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Mengyao Wang, Chao Yang, Xiuqing Zhang, Xiangchun Li
The key roles of the TP53 mutation in cancer have been well established. TP53 is the most frequently mutated gene, and its inactivation is widespread among human cancer types. However, the landscape of genomic alterations in human cancers stratified by the TP53 mutation has not yet been described. We obtained somatic mutation and copy number change data of 6551 regular-mutated samples from the Cancer Genome Atlas (TCGA) and compared significantly mutated genes (SMGs), copy number alterations, mutational signatures and mutational strand asymmetries between cancer samples with and without the TP53 mutation...
January 12, 2018: Molecular Genetics and Genomics: MGG
Chuanhong Wu, Wenwen Zhao, Jie Yu, Shaojing Li, Ligen Lin, Xiuping Chen
Neurodegenerative diseases (NDD) are typically associated with neuron loss in nervous system areas. Interventions with related death mechanisms may ameliorate NDD progression. Oxidative stress plays an important role in NDD cell death routines. However, tert-butylhydroperoxide (t-BHP), a widely used oxidative stress stimulus, induces neural cell death through a mechanism that remains elusive. In our study, the ferroptosis marker events occurred after co-treatment with 100 μM t-BHP for 1 h, all of which were reversed in the presence of the ferroptosis inhibitor ferrostatin-1 (Fer-1) and the iron chelator deferoxamine, implying the occurrence of ferroptosis...
January 12, 2018: Scientific Reports
Martin Pisár, Eva Schütznerová, Filip Hančík, Igor Popa, Zdeněk Trávníček, Petr Cankař
The cyclin-dependent kinase inhibitor, CAN508, was protected with di-tert-butyl dicarbonate to access the amino-benzoylated pyrazoles. The bromo derivatives were further arylated by Suzuki-Miyaura coupling using the XPhos Pd G2 pre-catalyst. The coupling reaction provided generally the para-substituted benzoylpyrazoles in the higher yields than the meta-substituted ones. The Boc groups were only utilized as directing functionalities for the benzoylation step and were hydrolyzed under conditions of Suzuki-Miyaura coupling, which allowed for elimination of the additional deprotection step...
January 12, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Chang-Lun Shao, Xiao-Feng Mou, Fei Cao, Carmenza Spadafora, Evgenia Glukhov, Lena Gerwick, Chang-Yun Wang, William H Gerwick
We reported previously the discovery of the potent antimalarial 40-membered macrolide bastimolide A (1) from the tropical marine cyanobacterium Okeania hirsute. Continued investigation has led to the discovery of a new analogue, bastimolide B (2), a 24-membered polyhydroxy macrolide with a long aliphatic chain and unique terminal tert-butyl group. Its complete structure was determined by a combination of extensive spectroscopic methods and comparative analysis of its methanolysis products with those of bastimolide A...
January 12, 2018: Journal of Natural Products
J S Haataja, N Houbenov, V Aseyev, P Fragouli, H Iatrou, R Sougrat, N Hadjichristidis, O Ikkala
Polystyrene-block-poly(1,4-isoprene)-block-poly(dimethyl siloxane)-block-poly(tert-butyl methacrylate)-block-poly(2-vinyl pyridine), PS-b-PI-b-PDMS-b-PtBMA-b-P2VP, self-assembles in acetone into polymersomes with asymmetric (directional) PI-b-PDMS membranes. The polymersomes, in turn, self-assemble into superstructures. Analogically to supravesicular structures at a smaller length scale, we refer to them as suprapolymersome structures. Electron tomograms are shown to be invaluable in the structural assessment of such complex self-assemblies...
January 12, 2018: Chemical Communications: Chem Comm
Maryam Nejat Dehkordi, Bjorn Akerman
Interaction of double stranded DNA with bulky and hydrophobic Salen type Schiff base complex: [N, N' Bis [3- tert-butyl-5-[triphenyl-phosphonium - methyl] - salicylidene] 1,2 ethylene-diamine nickel(III) acetate (refer to Ni Salen complex) was extensively investigated using the spectroscopic techniques and gel electrophoresis. Absorption titration experiment showed the hypochromic effect and the significant red shift of the complex absorption. In competition experiments with ethidium bromide (EB), Ni Salen complex exhibited non-competitive binding at high concentrations...
January 8, 2018: Chemico-biological Interactions
Kristina Schmitt, Michael Lämmerhofer
A new platform technology for the preparation of stable chiral stationary phases was successfully optimized. The chiral selector tert-butylcarbamoylquinine was firstly covalently connected to the polymer poly(3-mercaptopropyl)methylsiloxane by thiol-ene click reaction. Secondly, the quinine carbamate functionalized polysiloxane conjugate was coated onto the surface of vinyl modified silica particles and crosslinked via thiol-ene click reaction. The amount of polysiloxane, chiral selector, radical initiator, reaction solvent (chloroform and methanol), reaction time, and pore size of the supporting silica particles were varied and systematically optimized in terms of achievable plate numbers while maintaining simultaneously enantioselectivity...
January 11, 2018: Journal of Separation Science
Heibatullah Kalantari, Hossein Foruozandeh, Mohammad Javad Khodayar, Amir Siahpoosh, Najmaldin Saki, Parvin Kheradmand
The present study investigates the antioxidant and hepatoprotective effects of Capparis spinosa L. and Quercetin in tert-butyl hydroperoxide (t-BHP) induced acute liver damage. Different fractions of C. spinosa were examined for total phenolic content and antioxidant property. Among these fractions, hydroalcoholic extract was used to assess the hepatoprotective effect in tert-butyl hydroperoxide (t-BHP) induced hepatotoxicity model by determining serum biochemical markers, sleeping time and antioxidant assay such as reduced glutathione (GSH) as well as histopathological examination of liver tissues...
January 2018: Journal of Traditional and Complementary Medicine
Alberto Fabrizio, Clémence Corminboeuf
In the last two decades, linear-response time-dependent density functional theory (LR-TDDFT) has become one of the most widely used approaches for the computation of the excited-state properties of atoms and molecules. Despite its success in describing the photochemistry and the photophysics of a vast majority of molecular systems, its domain of applicability has been limited by several substantial drawbacks. Commonly identified problems of LR-TDDFT include the correct description of Rydberg states, charge-transfer excited states, doubly excited states, and nearly degenerate states...
January 12, 2018: Journal of Physical Chemistry Letters
Paul James Chirik, Mate Bezdek
Interconversion of the molybdenum amido [(PhTpy)(PPh2Me)2Mo(NHtBuAr)][BArF24] [PhTpy = 4'-Ph-2,2',6',2"-terpyridine; tBuAr = 4-tert-butyl-C6H4; ArF24 = (C6H3-3,5-(CF3)2)4)] and imido [(PhTpy)(PPh2Me)2Mo(NtBuAr)][BArF24] complexes has been accomplished by proton coupled electron transfer (PCET). Tert-butylphenoxyl radical was used as an oxidant and the non-classical ammine complex [(PhTpy)(PPh2Me)2Mo(NH3)][BArF24] as the reductant. The amido N-H BDFE formed and cleaved in the sequence was experimentally bracketed between 45...
January 10, 2018: Angewandte Chemie
Branislav Lukić, Uroš Grošelj, Marko Novinec, Jurij Svete
Eight novel 5-(N-Boc-N-benzyl-2-aminoethyl)-7-oxo-4,7-dihydropyrazolo[1,5-a]pyrimidin-3-carboxamides were prepared in three steps from methyl 3-amino-1H-pyrazole-4-carboxylate and methyl 5-(benzyl(tert-butoxycarbonyl)amino)-3-oxopentanoate. The synthetic procedure comprises cyclocondensation of the above starting compounds, hydrolysis of the ester, and bis(pentafluorophenyl) carbonate (BPC)-mediated amidation. Title carboxamides were tested for inhibition of cathepsins K and B. The N-butylcarboxamide 5a exhibited appreciable inhibition of cathepsin K (IC50 ~ 25 μM), while the strongest inhibition of cathepsin B was achieved with N-(2-picolyl)carboxamide 5c (IC50 ~ 45 μM)...
December 2017: Acta Chimica Slovenica
Diego A Garcia-Dios, Dina Levi, Vandna Shah, Cheryl Gillett, Michael A Simpson, Andrew Hanby, Ian Tomlinson, Elinor J Sawyer
BACKGROUND: MED12 and TERT promoter mutations have been shown to be the most common somatic mutations in phyllodes tumours (PTs). The aims of this study were to determine the frequency of these mutations in recurrent PTs, assess whether TERT promoter mutations could be helpful in distinguishing fibroadenomas (FAs) from PTs and identify novel mutations that may be driving malignant progression. METHODS: MED12 and the TERT promoter were Sanger sequenced in 75 primary PTs, 21 recurrences, 19 single FAs and 2 cases of multiple FAs with benign PTs...
January 9, 2018: British Journal of Cancer
Ola M Abdallah, Ahmed M Abdel-Megied, Amira S Gouda
The first simple and highly sensitive Liquid chromatography-tandem mass spectrometry (LC-MS/MS) bioanalytical method was developed and fully validated for the simultaneous determination of newly discovered antiviral drugs namely, Sofosbuvir (SOF) and Daclatasvir (DAC) in human plasma. Tadalafil (TAD) was used as internal standard (IS). SOF, DAC and TAD (IS) were extracted from plasma using liquid-liquid extraction technique with methyl tert-butyl ether. The chromatographic separation was carried out using ZorbaxSB-C18 column (4...
January 3, 2018: Biomedical Chromatography: BMC
Yahan Wu, Xiaoqiang Shi, Xihong Ding, Yingke Ren, Tasawar Hayat, Ahmed Alsaedi, Yong Ding, Pan Xu, Songyuan Dai
The synthesis and growth of CH3NH3PbI3 film with controlled nucleation was a key issue for high efficient and stable solar cells. Here, 4-tert-butylpyridine (tBP) was introduced into the CH3NH3PbI3 antisolvent to obtain high quality perovskite layers. In situ optical microscopy, X-ray diffraction patterns were used to prove that tBP significantly suppressed the perovskite nucleation by forming the intermediate phase. In addition, a gradient perovskite structure was obtained by this method, which greatly improved the efficiency and stability of perovskite...
January 9, 2018: ACS Applied Materials & Interfaces
Tareq A Juratli, Christian Thiede, Mara V A Koerner, Shilpa S Tummala, Dirk Daubner, Ganesh M Shankar, Erik A Williams, Maria Martinez-Lage, Silke Soucek, Katja Robel, Tristan Penson, Mechthild Krause, Steffen Appold, Matthias Meinhardt, Thomas Pinzer, Julie J Miller, Dietmar Krex, Heather A Ely, Ian M Silverman, Jason Christiansen, Gabriele Schackert, Hiroaki Wakimoto, Matthias Kirsch, Priscilla K Brastianos, Daniel P Cahill
Background: Recent studies have reported mutations in the telomerase reverse transcriptase promoter (TERTp) in meningiomas. We sought to determine the frequency, clonality and clinical significance of telomere gene alterations in a cohort of patients with progressive/higher-grade meningiomas. Methods: We characterized 64 temporally- and regionally-distinct specimens from 26 WHO grade III meningioma patients. On initial diagnoses, the meningiomas spanned all WHO grades (3 grade I, 13 grade II and 10 grade III)...
December 12, 2017: Oncotarget
Soo Yeon Hahn, Tae Hyuk Kim, Chang Seok Ki, Sun Wook Kim, Soohyun Ahn, Jung Hee Shin, Jae Hoon Chung
This study is to investigate if any relationship exists between the telomerase reverse transcriptase (TERT) promoter or proto-oncogene BRAF mutation and ultrasound (US) and clinicopathological features of papillary thyroid carcinomas (PTCs). The study included 150 patients with surgically confirmed PTC from October 1994 to December 2004. According to the existence of TERT promoter or BRAF mutations, we categorized patients into three groups (no mutation, BRAF mutation alone, or TERT+BRAF mutations) and analyzed the relationships between TERT promoter or BRAF mutation and US and clinicopathological features...
December 12, 2017: Oncotarget
Thiago Inácio Barros Lopes, Roberta Gomes Coelho, Neli Kika Honda
Several applications have been proposed for tyrosinase inhibitors in the pharmaceutical, food bioprocessing, and environmental industries. However, only a few compounds are known to serve as effective tyrosinase inhibitors. This study evaluated the tyrosinase-related activity of resorcinol (1), orcinol (2) lecanoric acid (3), and derivatives of this acid (4-15). Subjected to alcoholysis, lecanoric acid (3), a depside isolated from the lichen Parmotrema tinctorum, produces orsellinic acid (2,4-dihydroxy-6-methylbenzoic acid) (4) and orsellinates (2,4-dihydroxy-6-methyl benzoates) (5-15)...
2018: Chemical & Pharmaceutical Bulletin
Guillaume Blanchet-Chouinard, Dominic Larivière
In the present study, a new cloud point extraction methodology based on the selective preconcentration and the extraction of stable lead in acidic conditions with 4',4''(5'')-di-tert-butyldicyclohexano-18-crown-6 as a chelating agent was developed, optimized and validated. A mixture of Triton X-114 as non-ionic surfactant and CTAB as cationic surfactant was used to produce micellar structures that incorporate the chelating agent. Phase separation, induced by coacervation, was achieved by increasing the temperature of the system above the cloud point temperature...
March 1, 2018: Talanta
Xiuxiu Wang, Mingli Zhu, Fei Gao, Wei Wei, Yong Qian, Hong-Ke Liu, Jing Zhao
Iridium-based anticancer reagents are receiving increasing attention for their high cytotoxicity. Herein, by activating CH bonds in the well-known antioxidant α-phenyl-N-tert-butylnitrone (PBN), we synthesized and characterized a series of new iridium complexes. Complex 1-AMP exhibited the best antiproliferation activity towards human ovarian cancer A2780 cells. The azide group in complex 1-AMP underwent the Cu(I)-catalysed azide-alkyne cycloaddition (CuAAC) reaction and the resulting fluorescent imaging in cells suggested it mainly accumulated in mitochondria...
December 29, 2017: Journal of Inorganic Biochemistry
Karl Deacon, Alan J Knox
Airway smooth muscle (ASM) cells contribute to asthmatic lung pathology with chemokine hypersecretion and increased ASM cell mass. With little recent progress in the development of asthma therapies, a greater understanding of lung inflammation mechanisms has become a priority. Chemokine gene expression in ASM cells is dependent upon NF-κB transcription factor activity. The telomerase/shelterin complex maintains chromosomal telomere ends during cell division. Telomerase is a possible cofactor for NF-κB activity, but its role in NF-κB activity in airway tissue inflammation is not known...
January 5, 2018: Journal of Immunology: Official Journal of the American Association of Immunologists
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