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Brac1, 2

Leilei Fu, Shuya Wang, Xuan Wang, Peiqi Wang, Yaxin Zheng, Dahong Yao, Mingrui Guo, Lan Zhang, Liang Ouyang
Poly (ADP-ribose) polymerase-1 (PARP1) is a highly conserved enzyme focused on the self-repair of cellular DNA damage. Until now, numbers of PARP inhibitors have been reported and used for breast cancer therapy in recent years, especially in TNBC. However, developing a new type PARP inhibitor with distinctive skeleton is alternatively promising strategy for TNBC therapy. In this study, based on co-crystallization studies and pharmacophore-docking-based virtual screening, we discovered a series of dihydrodibenzo[b,e]-oxepin compounds as PARP1 inhibitors...
December 2016: Scientific Reports
Y Han, D P Yu, S J Zhou, X Y Song, Y S Li, N Xiao, Z D Liu, X J Sun, Q Y Zhao, S K Liu
More than 40 oncogenes associated with non-small cell lung cancer (NSCLC) have been identified with varied gene expression. The correlations between specific clinical characteristics and oncogene expression in NSCLC patients were examined. From October 2011 to September 2012, a total of 60 patients with NSCLC (male:female, 34:24; mean age, 59.5 ± 10.6 years; age range, 31-81 years) were diagnosed and evaluated for treatment with radical resection at a single facility. Eligible patients exhibiting tumor node metastasis (TNM) stage I-III NSCLC confirmed by post-surgical pathology were included...
2014: Genetics and Molecular Research: GMR
Lauris Gastaud, Esma Saâda-Bouzid, Valérie Le Morvan, Philippe Pourquier, Antoine Ianessi, Juliette Thariat, Antoine Italiano, Antoine Thyss
BACKGROUND: Treatment of osteosarcoma of the extremities consists of surgical resection preceded and followed by chemotherapy, including high-dose methotrexate or adriamycin-based protocols. When distant relapse occurs, therapeutic options are scarce. Trabectedin, a DNA-binding agent, is indicated for the treatment of patients with advanced soft tissue sarcomas after failure of anthracyclines and ifosfamide. In this indication, the 6-month progression-free survival is about 35-40%. Recent reports showed that some specific single nucleotide polymorphisms (SNPs) from DNA repair genes could be associated with sensitivity to trabectedin in soft tissue sarcomas...
2013: Onkologie
Yu-Jun He, Rui-Huan Liu, Cheng-Qing Ning, Nie-Fang Yu
The poly(ADP-ribose) polymerases (PARPs) is an important group of enzymes in DNA repair pathways, especially the base excision repair (BER) for DNA single-strand breaks (SSBs) repair. Inhibition of PARP in DNA repair-defective tumors (like those with BRAC1/2 mutations) can lead to cell death and genomic instability, what is so called "synthetic lethality". Currently, PARP inhibitors combined with cytotoxic chemotherapeutic agents in the treatment of BRCA-1/2 deficient cancers are in the clinical development...
May 2013: Yao Xue Xue Bao, Acta Pharmaceutica Sinica
M J Campbell, G S Reddy, H P Koeffler
The seco-steroid hormone, 1 alpha, 25 dihydroxyvitamin D3 (1 alpha,25(OH)2D3) binds to a specific nuclear receptor that acts as a ligand-inducible transcription factor. The resulting genomic effects include partial arrest in G0/G1 of the cell cycle and induction of differentiation; these effects have been observed in various types of cancer. Recently, we produced enzymatically the natural 24-oxo metabolites of 1 alpha,25(OH)2D3 and two of its potent synthetic analogs (1 alpha,25-(OH)2-16-ene-D3 and 1 alpha,25-(OH)2-20-epi-D3) using a rat kidney perfusion system...
September 1, 1997: Journal of Cellular Biochemistry
R G Gullberg
Breath alcohol measurements for forensic purposes are typically not made at the time of a driving incident but at some later time. Therefore, the magnitude of variation in breath alcohol concentration (BrAC) following the time of arrest is of concern. The use of roadside preliminary breath test (PBT) instruments can provide data on BrAC closer to the time of a driving incident and allow for comparison with later evidential analysis. This retrospective study evaluates two distributions (N = 968): differences between PBT results and the first evidential breath test (PBT-BrAC1) and differences between two (duplicate) evidential breath alcohol tests (BrAC1-BrAC2)...
July 1991: Journal of Studies on Alcohol
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