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https://www.readbyqxmd.com/read/28431244/bacterial-metabolism-affects-the-c-%C3%A2-elegans-response-to-cancer-chemotherapeutics
#1
Aurian P García-González, Ashlyn D Ritter, Shaleen Shrestha, Erik C Andersen, L Safak Yilmaz, Albertha J M Walhout
The human microbiota greatly affects physiology and disease; however, the contribution of bacteria to the response to chemotherapeutic drugs remains poorly understood. Caenorhabditis elegans and its bacterial diet provide a powerful system to study host-bacteria interactions. Here, we use this system to study how bacteria affect the C. elegans response to chemotherapeutics. We find that different bacterial species can increase the response to one drug yet decrease the effect of another. We perform genetic screens in two bacterial species using three chemotherapeutic drugs: 5-fluorouracil (5-FU), 5-fluoro-2'-deoxyuridine (FUDR), and camptothecin (CPT)...
April 20, 2017: Cell
https://www.readbyqxmd.com/read/28429734/neuroprotective-pentapeptide-cn-105-is-associated-with-reduced-sterile-inflammation-and-improved-functional-outcomes-in-a-traumatic-brain-injury-murine-model
#2
Daniel T Laskowitz, Haichen Wang, Tony Chen, David T Lubkin, Viviana Cantillana, Tian Ming Tu, Dawn Kernagis, Guanen Zhou, Gary Macy, Bradley J Kolls, Hana N Dawson
At present, there are no proven pharmacological treatments demonstrated to improve long term functional outcomes following traumatic brain injury(TBI). In the setting of non-penetrating TBI, sterile brain inflammatory responses are associated with the development of cerebral edema, intracranial hypertension, and secondary neuronal injury. There is increasing evidence that endogenous apolipoprotein E(apoE) modifies the neuroinflammatory response through its role in downregulating glial activation, however, the intact apoE holoprotein does not cross the blood-brain barrier due to its size...
April 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28429512/tailored-approach-for-management-of-ventricular-tachycardia-in-cardiac-sarcoidosis
#3
Sachin Yalagudri, Ngwe Zin Thu, Soumen Devidutta, Daljeet Saggu, Ajit Thachil, Sridevi Chennapragada, Calambur Narasimhan
INTRODUCTION: Treating ventricular tachycardia (VT) in patients with cardiac sarcoidosis (CS) is challenging as patients present in different phase of the disease (inflammatory, scar or sometimes both). A customized approach to treatment is required for better outcomes. We describe our experience in the management of VT in CS based on the phase of the disease. METHODS AND RESULTS: Patients were considered to have myocardial inflammation if there was an increased myocardial (18) Fluoro Deoxy Glucose (FDG) uptake in PET-CT scan of the chest (n=14)...
April 21, 2017: Journal of Cardiovascular Electrophysiology
https://www.readbyqxmd.com/read/28426991/clinical-usefulness-of-18-f-fdg-pet-ct-for-initial-staging-and-assessment-of-treatment-efficacy-in-patients-with-lymph-node-tuberculosis
#4
Nicolas Lefebvre, Xavier Argemi, Nicolas Meyer, Joy Mootien, Nawal Douiri, Stefania Sferrazza-Mandala, Frédéric Schramm, Noëlle Weingertner, Daniel Christmann, Yves Hansmann, Alessio Imperiale
INTRODUCTION: Few studies have evaluated the promising role of (18)F-fluoro-2-deoxy-D-glucose positron emission tomography (PET) and PET/computed tomography FDG PET/CT in evaluating and monitoring treatment response in patients with lymph node tuberculosis (LNTB). The aim of this clinical investigation was to assess the clinical usefulness of FDG PET/CT for initial tuberculosis staging and to determine the prognostic value of the decrease of (18)F-FDG uptake during antibiotic treatment in LNTB patients...
April 8, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28425702/oxidatively-induced-c-h-activation-at-high-valent-nickel
#5
Eugene Chong, Jeff W Kampf, Alireza Ariafard, Allan J Canty, Melanie S Sanford
This communication describes a series of oxidatively induced intramolecular arene C-H activation reactions of Ni(II) model complexes to yield Ni(IV) σ-aryl products. These reactions proceed within 10 min at room temperature, which represents among the mildest conditions reported for C-H cleavage at a Ni center. A combination of density functional theory and preliminary experimental mechanistic studies implicate a pathway involving initial 2e(-) oxidation of the Ni(II) starting materials by the F(+) transfer reagent N-fluoro-2,4,6-trimethylpyridinium triflate followed by triflate-assisted C-H cleavage at Ni(IV) to yield the products...
April 20, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28424014/semi-quantitative-analysis-of-cerebral-fdg-pet-reveals-striatal-hypermetabolism-and-normal-cortical-metabolism-in-a-case-of-vgkcc-limbic-encephalitis
#6
Patrick Moloney, Ruth Boylan, Marwa Elamin, Sean O'Riordan, Ronan Killeen, Christopher McGuigan
In the context of delayed autoimmune encephalitis antibody results, functional imaging can support the diagnosis of limbic encephalitis associated with anti-voltage-gated potassium channel complex (VGKCC) antibodies. Here we present a typical case of VGKCC encephalitis in a 69-year-old woman whose symptoms responded to plasmapheresis. A cerebral 18F-fluoro-2-deoxy-d-glucose positron emission tomography (FDG-PET) scan performed prior to commencing treatment revealed striatal hypermetabolism assessed qualitatively and semi-quantitatively, with normal uptake in the cortex and cerebellum when analysed semi-quantitatively...
April 2017: Neuroradiology Journal
https://www.readbyqxmd.com/read/28422979/correlation-of-egfr-or-kras-mutation-status-with-18f-fdg-uptake-on-pet-ct-scan-in-lung-adenocarcinoma
#7
Kazuya Takamochi, Kaoru Mogushi, Hideya Kawaji, Kota Imashimizu, Mariko Fukui, Shiaki Oh, Masayoshi Itoh, Yoshihide Hayashizaki, Weijey Ko, Masao Akeboshi, Kenji Suzuki
BACKGROUND: 18F-fluoro-2-deoxy-glucose (18F-FDG) positron emission tomography (PET) is a functional imaging modality based on glucose metabolism. The correlation between EGFR or KRAS mutation status and the standardized uptake value (SUV) of 18F-FDG PET scanning has not been fully elucidated. METHODS: Correlations between EGFR or KRAS mutation status and clinicopathological factors including SUVmax were statistically analyzed in 734 surgically resected lung adenocarcinoma patients...
2017: PloS One
https://www.readbyqxmd.com/read/28422433/rigid-non-fullerene-acceptors-based-on-triptycene-perylene-dye-for-organic-solar-cells
#8
Dong Meng, Huiting Fu, Bingbing Fan, Jianqi Zhang, Yan Li, Yanming Sun, Zhaohui Wang
Three kinds of non-conjugated rigid perylene bisimide (PBI) derivatives based on a triptycene core were designed, synthesized and characterized. The unique three-dimensional (3D) conformation of triptycene could enable formation of polymer with the favorable morphology for organic polymer solar cells (PSCs) by relieving the self-aggregation of rigid PBI units. The low-lying LUMO energy levels of these compounds demonstrated that they are very suitable for using as acceptors in organic solar cells. A higher power conversion efficiency (PCE) of 6...
April 19, 2017: Chemistry, An Asian Journal
https://www.readbyqxmd.com/read/28422079/synthetic-fluororutaecarpine-inhibits-inflammatory-stimuli-and-activates-endothelial-transient-receptor-potential-vanilloid-type-1
#9
Chi-Ming Lee, Jiun-An Gu, Tin-Gan Rau, Chi Wang, Chiao-Han Yen, Shih-Hao Huang, Feng-Yen Lin, Chun-Mao Lin, Sheng-Tung Huang
The natural product, rutaecarpine (RUT), is the main effective component of Evodia rutaecarpa which is a widely used traditional Chinese medicine. It has vasodilation, anticoagulation, and anti-inflammatory activities. However, further therapeutic applications are limited by its cytotoxicity. Thus, a derivative of RUT, 10-fluoro-2-methoxyrutaecarpine (F-RUT), was designed and synthesized that showed no cytotoxicity toward RAW264.7 macrophages at 20 μM. In an anti-inflammation experiment, it inhibited the production of nitric oxide (NO) and tumor necrosis factor (TNF)-α in lipopolysaccharide (LPS)-stimulated RAW264...
April 19, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28419929/-r-and-s-18-f-labeled-2-arylbenzofurans-with-improved-pharmacokinetics-as-%C3%AE-amyloid-imaging-probes
#10
Jia Song, Xiaoyang Zhang, Yunling Zhao, Hui Yang, Jinming Zhang, Xiaojun Zhang, Jiapei Dai, Mengchao Cui
A new class of optical isomers of 2-arylbenzofuran derivatives were synthesized and evaluated as potential β-amyloid plaques imaging agents. Both lipophilicity and signal-to-noise ratio were significantly improved by adding a chiral hydroxyl group to 1-fluoro-3-(oxidanyl)propan-2-ol side chain. These derivatives displayed moderate to high binding affinity towards Aβ1-42 aggregates. Four tracers possessing potent binding affinity (Ki < 30 nM) were chosen for further investigation. In in vitro autoradiography studies, the four selected probes showed effective binding to Aβ plaques in Tg mouse and AD human brain tissue after labeled by (18)F...
April 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28419799/synthesis-of-protected-3-deoxy-3-fluoro-and-4-deoxy-4-fluoro-d-galactopyranosides-from-levoglucosan
#11
Danny Lainé, Vincent Denavit, Denis Giguère
Fluorinated carbohydrates are invaluable tools to study various biochemical processes. Herein, we describe a new strategy to access orthogonally protected 3-deoxy-3-fluoro- galactopyranose and acetylated 4-deoxy-4-fluoro-galactopyranose. Starting from inexpensive levoglucosan, most reactions were performed on gram scale, allowed excellent regio- and stereocontrol with a minimal use of protection/deprotection cycles. Hence, we developed practical alternatives to the decade-long reported method to access both 3-deoxy-3-fluoro- and 4-deoxy-4-fluoro-galactopyranose...
April 18, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28419749/novel-19-f-mrs-%C3%AE-galactosidase-reporter-molecules-incorporated-nitrogen-mustard-analogues
#12
Zijun Yu, Jianru Zhao, Zhiming Hua, Xinping Wang, Xiaobo Wang, Hanqin Wang, Jian-Xin Yu
In this paper, we propose a novel molecular platform integrated fluorinated antitumor nitrogen mustards for (19) F-MRS assay of β-galactosidase (β-gal) activity. Following this idea, we have designed, synthesized and characterized 2-fluoro-4-[bis(2'-chloroethyl)amino]phenyl β-D-galactopyranoside 5, 2-fluoro-4-{bis[2'-O-(β-D-galactopyranosyl)ethyl]amino}phenyl β-D-galactopyranoside 8, 2-fluoro-4-{bis[[1''-(β-D-galactopyranosyl)-1'', 2'', 3''-triazol-4''-yl]methyl] amino}phenyl β-D-galactopyranoside 14 and 2-fluoro-4-{bis[[1''-(β-D-glucopyranosyl)-1'', 2'', 3''-triazol-4''-yl]methyl]amino}phenyl β-D-galactopyranoside 15 through glycosylation and click reaction strategies, and their structures were confirmed by NMR and HRMS or elemental analysis data...
April 16, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28419645/diagnostic-performance-of-different-imaging-modalities-in-the-assessment-of-distant-metastasis-and-local-recurrence-of-tumor-in-patients-with-non-small-cell-lung-cancer
#13
Yoshiharu Ohno, Takeshi Yoshikawa, Yuji Kishida, Shinichiro Seki, Hisanobu Koyama, Masao Yui, Yoshimori Kassai, Kota Aoyagi, Shigeo Kaminaga, Kazuro Sugimura
PURPOSE: To compare the diagnostic performance of positron emission tomography with [18F] fluoro-2-deoxy-glucose (FDG-PET) coregistered with magnetic resonance imaging (FDG-PET/MRI), MRI with and without diffusion-weighted imaging (DWI), FDG-PET fused with computed tomography (FDG-PET/CT) with brain contrast-enhanced (CE-) MRI, and routine radiological examination for assessment of postoperative recurrence in nonsmall-cell lung cancer (NSCLC) patients. MATERIALS AND METHODS: 96 consecutive postoperative NSCLC patients (52 men, 44 women; mean age 72 years) prospectively underwent whole-body 3T MRI with and without DWI; PET/CTs and routine radiological examinations consisted of CE-brain MRI, whole-body CE-CT, and bone scintigraphy...
April 17, 2017: Journal of Magnetic Resonance Imaging: JMRI
https://www.readbyqxmd.com/read/28417855/optimization-of-pediatric-pet-ct
#14
REVIEW
Marguerite T Parisi, Mohammed S Bermo, Adam M Alessio, Susan E Sharp, Michael J Gelfand, Barry L Shulkin
PET/CT, the most common form of hybrid imaging, has transformed oncologic imaging and is increasingly being used for nononcologic applications as well. Performing PET/CT in children poses unique challenges. Not only are children more sensitive to the effects of radiation than adults but, following radiation exposure, children have a longer postexposure life expectancy in which to exhibit adverse radiation effects. Both the PET and CT components of the study contribute to the total patient radiation dose, which is one of the most important risks of the study in this population...
May 2017: Seminars in Nuclear Medicine
https://www.readbyqxmd.com/read/28413749/targeted-fluoro-positioning-for-the-discovery-of-a-potent-and-highly-selective-matrix-metalloproteinase-inhibitor
#15
Thomas Fischer, Rainer Riedl
The incorporation of fluorine atoms into functional molecules is of wide interest in synthetic organic chemistry as well as cognate disciplines. In particular, in medicinal chemistry, there is a strong desire to positively influence the physicochemical molecular properties of drug compounds by introducing fluorine into biologically active molecules. Here, we present targeted fluoro positioning as the key design principle of converting a weak matrix metalloproteinase-13 (MMP-13) inhibitor into a very potent (IC50=6 nm) and highly selective (selectivity factors of >1000 over MMP-1, 2, 3, 7, 8, 9, 10, 12, 14) inhibitor with excellent plasma and microsomal stability, and no binding to the hERG channel (hERG: human ether-a-go-go related gene)...
April 2017: ChemistryOpen
https://www.readbyqxmd.com/read/28413746/targeted-fluoro-positioning-for-the-discovery-of-a-potent-and-highly-selective-matrix-metalloproteinase-inhibitor
#16
Thomas Fischer, Rainer Riedl
Invited for this month's cover picture is the group of Professor Rainer Riedl from the Institute of Chemistry and Biotechnology at the Zurich University of Applied Sciences (ZHAW), Switzerland. The cover picture depicts the structure-based design of a drug-like small molecule inhibitor of matrix metalloproteinase-13 (MMP-13) with a combined dual binding motif. The targeted introduction of a single fluoro atom was of vital importance for the optimization of the inhibitor. For more details, read the full text of the Communication at 10...
April 2017: ChemistryOpen
https://www.readbyqxmd.com/read/28413317/korean-red-ginseng-improves-atopic-dermatitis-like-skin-lesions-by-suppressing-expression-of-proinflammatory-cytokines-and-chemokines-in%C3%A2-vivo-and-in%C3%A2-vitro
#17
Ji-Ye Kee, Yong-Deok Jeon, Dae-Seung Kim, Yo-Han Han, Jinbong Park, Dong-Hyun Youn, Su-Jin Kim, Kwang Seok Ahn, Jae-Young Um, Seung-Heon Hong
BACKGROUND: The prevalence of allergic inflammatory diseases such as atopic dermatitis (AD), asthma, and allergic rhinitis worldwide has increased and complete recovery is difficult. Korean Red Ginseng, which is the heat-processed root of Panax ginseng Meyer, is widely and frequently used as a traditional medicine in East Asia. In this study, we investigated whether Korean Red Ginseng water extract (RGE) regulates the expression of proinflammatory cytokines and chemokines via the mitogen-activated protein kinases (MAPKs)/nuclear factor kappa B (NF-κB) pathway in allergic inflammation...
April 2017: Journal of Ginseng Research
https://www.readbyqxmd.com/read/28411455/identification-of-3-substituted-6-1-1h-1-2-3-triazolo-4-5-b-pyrazin-1-yl-ethyl-quinoline-derivatives-as-highly-potent-and-selective-mesenchymal-epithelial-transition-factor-c-met-inhibitors-via-metabolite-profiling-based-structural-optimization
#18
Fei Zhao, Le-Duo Zhang, Yu Hao, Na Chen, Rui Bai, Yu-Ji Wang, Chun-Chun Zhang, Gong-Sheng Li, Li-Jun Hao, Chen Shi, Jing Zhang, Yu Mao, Yi Fan, Guang-Xin Xia, Jian-Xin Yu, Yan-Jun Liu
c-Met/HGF signaling pathway plays an important role in cancer progression, and it was considered to be related to poor prognosis and drug resistance. Based on metabolite profiling of (S)-7-fluoro-6-(1-(6-(1-methyl-1H-pyrazol-4-yl)-1H-imidazo[4,5-b]pyrazin-1-yl)ethyl)quinoline (1), a series of 2-substituted or 3-substituted-6-(1-(1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)ethyl)quinoline derivatives was rationally designed and evaluated. Most of the 3-substituted derivatives not only exhibited potent activities in both enzymatic and cellular assays, but also were stable in liver microsomes among different species (human, rat and monkey)...
April 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28410229/in-vivo-evaluation-of-the-effects-of-simultaneous-inhibition-of-glut-1-and-hif-1%C3%AE-by-antisense-oligodeoxynucleotides-on-the-radiosensitivity-of-laryngeal-carcinoma-using-micro-18f-fdg-pet-ct
#19
Li-Fang Shen, Xin Zhao, Shui-Hong Zhou, Zhong-Jie Lu, Kui Zhao, Jun Fan, Min-Li Zhou
PURPOSE: Hypoxia-inducible factor 1α (HIF-1α) and glucose transporter-1 (GLUT-1) are two important hypoxic markers associated with the radioresistance of cancers including laryngeal carcinoma. We evaluated whether the simultaneous inhibition of GLUT-1 and HIF-1α expression improved the radiosensitivity of laryngeal carcinoma. We explored whether the expression of HIF-1α and GLUT-1 was correlated with 2'-deoxy-2'-[18F]fluoro-D-glucose (18F-FDG) uptake and whether 18F-FDG positron emission tomography-computed tomography (PET/CT) was appropriate for early evaluation of the response of laryngeal carcinoma to targeted treatment in vivo...
March 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28408218/synthesis-and-biological-evaluation-of-pyrimidine-derivatives-with-diverse-azabicyclic-ether-amine-as-novel-gpr119-agonist
#20
Zunhua Yang, Yuanying Fang, Haeil Park
A class of novel pyrimidine derivatives bearing diverse conformationally restricted azabicyclic ether/amine were designed, synthesized and evaluated for their GPR119 agonist activities against type 2 diabetes. Most compounds exhibited superior hEC50 values to endogenous lipid oleoylethanolamide (OEA). Analogs with 2-fluoro substitution in the aryl ring showed more potent GPR119 activation than those without fluorine. Especially compound 27m synthesized from endo-azabicyclic alcohol was observed to have the best EC50 value (1...
April 2, 2017: Bioorganic & Medicinal Chemistry Letters
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