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https://www.readbyqxmd.com/read/28432946/design-and-synthesis-of-sulfonamide-substituted-diphenylpyrimidines-sfa-dppys-as-potent-bruton-s-tyrosine-kinase-btk-inhibitors-with-improved-activity-toward-b-cell-lymphoblastic-leukemia
#1
He Liu, Menghua Qu, Lina Xu, Xu Han, Changyuan Wang, Xiaohong Shu, Jihong Yao, Kexin Liu, Jinyong Peng, Yanxia Li, Xiaodong Ma
A new series of diphenylpyrimidine derivatives (SFA-DPPYs) were synthesized by introducing a functional sulfonamide into the C-2 aniline moiety of pyrimidine template, and then were biologically evaluated as potent Bruton's tyrosine kinase (BTK) inhibitors. Among these molecules, inhibitors 10c, 10i, 10j and 10k displayed high potency against the BTK enzyme, with IC50 values of 1.18 nM, 0.92 nM, 0.42 nM and 1.05 nM, respectively. In particular, compound 10c could remarkably inhibit the proliferation of the B lymphoma cell lines at concentrations of 6...
April 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28432890/characterization-of-spectral-responses-of-dissolved-organic-matter-dom-for-atrazine-binding-during-the-sorption-process-onto-black-soil
#2
Yifan Wang, Xinyuan Zhang, Xing Zhang, Qingjuan Meng, Fengjie Gao, Ying Zhang
This study was aim to investigate the interaction between soil-derived dissolved organic matter (DOM) and atrazine as a kind of pesticides during the sorption process onto black soil. According to the experimental data, the adsorption capacity of Soil + DOM, Soil and DOM were 41.80, 31.45 and 9.35 mg kg(-1), separately, which indicated that DOM significantly enhanced the adsorption efficiency of atrazine by soil. Data implied that the pseudo-second-order kinetic equation could well explain the adsorption process...
April 14, 2017: Chemosphere
https://www.readbyqxmd.com/read/28432812/preparation-characterization-and-in-vivo-study-of-rhein-solid-lipid-nanoparticles-for-oral-delivery
#3
Haiyang Feng, Yuping Zhu, Zhixuan Fu, Dechuan Li
In this study, rhein-SLNs were successfully produced by hot homogenization followed by ultrasonication. Precirol ATO5 in which Rhein exhibited higher partition coefficient was selected for preparation of SLNs. In the dynamic light scattering, the rhein SLNs showed a smaller size with a mean value of 120.8 ± 7.9 nm and with zeta potential of -16.9 ± 2.3 mV. SLNs exhibited a good stability during the period of 2 months. The SLNs indicated faster drug release with a burst release within 2 hours and followed by a sustained release with a biphasic drug release pattern...
April 22, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28432798/therapeutic-drug-monitoring-of-mitotane-analytical-assay-and-patient-follow-up
#4
Yoann Cazaubon, Helene Guillemin, Damien Vautier, Olivier Oget, Hervé Millart, Claire Gozalo, Zoubir Djerada, Catherine Feliu
BACKGROUND: Adrenocortical carcinoma (ACC) is an aggressive malignancy of the adrenal gland. Mitotane (o,p'-DDD) is the most effective chemotherapy for ACC. According to literature, mitotane plasma trough concentrations within 14-20 mg.L(1) are correlated with a higher response rate with acceptable toxicity. Therapeutic drug monitoring (TDM) of mitotane is therefore recommended. The aim of this study was to propose a robust, and simple method for mitotane quantification in plasma. The validation procedures were based on international guidelines...
April 22, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28432776/exploring-non-obvious-hydrophobic-binding-pockets-on-protein-surfaces-increasing-affinities-in-peptide-protein-interactions
#5
Lars Baltzer, Aleksandra Balliu
A 42-residue polypeptide conjugated to a small organic molecule capable of targeting the phosphorylated side chain of Ser-15 was shown to bind glycogen phosphorylase a (GPa) with a KD of 280 nM. The replacement of hydrophobic amino acids by Ala reduced affinities, whereas the incorporation of L-2-aminooctanoic acid (Aoc) increased affinities. Replacing Nle-5, Ile-9 and Leu-12 by Aoc reduced the KD from 280 nM to 27 nM. Downsizing the 42-mer to an 11-mer gave rise to an order of magnitude lower affinity for GPa but the 11-mer where Nle-5, Ile-9 and Leu-12 were replaced by Aoc showed a KD of 550 nM, comparable to that of the parent 42-mer...
April 22, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/28432771/a-rare-variant-in-tor1a-exon-5-associated-with-isolated-dystonia-in-southwestern-chinese
#6
Yuzhou Long, Yang Chen, Yuan Qian, Jianlin Wang, Lihua Luo, Xiaoqin Huang, Li Li, Jiayou Chu, Zhaoqing Yang, Hao Sun
BACKGROUND: TOR1A has been proposed as an important genetic factor in early-onset isolated dystonia. Variants located in the 3' untranslated region of TOR1A are of particular importance because they may influence gene expression, although related studies are limited. The objectives of the present study focused on variants in the TOR1A 3' untranslated region. METHODS: The last exon of TOR1A was sequenced in 229 cases with isolated dystonia and in 210 controls. In addition, 471 controls were tested to determine the frequency of the variants in the 3' untranslated region...
April 22, 2017: Movement Disorders: Official Journal of the Movement Disorder Society
https://www.readbyqxmd.com/read/28432711/vdr-gene-methylation-as-a-molecular-adaption-to-light-exposure-historic-recent-and-genetic-influences
#7
Emma L Beckett, Patrice Jones, Martin Veysey, Konsta Duesing, Charlotte Martin, John Furst, Zoe Yates, Nina G Jablonski, George Chaplin, Mark Lucock
OBJECTIVES: The vitamin D receptor (VDR) is a member of the nuclear receptor family of transcription factors. We examined whether degree of VDR gene methylation acts as a molecular adaptation to light exposure. We explored this in the context of photoperiod at conception, recent UV irradiance at 305 nm, and gene-latitude effects. METHODS: Eighty subjects were examined for VDR gene-CpG island methylation density. VDR gene variants were also examined by PCR-RFLP. RESULTS: Photoperiod at conception was significantly positively related to VDR methylation density, explaining 17% of the variance in methylation (r(2)  = 0...
April 22, 2017: American Journal of Human Biology: the Official Journal of the Human Biology Council
https://www.readbyqxmd.com/read/28432685/chiral-analysis-of-%C3%AE-diimine-ru-ii-and-fe-ii-complexes-by-capillary-electrophoresis-using-sulfated-cyclodextrins-as-stereoselectors
#8
Petra Sázelová, Dušan Koval, Lukáš Severa, Filip Teplý, Václav Kašička
Capillary electrophoresis (CE) using randomly highly sulfated α-, β-, and γ-cyclodextrins (S-α-CD, S-β-CD, S-γ-CD), sulfobutylether-β-CD (SBE-β-CD), single isomer (6-O-sulfo) α-, β-, and γ-CDs and their derivatives as stereoselectors was applied to chiral analysis of polypyridyl complexes of [Ru(bpy)3 ](2+) , [Ru(phen)3 ](2+) , and [Fe(phen)3 ](2+) (bpy = 2,2'-bipyridine; phen = 1,10 phenanthroline). The best separations of Δ- and Λ-enantiomers of the these complexes with high resolution (up to R1,2  = 7...
April 22, 2017: Electrophoresis
https://www.readbyqxmd.com/read/28432681/retrospective-single-center-study-of-the-efficacy-of-large-spot-532%C3%A2-nm-laser-for-the-treatment-of-facial-capillary-malformations-in-44-patients-with-the-use-of-three-dimensional-image-analysis
#9
Bartłomiej Kwiek, Michał Rożalski, Cezary Kowalewski, Marcin Ambroziak
OBJECTIVE: We wanted to asses the efficacy of large spot 532 nm laser for the treatment of facial capillary malformations with the use of three-dimensional (3D) image analysis. STUDY DESIGN AND METHODS: Retrospective single center study on previously non-treated patients with facial capillary malformations (CM) was performed. A total of 44 consecutive Caucasian patients aged 5-66 were included. Patients had 3D photography performed before and after and had at least one single session of treatment with 532 nm neodymium-doped yttrium aluminum garnet (Nd:YAG) laser with contact cooling, fluencies ranging from 8 to 11...
April 22, 2017: Lasers in Surgery and Medicine
https://www.readbyqxmd.com/read/28432654/laser-desorption-ionization-mass-spectrometric-imaging-of-endogenous-lipids-from-rat-brain-tissue-implanted-with-silver-nanoparticles
#10
Ludovic Muller, Kathrine Baldwin, Damon C Barbacci, Shelley N Jackson, Aurélie Roux, Carey D Balaban, Bruce E Brinson, Michael I McCully, Ernest K Lewis, J Albert Schultz, Amina S Woods
Mass spectrometry imaging (MSI) of tissue implanted with silver nanoparticulate (AgNP) matrix generates reproducible imaging of lipids in rodent models of disease and injury. Gas-phase production and acceleration of size-selected 8 nm AgNP is followed by controlled ion beam rastering and soft landing implantation of 500 eV AgNP into tissue. Focused 337 nm laser desorption produces high quality images for most lipid classes in rat brain tissue (in positive mode: galactoceramides, diacylglycerols, ceramides, phosphatidylcholines, cholesteryl ester, and cholesterol, and in negative ion mode: phosphatidylethanolamides, sulfatides, phosphatidylinositol, and sphingomyelins)...
April 21, 2017: Journal of the American Society for Mass Spectrometry
https://www.readbyqxmd.com/read/28432634/new-chromophore-systems-from-coumarin-oxazol-5-one-combination
#11
Derya Topkaya, Serap Alp
Coumarin-oxazol-5-one (COX), 3a-d, were synthesized with 7-methoxy-2-oxo-2H-chromene-4-carbaldehyde and benzoylglycine derivatives. The characterizations of the COX derivatives by (1)H NMR, FT-IR and elemental analysis were achieved. To obtain the photophysical data of the synthesized COX derivatives were used spectrophotometric and spectrofluorimetric methods. Evaluation of the absorption and emission properties of the structures was carried out in six different solvents. Maximum absorption and emission wavelengths (λ; nm), molar extinction coefficients (ε; cm(-1) M(-1)), Stoke's shifts (ΔλST; nm) and quantum yields (ϕF), of the COX derivatives were declared...
April 22, 2017: Journal of Fluorescence
https://www.readbyqxmd.com/read/28432599/the-beneficial-effect-of-repaglinide-on-in-vitro-maturation-and-development-ability-of-immature-mouse-oocytes
#12
Eshrat Kalehoei, Mehri Azadbakht
Repaglinide is a hypoglycemic drug, causing depolarization of the cell membrane, opening the voltage-gated calcium channels, and then increasing intracellular calcium in the pancreatic B cells by inhibition of the K-ATP-sensitive channels. Oocyte in vitro maturation (IVM) is influenced by different factors such as calcium signaling. In this study, we examined the effects of repaglinide on in vitro maturation and fertilization ability of mouse oocyte. Immature oocytes were isolated from female Naval Medical Research Institute mice which are 6-8 wk old mechanically and then cultured in 30 μl droplets of T6 medium with different concentrations of repaglinide...
April 21, 2017: In Vitro Cellular & Developmental Biology. Animal
https://www.readbyqxmd.com/read/28432501/high-scale-yield-of-nano-hydroxyapatite-through-combination-of-mechanical-activation-and-chemical-dispersion
#13
Xueling Gao, Chunchu Dai, Weiwei Liu, Yumei Liu, Ru Shen, Xiaotong Zheng, Ke Duan, Jie Weng, Shuxin Qu
The aim of this study is to develop a simple, convenient and effective approach to synthesize nano-sized hydroxyapatite (nano-HA) at high-scale yield. Nano-HA was wet synthesized in the presence or absence of alendronate sodium (ALN), one of bisphosphonates for anti-osteoporotic. Then aged and washed nano-HA precipitate was directly treated by mechanical activation combined with the chemical dispersion of ALN to prevent the agglomeration of nano-HA. ALN acted not only as a chemical dispersant but also as an orthopedic drug...
June 2017: Journal of Materials Science. Materials in Medicine
https://www.readbyqxmd.com/read/28432452/fluorescent-angioscopic-imaging-of-calcium-phosphate-tribasic-precursor-of-hydroxyapatite-the-major-calcium-deposit-in-human-coronary-plaques
#14
Takanobu Kobayashi, Osamu Nakagawa, Seiichiro Shirai, Ei Shimoyama, Nobuyuki Hiruta, Yasumi Uchida
Coronary calcification is a risk factor for ischemic heart disease. Hydroxyapatite that is formed by polymerization from calcium phosphate tribasic (CPT) is the major constituent of coronary calcium deposits. If CPT could be visualized, coronary calcification could be predicted and prevented. We discovered that when CPT and collagen I, the main constituent of collagen fibers, are mixed with lac dye (LD) and then exposed to fluorescent light excited at 345 ± 15 nm and emitted at 420 nm, a purple fluorescence that is characteristic of CPT only is elicited...
April 21, 2017: International Journal of Cardiovascular Imaging
https://www.readbyqxmd.com/read/28432365/effects-of-porosity-on-dynamic-indentation-resistance-of-silica-nanofoam
#15
Zhao Cang, Zhong Ying, Qiao Yu
The dynamic indentation behaviors of monolithic silica nanofoams of various porosities are investigated. When the pore size is on the nm scale, as the porosity increases, despite the decrease in mass density, the resistance offered by silica nanofoam to dynamic indentation is maintained at a high level, higher than the resistance of solid silica or regular porous silica. This phenomenon is related to the fast collapse of nanocells, which produces a locally hardened region and significantly increases the volume of material involved in impact energy dissipation...
April 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28432344/aptamer-based-label-free-electrochemical-biosensor-array-for-the-detection-of-total-and-glycated-hemoglobin-in-human-whole-blood
#16
Shimaa Eissa, Mohammed Zourob
The increase of the level of glucose in blood leads to an increase in the fraction of glycated hemoglobin (HbA1c). Therefore, the percentage of HbA1c in the blood can serve as a marker for the average glucose level over the past three months and thus, it can be used to diagnose diabetes. Here, we report the selection, identification and characterization of specific DNA aptamers against HbA1c- and total hemoglobin (tHb) and their integration into an electrochemical array sensing platform. High affinity and specificity aptamers were selected in vitro showing dissociation constants of 2...
April 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28432329/affinity-biosensors-using-recombinant-native-membrane-proteins-displayed-on-exosomes-application-to-botulinum-neurotoxin-b-receptor
#17
Richard Desplantes, Christian Lévêque, Benjamin Muller, Manuela Lotierzo, Géraldine Ferracci, Michel Popoff, Michael Seagar, Robert Mamoun, Oussama El Far
The development of simple molecular assays with membrane protein receptors in a native conformation still represents a challenging task. Exosomes are extracellular vesicles which, due to their stability and small size, are suited for analysis in various assay formats. Here, we describe a novel approach to sort recombinant fully native and functional membrane proteins to exosomes using a targeting peptide. Specific binding of high affinity ligands to the potassium channel Kv1.2, the G-protein coupled receptor CXCR4, and the botulinum neurotoxin type B (BoNT/B) receptor, indicated their correct assembly and outside out orientation in exosomes...
April 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28432306/simple-rectangular-gratings-as-a-near-field-anti-reflection-pattern-for-gasb-tpv-cells
#18
Haitong Yu, Dong Liu, Zhen Yang, Yuanyuan Duan
We show theoretically that 2D rectangular gratings on the surface of GaSb can serve as an "anti-reflection" pattern for nano-gap thermophotovoltaic (TPV) devices, which significantly enhances near-field radiative flux from the emitter to a GaSb cell, thus improving output power and conversion efficiency. The system in this study is a 200-nm gap TPV power generation system with a planar infrared plasmonic emitter and GaSb cell. Rigorous coupled-wave analysis is used to calculate the spectral near-field radiative flux involving periodic structures...
April 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28432073/in-situ-laser-fenestration-is-a-feasible-method-for-revascularization-of-aortic-arch-during-thoracic-endovascular-aortic-repair
#19
Jinbao Qin, Zhen Zhao, Ruihua Wang, Kaichuang Ye, Weimin Li, Xiaobing Liu, Guang Liu, Chaoyi Cui, Huihua Shi, Zhiyou Peng, Fukang Yuan, Xinrui Yang, Min Lu, Xintian Huang, Mier Jiang, Xin Wang, Minyi Yin, Xinwu Lu
BACKGROUND: Reconstruction of the aortic major branches during thoracic endovascular aortic repair is complicated because of the complex anatomic configuration and variation of the aortic arch. In situ laser fenestration has shown great potential for the revascularization of aortic branches. This study aims to evaluate the feasibility, effectiveness, and safety of in situ laser fenestration on the three branches of the aortic arch during thoracic endovascular aortic repair. METHODS AND RESULTS: Before clinical application, the polytetrafluoroethylene and Dacron grafts were fenestrated by an 810-nm laser system ex vivo, which did not damage the bare metal portion of the endografts and created a clean fenestration while maintaining the integrity of the endografts...
April 21, 2017: Journal of the American Heart Association
https://www.readbyqxmd.com/read/28432000/determination-of-thiol-to-protein-ratio-and-drug-to-antibody-ratio-by-in-line-size-exclusion-chromatography-with-post-column-reaction
#20
Kenichiro Furuki, Toshimasa Toyo'oka
An in-line size-exclusion (SE) ultra-high-performance liquid chromatography (UHPLC)- 5,5-dithio-bis-(2-nitrobenzoic acid) (DTNB) method to quantify thiols in monoclonal antibodies (mAb) when manufacturing antibody-drug conjugates (ADCs) was developed. The mAbs are separated on an SE-UHPLC column and monitored with a UV detector at a wavelength of 280 nm. Eluents are channeled into a reaction coil and mixed with DTNB to form 5-thio-2-nitrobenzoic acid (TNB). Thiol concentration is calculated using absorption at 412 nm...
April 18, 2017: Analytical Biochemistry
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