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Boris Pinchuk, Thorsten von Drathen, Viktoria Opel, Christian Peifer
Dabrafenib (Tafinlar) was approved in 2013 by the FDA as a selective single agent treatment for patients with BRAF(V600E) mutation-positive advanced melanoma. One year later, a combination of dabrafenib and trametinib was used for treatment of BRAF(V600E/K) mutant metastatic melanoma. In the present study, we report on hitherto not described photosensitivity of dabrafenib both in organic and aqueous media. The half-lives for dabrafenib degradation were determined. Moreover, we revealed photoinduced chemical conversion of dabrafenib to its planar fluorescent derivative dabrafenib_photo 2...
October 13, 2016: ACS Medicinal Chemistry Letters
Abd Elaziz Suliemn Ishag, Azhari Omer Abdelbagi, Ahmed Mohammed Ali Hammad, Elsiddg Ahmed Elmustafa Elsheikh, Osama Elgialani Elsaid, Jang-Hyun Hur, Mark Delmege Laing
This study was done to identify promising pesticide biodegrading microorganisms and characterize degradation rates. Bacillus safensis strain FO-36bT, Bacillus subtilis sub sp. inaquosorum strain KCTC13429T and Bacillus cereus strain ATCC14579T were isolated from pesticides polluted soil in Sudan, incubated with tested pesticides with samples drawn for GC-FID and GC-MS. Biodegradation of pesticides followed biphasic model. Alpha and beta half-lives (days) of chlorpyrifos, malathion and dimethoate in B. safensis culture were; 2...
October 22, 2016: Journal of Agricultural and Food Chemistry
Lei Wu, Hua Feng, Jinhua Hu, Xiangguo Tian, Chunqing Zhang
Due to the low cost and favorable safety profile, valproic acid (VPA) has been considered as a potential candidate drug for therapy of various cancers. Our present study revealed that VPA, at the concentration (1mM) which has no effect on cell proliferation, can significantly increase the in vitro migration and invasion of hepatocarcinoma (HCC) HepG2 and Huh7 cells via induction of epithelial mesenchymal transition (EMT). VPA treatment can significantly increase the mRNA and protein expression of Snail, the key transcription factor of EMT...
October 18, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Alexander N Zelikin, Carsten Ehrhardt, Anne Marie Healy
Biological drugs generated via recombinant techniques are uniquely positioned due to their high potency and high selectivity of action. The major drawback of this class of therapeutics, however, is their poor stability upon oral administration and during subsequent circulation. As a result, biological drugs have very low bioavailability and short therapeutic half-lives. Fortunately, tools of chemistry and biotechnology have been developed into an elaborate arsenal, which can be applied to improve the pharmacokinetics of biological drugs...
October 21, 2016: Nature Chemistry
Jong Min Lee, Soo Young Moon, Yu-Ri Kim, Kang Woong Kim, Bong-Joo Lee, In-Soo Kong
The aim of this study was to improve the stability of β-1,3-1,4-glucanase by substituting hydrophobic residue for specific amino acid. The results indicated that the catalytic efficiency, thermostability and halostability were enhanced simultaneously by replacement of Lys48 with Ala (K48A) or Leu (K48L). Comparison of kinetic parameters revealed that catalytic efficiency of mutants is enhanced as a result of the increase in substrate affinity. A great improvement in thermostability and halostability was observed...
October 17, 2016: International Journal of Biological Macromolecules
R Periáñez, Kyung-Suk Suh, Byung-Il Min
A Lagrangian model which simulates the dispersion of (137)Cs in the North Atlantic has been developed. The model includes water/sediment interactions. It has been tested comparing calculated and measured (137)Cs concentrations in water and sediments of the European Shelf resulting after the releases from the nuclear fuel reprocessing plants of Sellafield and La Hague. Some additional numerical experiments have been carried out. First, the redissolution of (137)Cs from contaminated sediments after the reduction in releases from the reprocessing plants has been studied...
October 17, 2016: Marine Pollution Bulletin
Lobna A Hussein, Noha F El Azab, Maha F Abdel-Ghany
A sensitive, selective, and validated HPLC-diode-array detection method was developed for the simultaneous determination of five neonicotinoid insecticides-acetamiprid, imidacloprid, nitenpyram, flonicamid, and thiacloprid-and their primary metabolite, 6-chloronicotinic acid, in cucumbers and soil based on the quick, easy, cheap, effective, rugged, and safe (QuEChERS) technique as a pretreatment procedure. In the QuEChERS procedure, cucumber samples were extracted with acetonitrile and cleaned using C18, whereas soil samples were extracted with an acetonitrile-dichloromethane mixture (1 + 2)...
October 19, 2016: Journal of AOAC International
Kasper D Tidemand, Hans E M Christensen, Niclas Hoeck, Pernille Harris, Jane Boesen, Günther H Peters
Tryptophan hydroxylase 2 (TPH2) catalyses the initial and rate-limiting step in the biosynthesis of serotonin, which is associated with a variety of disorders such as depression, obsessive compulsive disorder, and schizophrenia. Full-length TPH2 is poorly characterized due to low purification quantities caused by its inherent instability. Three truncated variants of human TPH2 (rch TPH2; regulatory and catalytic domain, NΔ47-rch TPH2; truncation of 47 residues in the N terminus of rch TPH2, and ch TPH2; catalytic domain) were expressed, purified, and examined for changes in transition temperature, inactivation rate, and oligomeric state...
October 2016: FEBS Open Bio
Karen Kerkhof, Vincent Sluydts, Somony Heng, Saorin Kim, Myrthe Pareyn, Laura Willen, Lydie Canier, Siv Sovannaroth, Didier Ménard, Tho Sochantha, Marc Coosemans, Lies Durnez
BACKGROUND: Malaria transmission is highly heterogeneous, especially in low endemic countries, such as Cambodia. This results in geographical clusters of residual transmission in the dry, low transmission season, which can fuel the transmission to wider areas or populations during the wet season. A better understanding of spatial clustering of malaria can lead to a more efficient, targeted strategy to reduce malaria transmission. This study aims to evaluate the potential of the use of serological markers to define spatial patterns in malaria exposure...
October 19, 2016: Malaria Journal
Jiao Ren, Xiaoping Wang, Chuanfei Wang, Ping Gong, Xiruo Wang, Tandong Yao
Biomagnification of some persistent organic pollutants (POPs) has been found in marine and freshwater food chains; however, due to the relatively short food chains in high-altitude alpine lakes, whether trophic transfer would result in the biomagnification of POPs is not clear. The transfer of various POPs, including organochlorine pesticides and polychlorinated biphenyls (PCBs), along the aquatic food chain in Nam Co Lake (4700 m), in the central Tibetan Plateau, was studied. The POPs levels in the water, sediment and biota [plankton, invertebrates and fish (Gymnocypris namensis)] of Nam Co were generally low, with concentrations comparable to those reported for the remote Arctic...
October 14, 2016: Environmental Pollution
Carlos E Rodríguez-Rodríguez, Karina Madrigal-León, Mario Masís-Mora, Marta Pérez-Villanueva, Juan Salvador Chin-Pampillo
The use of fungal bioaugmentation represents a promising way to improve the performance of biomixtures for the elimination of pesticides. The ligninolyitc fungus Trametes versicolor was employed for the removal of three carbamates (aldicarb, ALD; methomyl, MTM; and methiocarb, MTC) in defined liquid medium; in this matrix ALD and MTM showed similar half-lives (14d), nonetheless MTC exhibited a faster removal, with a half-life of 6.5d. Then the fungus was employed in the bioaugmentation of an optimized biomixture to remove the aforementioned carbamates plus carbofuran (CFN)...
October 14, 2016: Ecotoxicology and Environmental Safety
Xiaofeng Zheng, Pengyi Yang, Brad Lackford, Brian D Bennett, Li Wang, Hui Li, Yu Wang, Yiliang Miao, Julie F Foley, David C Fargo, Ying Jin, Carmen J Williams, Raja Jothi, Guang Hu
Poly(A) tail length and mRNA deadenylation play important roles in gene regulation. However, how they regulate embryonic development and pluripotent cell fate is not fully understood. Here we present evidence that CNOT3-dependent mRNA deadenylation governs the pluripotent state. We show that CNOT3, a component of the Ccr4-Not deadenylase complex, is required for mouse epiblast maintenance. It is highly expressed in blastocysts and its deletion leads to peri-implantation lethality. The epiblast cells in Cnot3 deletion embryos are quickly lost during diapause and fail to outgrow in culture...
October 8, 2016: Stem Cell Reports
Devyani Deshpande, Shashikant Srivastava, Eric Nuermberger, Jotam G Pasipanodya, Soumya Swaminathan, Tawanda Gumbo
BACKGROUND:  No treatment regimens have been specifically designed for children, in whom tuberculosis is predominantly intracellular. Given their activity as monotherapy and their ability to penetrate many diseased anatomic sites that characterize disseminated tuberculosis, linezolid and moxifloxacin could be combined to form a regimen for this need. METHODS:  We examined microbial kill of intracellular Mycobacterium tuberculosis (Mtb) by the combination of linezolid and moxifloxacin multiple exposures in a 7-by-7 mathematical matrix...
November 1, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
Barbara Spolaore, Samanta Raboni, Abhijeet Ajit Satwekar, Antonella Grigoletto, Anna Mero, Isabella Monia Montagner, Antonio Rosato, Gianfranco Pasut, Angelo Fontana
Interferon alpha (IFN α) subtypes are important protein drugs that have been used to treat infectious diseases and cancers. Here, we studied the reactivity of IFN α-2b to microbial transglutaminase (TGase) with the aim to obtain a site-specific conjugation of this protein drug. Interestingly, TGase allowed the production of two mono-derivatized isomers of IFN with high yields. Characterization by mass spectrometry of the two conjugates indicated that they are exclusively modified at the level of Gln101 if the protein is reacted in the presence of an amino containing ligand (i...
October 12, 2016: Bioconjugate Chemistry
Ian R Wilkinson, Sarbendra L Pradhananga, Rowena Speak, Peter J Artymiuk, Jon R Sayers, Richard J Ross
: Acromegaly is a human disease of growth hormone (GH) excess with considerable morbidity and increased mortality. Somatostatin analogues are first line medical treatment but the disease remains uncontrolled in up to 40% of patients. GH receptor (GHR) antagonist therapy is more effective but requires frequent high-dose injections. We have developed an alternative technology for generating a long acting potent GHR antagonist through translational fusion of a mutated GH linked to GH binding protein and tested three candidate molecules...
October 12, 2016: Scientific Reports
N Schunck, L M Robledo
This article reviews how nuclear fission is described within nuclear density functional theory. A distinction should be made between spontaneous fission, where half-lives are the main observables and quantum tunnelling the essential concept, and induced fission, where the focus is on fragment properties and explicitly time-dependent approaches are often invoked. Overall, the cornerstone of the density functional theory approach to fission is the energy density functional formalism. The basic tenets of this method, including some well-known tools such as the Hartree-Fock-Bogoliubov (HFB) theory, effective two-body nuclear potentials such as the Skyrme and Gogny force, finite-temperature extensions and beyond mean-field corrections, are presented succinctly...
November 2016: Reports on Progress in Physics
Sara Armorini, James E Yeatts, Keena A E Mullen, Sharon E Mason, Elmira Mehmeti, Kevin L Anderson, Steve P Washburn, Ronald E Baynes
Thymol and carvacrol may be present in several phytoceutical products but there are no well-defined methods to measure these compounds in meat and milk from treated animals. U.S. regulatory authorities deem their presence as an adulteration of food. A rapid and sensitive HS-SPME-GC-MS/MS method was developed for the detection of thymol and carvacrol in bovine milk, plasma, liver, kidney, and fat. Inter- and intraday precision values were all less than 15.7 and 20.2% for thymol and carvacrol, respectively. The accuracy was in ranges of 69...
October 11, 2016: Journal of Agricultural and Food Chemistry
Yan Fu, Ting Yang, Jian Zhao, Liang Zhang, Ruoxia Chen, Yinliang Wu
A LC-MS/MS method for determination of eight pesticides (triadimefon, sulfoxaflor, flusilazole, tebuconazole, difenoconazole, amitraz, azoxystrobin, and thiophanate-methyl) in Lycium barbarum was established. The samples were extracted with acetonitrile, and then cleaned up by primary secondary amine. The extracts were diluted with 0.1% formic acid in water. The results showed that at the fortified levels of 0.01-10mg/kg, the average recoveries of these pesticides ranged from 82.1% to 96.2% with the relative standard deviations lower than 7%...
March 1, 2017: Food Chemistry
John J Veillette, James Truong, Steven C Forland
Limited data exist regarding optimal dosing of ceftazidime/avibactam (C/A) in patients with unique physiology, who were excluded from published clinical trials. Data are also lacking regarding clinical efficacy of C/A in patients with infections due to multidrug-resistant Gram-negative pathogens. To expand knowledge in these areas, we present pharmacokinetic data from two patients with KPC-producing Klebsiella pneumoniae bloodstream infections, both of whom had renal impairment, and one of whom was morbidly obese...
September 26, 2016: Pharmacotherapy
Yongkun Sun, Wei Niu, Feng Du, Chunxia Du, Shuting Li, Jinwan Wang, Li Li, Fengqing Wang, Yu Hao, Chuan Li, Yihebali Chi
BACKGROUND: Anlotinib is a novel multi-target tyrosine kinase inhibitor that is designed to primarily inhibit VEGFR2/3, FGFR1-4, PDGFR α/β, c-Kit, and Ret. We aimed to evaluate the safety, pharmacokinetics, and antitumor activity of anlotinib in patients with advanced refractory solid tumors. METHODS: Anlotinib (5-16 mg) was orally administered in patients with solid tumor once a day on two schedules: (1) four consecutive weeks (4/0) or (2) 2-week on/1-week off (2/1)...
October 4, 2016: Journal of Hematology & Oncology
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