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Pazit Shaul et al.
ChemMedChem, 10(9), 1528-1538 (2015-08-04)
Herein we report the synthesis and biological evaluation of symmetric and asymmetric analogues of the DNA intercalating drug mitoxantrone (MTX) in which the side chains of the parent drug were modified through glycosylation or methyl etherification. Several analogues with glycosylated
Michal Cichocki et al.
Molecular and cellular biochemistry, 396(1-2), 221-228 (2014-07-27)
Epidermal growth factor receptor (EGFR) interacting with Stat3 is considered to be an attractive therapeutic target. In the current study, we investigated the effect of resveratrol and its two 4'-methylthio-trans-stilbene derivatives (3-M-4'-MTS; S2) (3,5-DM-4″-MTS; S5) on EGFR and Stat3 activation
Minyi Hu et al.
Archives of biochemistry and biophysics, 579, 55-61 (2015-06-06)
Distribution of intramedullary pressure (ImP) induced bone fluid flow has been suggested to influence the magnitude of mechanotransductory signals within bone. As osteocytes have been suggested as major mechanosensors in bone network, it is still unclear how osteocytes embedded within
Anke Vanderstraeten et al.
Journal of immunotherapy (Hagerstown, Md. : 1997), 38(6), 239-249 (2015-06-08)
Survivin is an antiapoptotic protein, not expressed in terminally differentiated adult tissues, yet overexpressed in several tumors. Therefore, it is an interesting target for immunotherapeutic strategies. In addition to specific overexpression in tumors, tumor survival is mediated by survivin and
Morten P Oksvold et al.
Experimental hematology, 43(5), 352-363 (2015-02-03)
Dasatinib inhibits B-cell receptor-Abelson murine leukemia viral oncogene homologue 1, Src, and other tyrosine kinases. Few studies have addressed the impact of dasatinib on normal blood cells, especially in vivo. Here we show that dasatinib leads to a reduced number
Lisa M Johansen et al.
Science translational medicine, 7(290), 290ra89-290ra89 (2015-06-05)
Currently, no approved therapeutics exist to treat or prevent infections induced by Ebola viruses, and recent events have demonstrated an urgent need for rapid discovery of new treatments. Repurposing approved drugs for emerging infections remains a critical resource for potential
Kenichi Kawano et al.
Journal of molecular biology, 426(14), 2679-2691 (2014-05-13)
When influenza A virus infects host cells, its integral matrix protein M2 forms a proton-selective channel in the viral envelope. Although X-ray crystallography and NMR studies using fragment peptides have suggested that M2 stably forms a tetrameric channel irrespective of
Kay Ka-Wai Li et al.
PloS one, 10(5), e0127910-e0127910 (2015-05-27)
Many facets of the tumor biology of medulloblastoma (MB) have not been fully elucidated. Collapsin response mediator protein 1 (CRMP1) is a member of cytoplasmic family of proteins that regulate the development of central nervous system. Recent studies demonstrated that
Giovane S Galdino et al.
The International journal of neuroscience, 125(10), 765-773 (2014-10-02)
Resistance exercise (RE) is characterized to increase strength, tone, mass, and/or muscular endurance and also for produces many beneficial effects, such as blood pressure and osteoporosis reduction, diabetes mellitus control, and analgesia. However, few studies have investigated endogenous mechanisms involved
Katharina Leitmeyer et al.
BioMed research international, 2015, 925890-925890 (2015-04-29)
Rapamycin is an antifungal agent with immunosuppressive properties. Rapamycin inhibits the mammalian target of rapamycin (mTOR) by blocking the mTOR complex 1 (mTORC1). mTOR is an atypical serine/threonine protein kinase, which controls cell growth, cell proliferation, and cell metabolism. However
Kazunari Nohara et al.
Nutrition & metabolism, 12, 23-23 (2015-06-16)
Ammonia detoxification is essential for physiological well-being, and the urea cycle in liver plays a predominant role in ammonia disposal. Nobiletin (NOB), a natural dietary flavonoid, is known to exhibit various physiological efficacies. In the current study, we investigated a
William F Borschel et al.
The Journal of biological chemistry, 290(44), 26846-26855 (2015-09-16)
Among glutamate-gated channels, NMDA receptors produce currents that subside with unusually slow kinetics, and this feature is essential to the physiology of central excitatory synapses. Relative to the homologous AMPA and kainate receptors, NMDA receptors have additional intersubunit contacts in
Bizunesh M Borena et al.
Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology, 34(4), 1291-1303 (2014-10-04)
Mammal skin plays a pivotal role in several life preserving processes and extensive damage may therefore be life threatening. Physiological skin regeneration is achieved through ongoing somatic stem cell differentiation within the epidermis and the hair follicle. However, in severe
Junhong Guan et al.
Inflammation, 37(4), 1289-1296 (2014-04-01)
Cerebral ischemic preconditioning (IPC), which refers to a transient and noninjurious ischemia is able to induce tolerance against the subsequent lethal ischemia, including ischemic stroke. We have previously reported that bone morphogenic protein-7 (BMP-7) contributes to the neuroprotective effects of
Shuai Wu et al.
Molecules (Basel, Switzerland), 20(10), 18704-18716 (2015-10-27)
Tongmai formula (TMF) is a well-known Chinese medicinal preparation that contains isoflavones as its major bioactive constituents. As traditional Chinese medicines (TCMs) are usually used by oral administration, their fate inside the intestinal lumen, including their biotransformation by human intestinal
Marina A Guvakova et al.
The Biochemical journal, 463(2), 257-270 (2014-07-17)
The Ras-related GTPase Rap1 promotes cell adhesion and migration. Although the significance of Rap1 contribution to cell migration is increasingly being recognized, little is known about the biochemical mechanisms driving this process. In the present study, we discovered a previously
Daniela Michlmayr et al.
Journal of virology, 88(17), 9553-9567 (2014-06-06)
The encephalitic response to viral infection requires local chemokine production and the ensuing recruitment of immune and inflammatory leukocytes. Accordingly, chemokine receptors present themselves as plausible therapeutic targets for drugs aimed at limiting encephalitic responses. However, it remains unclear which
Elise S Demitrack et al.
The EMBO journal, 34(20), 2522-2536 (2015-08-15)
The major signaling pathways regulating gastric stem cells are unknown. Here we report that Notch signaling is essential for homeostasis of LGR5(+) antral stem cells. Pathway inhibition reduced proliferation of gastric stem and progenitor cells, while activation increased proliferation. Notch
Jef Stappaerts et al.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 90, 1-7 (2015-01-17)
The aim of this study was to evaluate the intestinal disposition of abiraterone acetate, an ester prodrug of the anticancer agent abiraterone. Stability of the prodrug and solubility and dissolution characteristics of both abiraterone and abiraterone acetate were monitored in
Profiling of biomarkers for the exposure of polycyclic aromatic hydrocarbons: lamin-A/C isoform 3, poly[ADP-ribose] polymerase 1, and mitochondria copy number are identified as universal biomarkers.
Kim HY, Kim HR, Kang MG, et al.
BioMed Research International, 2014, 605135-605135 (2014)
Bhumsuk Keam et al.
Anticancer research, 35(1), 175-182 (2015-01-01)
The purpose of the present study was to explore the antiproliferative effect of BYL719, a specific inhibitor for phosphatidylinositol 3-kinase (PI3K) p110α, in human head and neck cancer cell lines, as a single agent or in combination with the irreversible
Feng Zhang et al.
ACS nano, 9(4), 4533-4542 (2015-04-01)
Organometal halide perovskites are inexpensive materials with desirable characteristics of color-tunable and narrow-band emissions for lighting and display technology, but they suffer from low photoluminescence quantum yields at low excitation fluencies. Here we developed a ligand-assisted reprecipitation strategy to fabricate
K J Qiu et al.
Acta biomaterialia, 15, 254-265 (2015-01-18)
In this study, the microstructure, mechanical properties, castability, electrochemical behaviors, cytotoxicity and hemocompatibility of Ti-Bi alloys with pure Ti as control were systematically investigated to assess their potential applications in the dental field. The experimental results showed that, except for
Kalpana Rathore et al.
Journal of ethnopharmacology, 155(2), 1171-1176 (2014-07-11)
The plant Diospyros melanoxylon (Roxb) belongs to the family Ebenaceae that is native to India and Sri-lanka. This is a medium-sized tree, reaching a height of 15 m and is well known for its beedi making leaves throughout the world.
Leanne G Ahronian et al.
Cancer discovery, 5(4), 358-367 (2015-02-13)
BRAF mutations occur in approximately 10% of colorectal cancers. Although RAF inhibitor monotherapy is highly effective in BRAF-mutant melanoma, response rates in BRAF-mutant colorectal cancer are poor. Recent clinical trials of combined RAF/EGFR or RAF/MEK inhibition have produced improved efficacy
Patrícia Branco et al.
International journal of food microbiology, 205, 112-118 (2015-04-22)
Saccharomyces cerevisiae produces antimicrobial peptides (AMPs) during alcoholic fermentation that are active against several wine-related yeasts (e.g. Hanseniaspora guilliermondii) and bacteria (e.g. Oenococcus oeni). In the present study, the physiological changes induced by those AMPs on sensitive H. guilliermondii cells
Ayşe Ufuk et al.
Pharmaceutical research, 32(12), 3937-3951 (2015-08-01)
To assess accumulation and lysosomal sequestration of 9 drugs used in respiratory indications (plus imipramine as positive control) in the alveolar macrophage (AM) cell line NR8383. For all drugs, uptake at 5 μM was investigated at 37 and 4°C to delineate
Wei-Lan Yeh et al.
PloS one, 9(6), e98805-e98805 (2014-06-03)
Tamoxifen has long been used and still is the most commonly used endocrine therapy for treatment of both early and advanced estrogen receptor-positive breast cancer in pre- and post-menopause women. Tamoxifen exerts its cytotoxic effect primarily through cytostasis which is
Bo Kyung Lee et al.
Molecular carcinogenesis, 54(5), 351-358 (2013-11-20)
Benzo[a]pyrene-7,8-diol-9,10-epoxide (B[a]PDE), a major metabolite of benzo[a]pyrene, has been reported to function as a human carcinogen. However, the molecular mechanism of how B[a]PDE regulates signaling pathways during tumor promotion remains unclear. In this study, we investigated the effects of B[a]PDE
Isabel Correia et al.
Journal of toxicology and environmental health. Part A, 77(14-16), 916-923 (2014-07-30)
The purpose of this study was to determine the efficacy of naproxen, a nonsteroidal anti-inflammatory drug, on the MG-63 human osteosarcoma cell line. MG-63 cells were exposed to naproxen in a wide range of concentrations of 0.03, 0.05, 0.1, 0.42
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