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https://www.readbyqxmd.com/read/29156708/a-preclinical-evaluation-of-the-mek-inhibitor-refametinib-in-her2-positive-breast-cancer-cell-lines-including-those-with-acquired-resistance-to-trastuzumab-or-lapatinib
#1
John O'Shea, Mattia Cremona, Clare Morgan, Malgorzata Milewska, Frankie Holmes, Virginia Espina, Lance Liotta, Joyce O'Shaughnessy, Sinead Toomey, Stephen F Madden, Aoife Carr, Naomi Elster, Bryan T Hennessy, Alex J Eustace
Purpose: The MEK/MAPK pathway is commonly activated in HER2-positive breast cancer, but little investigation of targeting this pathway has been undertaken. Here we present the results of an in vitro preclinical evaluation of refametinib, an allosteric MEK1/2 inhibitor, in HER2-positive breast cancer cell lines including models of acquired resistance to trastuzumab or lapatinib. Methods: A panel of HER2-positive breast cancer cells were profiled for mutational status and also for anti-proliferative response to refametinib alone and in combination with the PI3K inhibitor (PI3Ki) copanlisib and the HER2-targeted therapies trastuzumab and lapatinib...
October 17, 2017: Oncotarget
https://www.readbyqxmd.com/read/29156703/preclinical-efficacy-of-the-novel-competitive-nampt-inhibitor-stf-118804-in-pancreatic-cancer
#2
Jair Machado Espindola-Netto, Claudia C S Chini, Mariana Tarragó, Enfeng Wang, Shamit Dutta, Krishnendu Pal, Debabrata Mukhopadhyay, Mauro Sola-Penna, Eduardo N Chini
NAD salvage is one of the pathways used to generate NAD in mammals. Nicotinamide phosphoribosyltransferase (NAMPT), the rate-limiting enzyme in this pathway, uses nicotinamide (NAM) to generate nicotinamide mononucleotide (NMN). NMN is one of the main precursors of NAD synthesis in cells. Our previous study showed the importance of NAMPT in maintaining NAD levels in pancreatic ductal adenocarcinoma cells (PDAC), and that the NAMPT inhibitor FK866 decreased pancreatic cancer growth. We now tested the effect of STF-118804, a new highly specific NAMPT inhibitor, in models of pancreatic ductal adenocarcinoma...
October 17, 2017: Oncotarget
https://www.readbyqxmd.com/read/29156682/pharmacologic-inhibition-of-pi3k-p110%C3%AE-in-mutant-shp2e76k-expressing-mice
#3
Lisa Deng, Elizabeth L Virts, Reuben Kapur, Rebecca J Chan
Juvenile myelomonocytic leukemia is a childhood malignancy that lacks effective chemotherapies and thus has poor patient outcomes. PI3K p110δ has been found to promote hyperproliferation of cells expressing mutant Shp2. In this study, we tested the efficacy of a PI3Kδ inhibitor in mice expressing the Shp2 gain-of-function mutation, E76K. We found that in vivo treatment of mice led to significantly decreased splenomegaly, reduced frequency of bone marrow progenitor cells, and increased terminally differentiated peripheral blood myeloid cells...
October 17, 2017: Oncotarget
https://www.readbyqxmd.com/read/29156646/inhibition-of-bcl-2-and-cox-2-protein-expression-after-local-application-of-a-new-carmustine-loaded-clinoptilolite-based-delivery-system-in-a-chemically-induced-skin-cancer-model-in-mice
#4
Cristina Mihaela Ghiciuc, Aurel Lulu Strat, Lacramioara Ochiuz, Catalina Elena Lupusoru, Maria Ignat, Aurelia Vasile, Alexandru Grigorovici, Iulian Stoleriu, Carmen Solcan
Our research has focused on in vitro and in vivo evaluations of a new Carmustine (BCNU)-loaded clinoptilolite-based delivery system. Two clinoptilolite ionic forms-hydrogen form (HCLI) and sodium form (NaCLI)-were prepared, allowing a loading degree of about 5-6 mg BCNU/g of zeolite matrix due to the dual porous feature of clinoptilolite. Clinoptilolite-based delivery systems released 35.23% of the load in 12 h for the BCNU@HCLI system and only 10.82% for the BCNU@NaCLI system. The BCNU@HCLI system was chosen to develop gel and cream semisolid dosage forms...
November 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29156624/evaluation-of-posaconazole-pharmacokinetics-in-adult-patients-with-invasive-fungal-infection
#5
Sarah Allegra, Giovanna Fatiguso, Silvia De Francia, Fabio Favata, Elisa Pirro, Chiara Carcieri, Amedeo De Nicolò, Jessica Cusato, Giovanni Di Perri, Antonio D'Avolio
Mortality and morbidity due to invasive fungal infections have increased over the years. Posaconazole is a second-generation triazole agent with an extended spectrum of activity, which shows a high interindividual variability in its plasma levels, rendering dosing in many patients inconsistent or inadequate. Hence, posaconazole therapeutic drug monitoring, which is easily available in clinical practice, may improve treatment success and safety. The aim of the study was to describe posaconazole pharmacokinetics, and to evaluate the utility of therapeutic drug monitoring for therapy and prophylaxis in a cohort of adult patients...
November 20, 2017: Biomedicines
https://www.readbyqxmd.com/read/29156613/synthesis-and-swelling-behavior-of-ph-sensitive-semi-ipn-superabsorbent-hydrogels-based-on-poly-acrylic-acid-reinforced-with-cellulose-nanocrystals
#6
Lim Sze Lim, Noor Afizah Rosli, Ishak Ahmad, Azwan Mat Lazim, Mohd Cairul Iqbal Mohd Amin
pH-sensitive poly(acrylic acid) (PAA) hydrogel reinforced with cellulose nanocrystals (CNC) was prepared. Acrylic acid (AA) was subjected to chemical cross-linking using the cross-linking agent MBA (N,N-methylenebisacrylamide) with CNC entrapped in the PAA matrix. The quantity of CNC was varied between 0, 5, 10, 15, 20, and 25 wt %. X-ray diffraction (XRD) data showed an increase in crystallinity with the addition of CNC, while rheology tests demonstrated a significant increase in the storage modulus of the hydrogel with an increase in CNC content...
November 20, 2017: Nanomaterials
https://www.readbyqxmd.com/read/29156531/heated-naringin-mitigate-the-genotoxicity-effect-of-mitomycin-c-in-balb-c-mice-through-enhancing-the-antioxidant-status
#7
Mouna Maatouk, Nadia Mustapha, Imen Mokdad-Bzeouich, Hind Chaaban, Irina Ioannou, Kamel Ghedira, Mohamed Ghoul, Leila Chekir-Ghedira
A major problem with cancer chemotherapy is its severe toxic effects on non-target tissues. Assessment of natural products for their protective effect against anticancer drugs induced toxicity is gaining importance in cancer biology. The aim of the present study was to evaluate the effect of native and thermal treated naringin on the protective effect against mitomycin C (MMC) induced genotoxicity. The genotoxicity in liver kidney and brain cells isolated from Balb/C mice were evaluated by performing the comet assay...
November 15, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29156492/bayesian-monotonic-errors-in-variables-models-with-applications-to-pathogen-susceptibility-testing
#8
Glen DePalma, Bruce A Craig
Drug dilution (MIC) and disk diffusion (DIA) are the 2 most common antimicrobial susceptibility assays used by hospitals and clinics to determine an unknown pathogen's susceptibility to various antibiotics. Since only one assay is commonly used, it is important that the 2 assays give similar results. Calibration of the DIA assay to the MIC assay is typically done using the error-rate bounded method, which selects DIA breakpoints that minimize the observed discrepancies between the 2 assays. In 2000, Craig proposed a model-based approach that specifically models the measurement error and rounding processes of each assay, the underlying pathogen distribution, and the true monotonic relationship between the 2 assays...
November 20, 2017: Statistics in Medicine
https://www.readbyqxmd.com/read/29156432/the-effects-of-human-drugs-in-corbicula-fluminea-assessment-of-neurotoxicity-inflammation-gametogenic-activity-and-energy-status
#9
G V Aguirre-Martínez, C André, F Gagné, L M Martín-Díaz
The constant release of pharmaceuticals products to aquatic environment even at low concentrations (ng L(-1) to µg L(-1)) could lead to unknown chronic effects to non-target organisms. The aim of this study was to evaluate neurotoxic responses, inflammation, gametogenic activity and energy status on the fresh water clam C. fluminea after exposure to different concentrations of caffeine (CAF), ibuprofen (IBU), carbamazepine (CBZ), novobiocin (NOV) and tamoxifen (TMX) for 21 days under laboratory conditions...
November 17, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29156382/discovery-of-selective-dengue-virus-inhibitors-using-combination-of-molecular-fingerprint-based-virtual-screening-protocols-structure-based-pharmacophore-model-development-molecular-dynamics-simulations-and-in-vitro-studies
#10
Shaher Bano Mirza, Regina Ching Hua Lee, Justin Jang Hann Chu, Ramin Ekhteiari Salmas, Thomas Mavromoustakos, Serdar Durdagi
Dengue virus is a major issue of tropical and sub-tropical regions. The proliferation of virus results in immense number of deaths each year because of unavailability of on-shelf drugs. This issue necessitates the design of novel anti-Dengue drugs. The protease enzyme pathway is the critical target for drug design due to its significance in the replication, survival and other cellular activities of Dengue virus. Keeping in mind the worsening situation regarding Dengue virus, approximately eighteen million drug-like compounds from the ZINC small molecule database have been screened against Nonstructural Protein 3 (NS3) previously by our group...
October 24, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/29156349/biopolymer-gelatin-coated-zinc-oxide-nanoparticles-showed-high-antibacterial-antibiofilm-and-anti-angiogenic-activity
#11
Mani Divya, Baskaralingam Vaseeharan, Muthukumar Abinaya, Sekar Vijayakumar, Marimuthu Govindarajan, Naiyf S Alharbi, Shine Kadaikunnan, Jamal M Khaled, Giovanni Benelli
The use of natural polymers in drug design plays an important role in biomedical applications. Combinations of nanoparticles (NPs) and biopolymers have been shown to be useful for many purposes. This study focused on gelatin-coated zinc oxide NPs synthesized by co-precipitation. The particles were characterized by UV-Vis spectrum, showing a main peak at 375nm. The stability and crystalline nature of the particles was evaluated by Zeta potential and X-ray diffraction analysis. Fourier transform infrared spectroscopy (FTIR) revealed the possible functional groups of Ge-ZnO NPs, with strong bands at 3851, 3447, and 2923cm(-1)...
November 10, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/29156348/development-of-photoprotective-antiphototoxic-and-antiphotogenotoxic-formulations-of-ocular-drugs-with-fluoroquinolones
#12
Anna Zgadzaj, Joanna Kornacka, Anita Jastrzębska, Andrzej Parzonko, Sylwester Sommer, Grzegorz Nałęcz-Jawecki
The development of innovative solutions in photosafety of photolabile pharmaceutical products may help to reduce the adverse effects of these products, caused by light exposure. Providing new data in this area of study is particularly important in case of drugs applied topically on sensitive organs such as eyes. The main goal of this research is to investigate whether two potential excipients, namely: p-coumaric acid and benzophenone-4, affect the photodegradation, phototoxicity and photogenotoxicity of water solutions of four fluoroquinolones: ciprofloxacin, lomefloxacin, fleroxacin and clinafloxacin...
November 9, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/29156244/isolation-and-characterization-of-polyvalent-bacteriophages-infecting-multi-drug-resistant-salmonella-serovars-isolated-from-broilers-in-egypt
#13
Mayada Mahmoud, Ahmed Askora, Ahmed Barakat Barakat, Omar El-Farouk Rabie, Sayed Emam Hassan
In this study, we isolated and characterized three phages named as Salmacey1, Salmacey2 and Salmacey3, infecting multi drug resistant Salmonella serovars isolated from broilers in Egypt. The most prevalent Salmonella serovars were S. typhimurium, S. enteritidis, and S. kentucky. All these Salmonella serovars were found to be resistant to more than two of the ten antimicrobial agents tested. Only S. kentucky was found to be resistant to seven antimicrobial agents. Examination of these phage particles by transmission electron microscopy (TEM), demonstrated that two phages (Salmacey1, Salmacey2) were found to belong to family Siphoviridae, and Salmacey3 was assigned to the family Myoviridae...
November 14, 2017: International Journal of Food Microbiology
https://www.readbyqxmd.com/read/29156151/limited-evidence-of-fungicide-driven-triazole-resistant-i-aspergillus-fumigatus-i-in-hamilton-canada
#14
Eta Ashu, Ga Young Kim, Patrick Roy-Gayos, Kelly Dong, Adrian Forsythe, Victoria Giglio, Gregory Korfanty, Deborah Yamamura, Jianping Xu
Aspergillus fumigatus is a ubiquitous opportunistic fungal pathogen that can cause aspergillosis in humans. Over the last decade there have been increasing global reports of treatment failure due to triazole resistance. An emerging hypothesis states that agricultural triazole fungicide use causes clinical triazole-resistance. Here we test this hypothesis in Hamilton, Ontario, Canada by examining a total of 195 agricultural, urban and clinical isolates using 9 highly polymorphic microsatellite markers. For each isolate, the in vitro susceptibilities to itraconazole and voriconazole, two triazole drugs commonly used in the management of patients, were also determined...
November 20, 2017: Canadian Journal of Microbiology
https://www.readbyqxmd.com/read/29156123/a-nanopore-based-label-free-and-real-time-monitoring-assay-for-dna-methyltransferase-activity-and-inhibition
#15
Sana Rauf, Ling Zhang, Asghar Ali, Jalal Ahmad, Yang Liu, Jinghong Li
DNA methylation catalyzed by DNA methyltransferase plays an important role in many biological processes. However, conventional assays proposed for DNA methyltransferase activity are laborious and discontinuous. We describe a novel method for real-time monitoring of the activity and kinetics of Escherichia coli DNA adenine methyltransferase (Dam), using nanopore technique coupled with enzyme-linkage reactions. A double-stranded DNA probe AB having a recognition sequence 5'-GATC-3' for both Dam and MboI restriction endonuclease was prepared...
November 20, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/29156121/the-toxmatrix-chemo-genomic-profiling-identifies-interactions-that-reveal-mechanisms-of-toxicity
#16
Zhi-Bin Tong, Ruili Huang, Yuhong Wang, Carleen Klumpp-Thomas, John Braisted, Zina Itkin, Paul Shinn, Menghang Xia, Anton Simeonov, David Gerhold
A chemical genomics 'Toxmatrix' method was developed to elucidate mechanisms of cytotoxicity using neuronal models. Quantitative high-throughput screening (qHTS) was applied to systematically screen each toxicant against a panel of 70 modulators, drugs or chemicals that act on a known target, to identify interactions that either protect or sensitize cells to each toxicant. Thirty-two toxicants were tested at 10 concentrations for cytotoxicity to SH-SY5Y human neuroblastoma cells, with results fitted to the Hill equation to determine an IC50 for each toxicant...
November 20, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/29156068/lmwf-5a-for-the-treatment-of-severe-osteoarthritis-of-the-knee-integrated-analysis-of-safety-and-efficacy
#17
Brian Cole, Brian McGrath, Kristin Salottolo, David Bar-Or
The low-molecular-weight fraction of 5% human serum albumin (LMWF-5A) is being developed to treat the signs and symptoms of severe osteoarthritis of the knee. This study was a post hoc pooled analysis of 3 randomized placebo-controlled trials of a single intra-articular injection of LMWF-5A, focusing on the subset of patients with severe osteoarthritis of the knee (Kellgren-Lawrence grade 4). Patients were randomized 1:1 to receive a single 4-mL intra-articular knee injection of either LMWF-5A or saline. Safety was assessed as the incidence and severity of adverse events...
November 20, 2017: Orthopedics
https://www.readbyqxmd.com/read/29155836/genetic-variation-in-dip5-an-amino-acid-permease-and-pdr5-a-multiple-drug-transporter-regulates-glyphosate-resistance-in-s-cerevisiae
#18
Xiaoqing Rong-Mullins, Apoorva Ravishankar, Kirsten A McNeal, Zachery R Lonergan, Audrey C Biega, J Philip Creamer, Jennifer E G Gallagher
S. cerevisiae from different environments are subject to a wide range of selective pressures, whether intentional or by happenstance. Chemicals classified by their application, such as herbicides, fungicides and antibiotics, can affect non-target organisms. First marketed as RoundUp™, glyphosate is the most widely used herbicide. In plants, glyphosate inhibits EPSPS, of the shikimate pathway, which is present in many organisms but lacking in mammals. The shikimate pathway produces chorismate which is the precursor to all the aromatic amino acids, para-aminobenzoic acid, and Coenzyme Q10...
2017: PloS One
https://www.readbyqxmd.com/read/29155831/prevalence-and-risk-factors-associated-with-leishmania-infection-in-trang-province-southern-thailand
#19
Jipada Manomat, Saovanee Leelayoova, Lertwut Bualert, Peerapan Tan-Ariya, Suradej Siripattanapipong, Mathirut Mungthin, Tawee Naaglor, Phunlerd Piyaraj
BACKGROUND: Autochthonous cutaneous and visceral leishmaniasis (VL) caused by Leishmania martiniquensis and Leishmania siamensis have been considered emerging infectious diseases in Thailand. The disease burden is significantly underestimated, especially the prevalence of Leishmania infection among HIV-positive patients. METHODS: A cross-sectional study was conducted to determine the prevalence and risk factors associated with Leishmania infection among patients with HIV/AIDS living in Trang province, southern Thailand, between 2015 and 2016...
November 20, 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/29155559/crafting-of-neuroprotective-octapeptide-from-taxol-binding-pocket-of-%C3%AE-tubulin
#20
Prasenjit Mondal, Gaurav Das, Juhee Khan, Krishnangsu Pradhan, Surajit Ghosh
Microtubules play crucial role in maintaining the shape and function of neurons. During progression of Alzheimer's disease (AD), severe destabilization of microtubule occurs, which leads to the permanent disruption of signal transduction process and memory loss. Thus, microtubule stabilization is one of the key requirements for the treatment of AD. Taxol, a microtubule stabilizing anti-cancer drug has been considered as potential anti-AD drug but never tested in AD patients, likely because of its' toxic nature and poor brain exposure...
November 20, 2017: ACS Chemical Neuroscience
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