhibition potentiates the activity of anticancer drugs such as 5-fluorouracil in enhancing DNA damage, whose repair involves PARP-1 activity. The aim of this study was to evaluate the inhibitory effects of a novel PARPI, HYDAMTIQ, on growth in human tumor cell lines characterized by different features with regard to DNA damage response pathways (BRCA mutational status, microsatellite status, and ATM expression level) and degree of sensitivity/resistance to 5-fluorouracil...
March 5, 2018: Oncology Research
https://www.readbyqxmd.com/read/29512738/poly-adp-ribose-polymerase-inhibitor-olaparib-hampers-placental-growth-factor-driven-activation-of-myelomonocytic-cells
#18
Pedro Miguel Lacal, Maria Grazia Atzori, Federica Ruffini, Lucio Tentori, Grazia Graziani
The vascular endothelial growth factor receptor-1 (VEGFR-1) is a tyrosine kinase receptor activated by the angiogenic factors VEGF‑A and placental growth factor (PlGF). While VEGF‑A binds to both VEGFR‑1 and VEGFR‑2, PlGF interacts exclusively with VEGFR‑1 triggering a signaling pathway involved in: i) tumor‑associated angiogenesis; ii) chemotaxis and invasion of the extracellular matrix (ECM) by cancer cells; and iii) mobilization of bone marrow‑derived myeloid cells that generate tumor‑associated macrophages...
March 5, 2018: Oncology Reports
https://www.readbyqxmd.com/read/29511347/parp-1-inhibition-with-or-without-ionizing-radiation-confers-reactive-oxygen-species-mediated-cytotoxicity-preferentially-to-cancer-cells-with-mutant-tp53
#19
Qi Liu, Liliana Gheorghiu, Michael Drumm, Rebecca Clayman, Alec Eidelman, Matthew F Wszolek, Aria Olumi, Adam Feldman, Meng Wang, Lynnette Marcar, Deborah E Citrin, Chin-Lee Wu, Cyril H Benes, Jason A Efstathiou, Henning Willers
Biomarkers and mechanisms of poly (ADP-ribose) polymerase (PARP) inhibitor-mediated cytotoxicity in tumor cells lacking a BRCA-mutant or BRCA-like phenotype are poorly defined. We sought to explore the utility of PARP-1 inhibitor (PARPi) treatment with/without ionizing radiation in muscle-invasive bladder cancer (MIBC), which has poor therapeutic outcomes. We assessed the DNA damaging and cytotoxic effects of the PARPi olaparib in nine bladder cancer cell lines. Olaparib radiosensitized all cell lines with dose enhancement factors from 1...
March 7, 2018: Oncogene
https://www.readbyqxmd.com/read/29509546/a-pet-imaging-agent-for-evaluating-parp-1-expression-in-ovarian-cancer
#20
Mehran Makvandi, Austin Pantel, Lauren Schwartz, Erin Schubert, Kuiying Xu, Chia-Ju Hsieh, Catherine Hou, Hyoung Kim, Chi-Chang Weng, Harrison Winters, Robert Doot, Michael D Farwell, Daniel A Pryma, Roger A Greenberg, David A Mankoff, Fiona Simpkins, Robert H Mach, Lilie L Lin
BACKGROUND: Poly(ADP-ribose) polymerase (PARP) inhibitors are effective in a broad population of ovarian cancer patients, however resistance caused by low enzyme expression of the drug target, poly(ADP-ribose) polymerase 1 (PARP-1), remains to be clinically evaluated in this context. We hypothesize that PARP-1 expression is variable in ovarian cancer and can be quantified in primary and metastatic disease using a novel positron emitting tomography (PET) imaging agent. METHODS: We used a translational approach to describe the significance of PET imaging of PARP-1 in ovarian cancer...
March 6, 2018: Journal of Clinical Investigation
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