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https://www.readbyqxmd.com/read/27911800/an-%C3%AE-%C3%AE-hydrolase-fold-protein-in-the-biosynthesis-of-thiostrepton-exhibits-a-dual-activity-for-endopeptidyl-hydrolysis-and-epoxide-ring-opening-macrocyclization
#1
Qingfei Zheng, Shoufeng Wang, Panpan Duan, Rijing Liao, Dandan Chen, Wen Liu
Thiostrepton (TSR), an archetypal bimacrocyclic thiopeptide antibiotic that arises from complex posttranslational modifications of a genetically encoded precursor peptide, possesses a quinaldic acid (QA) moiety within the side-ring system of a thiopeptide-characteristic framework. Focusing on selective engineering of the QA moiety, i.e., by fluorination or methylation, we have recently designed and biosynthesized biologically more active TSR analogs. Using these analogs as chemical probes, we uncovered an unusual indirect mechanism of TSR-type thiopeptides, which are able to act against intracellular pathogens through host autophagy induction in addition to direct targeting of bacterial ribosome...
November 23, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27910989/catalytic-asymmetric-aldol-addition-reactions-of-3-fluoro-indolinone-derived-enolates
#2
Lijun Zhang, Wenzhong Zhang, Haibo Mei, Jianlin Han, Vadim A Soloshonok, Yi Pan
Reported herein is a Cu(i)/bisoxazoline ligand-catalyzed aldol reaction of unprotected tertiary enolates generated in situ from 3-(1,1-dihydroxy-2,2,2-trifluoroethyl)-substituted derivatives of 3-fluoro-2-oxindoles. A range of α-fluoro-β-aryl/hetaryl/alkyl-β-hydroxy-indolin-2-ones containing C-F quaternary stereogenic centers of high pharmaceutical importance were furnished in good yields and satisfactory diastereo- and enantioselectivities. The reactions were conducted under operationally convenient conditions and displayed wide substrate/functional group generality including unprotected N-H on the tertiary enolates, and aromatic, hetero-aromatic and aliphatic aldehydes...
December 2, 2016: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/27908969/synthesis-and-evaluation-of-the-new-estrogen-receptor-%C3%AE-selective-radioligand-18f-fhnp-comparison-with-18f-fes
#3
Inês F Antunes, Aren van Waarde, Rudi A Dierckx, Elisabeth G E de Vries, Geke A P Hospers, Erik F de Vries
: Estrogen receptors (ER) are targets for endocrine treatment of estrogen-dependent cancers. The ER consists of 2 isoforms, ERα and ERβ, which have distinct biological functions. While activation of ERα stimulates cell proliferation and cell survival, ERβ promotes apoptosis. Positron emission tomography (PET) of ERα and ERβ levels could provide more insight in response to hormonal treatment. 16α-(18)F-Fluoro-17β-estradiol ((18)F-FES) is a PET tracer for ER with relative selectivity for ERα...
December 1, 2016: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/27908580/antimicrobial-activity-of-novel-4h-4-oxoquinolizine-compounds-against-extensively-drug-resistant-acinetobacter-baumannii-strains
#4
Seok Hyeon Na, Hyejin Jeon, Yoo Jeong Kim, Hyo Il Kwon, Gati Noble Selasi, Asiimwe Nicholas, Chang-Soo Yun, Sang Ho Lee, Je Chul Lee
The aim of this study was to screen lead compounds exhibiting potent in vitro antimicrobial activity against multidrug-resistant (MDR) Acinetobacter baumannii strains from a library of chemical compounds. In a high-throughput screening analysis of 7520 compounds representative of 340,000 small molecules, two 4H-4-oxoquinolizine compounds were the most active against A. baumannii ATCC 17978. Subsequent selection and analysis of 70 4H-4-oxoquinolizine compounds revealed that the top 7 compounds were extremely active against extensively drug-resistant (XDR) A...
November 21, 2016: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/27908268/synthesis-of-new-fluoro-benzimidazole-derivatives-as-an-approach-towards-the-discovery-of-novel-intestinal-antiseptic-drug-candidates
#5
Ulviye Acar, Begüm Nurpelin Sağlık, Yusuf Özkay, Zerrin Cantürk, Juan Bueno, Fatih Demirci
In the present study, nineteen new fluoro-benzimidazole derivatives, including nifuroxazide analogues, were synthesized by microwave-supported reactions and tested against a panel of pathogenic microorganisms consisting of resistant strains. The synthesized compounds were characterised and identified by FT-IR, 1H- and 13C-NMR, mass spectroscopy, and elemental analyses, respectively. In vitro antimicrobial and cytotoxic effects of the synthesized compounds were determined by microdilution and by [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] (MTT) assay...
December 1, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27905592/the-conformational-landscape-of-2-4-fluoro-phenyl-ethylamine-consequences-of-fluorine-substitution-at-the-para-position
#6
Afik Shachar, Nitzan Mayorkas, Hanan Sachs, Ilana Bar
Fluorination is considered as a possible means for alteration of conformational landscapes in molecules. The effect of fluorine substitution was studied here by measuring the vibronic and vibrational spectra of gas phase 2-(4-fluoro-phenyl)-ethylamine (4-FPEA) by resonant two-photon ionization (R2PI) and by ionization-loss stimulated Raman spectroscopy (ILSRS). The measurement of survey ILSR spectra of 4-FPEA in the amino group region allowed to associate the bands in the R2PI spectrum to origin and vibronic transitions of the ground (S0) to the excited (S1) electronic states of three different conformers...
December 1, 2016: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/27903546/positron-emission-tomography-fluorine-18-labeled-2-deoxy-2-fluoro-d-glucose-tells-a-complicated-story-in-the-aortic-aneurysm-wall
#7
EDITORIAL
John A Curci, Joshua A Beckman
No abstract text is available yet for this article.
November 2016: Circulation. Cardiovascular Imaging
https://www.readbyqxmd.com/read/27903534/high-structural-stress-and-presence-of-intraluminal-thrombus-predict-abdominal-aortic-aneurysm-18f-fdg-uptake-insights-from-biomechanics
#8
Yuan Huang, Zhongzhao Teng, Maysoon Elkhawad, Jason M Tarkin, Nikhil Joshi, Jonathan R Boyle, John R Buscombe, Timothy D Fryer, Yongxue Zhang, Ah Yeon Park, Ian B Wilkinson, David E Newby, Jonathan H Gillard, James H F Rudd
BACKGROUND: Abdominal aortic aneurysm (AAA) wall inflammation and mechanical structural stress may influence AAA expansion and lead to rupture. We hypothesized a positive correlation between structural stress and fluorine-18-labeled 2-deoxy-2-fluoro-d-glucose ((18)F-FDG) positron emission tomography-defined inflammation. We also explored the influence of computed tomography-derived aneurysm morphology and composition, including intraluminal thrombus, on both variables. METHODS AND RESULTS: Twenty-one patients (19 males) with AAAs below surgical threshold (AAA size was 4...
November 2016: Circulation. Cardiovascular Imaging
https://www.readbyqxmd.com/read/27901472/effects-of-low-and-high-deprenyl-dose-on-antioxidant-enzyme-activities-in-the-adult-rat-brain
#9
Maria Lalkovicova, Frantiska Horvathova, Igor Sulla, Jozef Mihalik, Viera Danielisova
We evaluated the effects of low dose deprenyl (LDD, 0.0025 mg/kg per day) and high dose deprenyl (HDD, 0.25 mg/kg per day) treatment of male Wistar rats for 30 days on the activities of SOD and CAT in the cortex, striatum, and hippocampus. Total SOD and MnSOD activities were increased with LDD (p <0.05) in the cortex (0.74 ± 0.03; 0.31 ± 0.02), striatum (0.75 ± 0.02; 0.27 ± 0.03) and CA1 region of the hippocampus (0.75 ± 0.02; 0.29 ± 0.03) compared to the control (0.53 ± 0.02; 0.15 ± 0.02), but reduced (p <0...
November 30, 2016: General Physiology and Biophysics
https://www.readbyqxmd.com/read/27900591/treatment-of-lung-tumours-with-high-energy-microwave-ablation-a-single-centre-experience
#10
Anna Maria Ierardi, Andrea Coppola, Natalie Lucchina, Gianpaolo Carrafiello
The purpose of our study is to report safety, technical success, effectiveness, local progression-free survival (LPFS) and overall survival of percutaneous microwave ablation (MWA) to treat lung tumours unsuitable for surgery. Nineteen patients with thirty-one tumours (mean diameter 2.4 cm) underwent percutaneous MWA in 28 sessions. Microwave ablation was carried out using a 2450-MHz generator (Emprint/Covidien, Boulder, CO, USA). Procedures were performed under cone-beam CT (CBCT) and under fluoro-CT (one session) guidance...
January 2017: Medical Oncology
https://www.readbyqxmd.com/read/27900005/fluoro-edenite-induces-fibulin-3-overexpression-in-non-malignant-human-mesothelial-cells
#11
Venerando Rapisarda, Rossella Salemi, Andrea Marconi, Carla Loreto, Adriana C Graziano, Venera Cardile, Maria S Basile, Saverio Candido, Luca Falzone, Demetrios A Spandidos, Concettina Fenga, Massimo Libra
Exposure to asbestos is associated with the development of mesothelioma. In addition to asbestos, other fibers have been identified as risk factors for malignant and non-malignant diseases of the lungs. Among these, fluoro-edenite (FE) was found in patients from Biancavilla (Sicily, Italy) with pleural and lung disease, suggesting its role for tumor expansion. In this context, the identification of early biomarkers useful for the diagnosis of cancer is mandatory. Fibulin-3 represents an important marker for the diagnosis of mesothelioma...
November 2016: Oncology Letters
https://www.readbyqxmd.com/read/27896836/radiosynthesis-and-biological-evaluation-of-the-new-pde10a-radioligand-18-f-aq28a
#12
Sally Wagner, Rodrigo Teodoro, Winnie Deuther-Conrad, Mathias Kranz, Matthias Scheunemann, Steffen Fischer, Barbara Wenzel, Ute Egerland, Norbert Hoefgen, Jörg Steinbach, Peter Brust
Cyclic nucleotide phosphodiesterase 10A (PDE10A) regulates the level of the second messengers cAMP and cGMP in particular in brain regions assumed to be associated with neurodegenerative and psychiatric diseases. A better understanding of the pathophysiological role of the expression of PDE10A could be obtained by quantitative imaging of the enzyme by positron emission tomography (PET). Thus, in this study we developed, radiolabeled, and evaluated a new PDE10A radioligand, 8-bromo-1-(6-[(18) F]fluoropyridin-3-yl)-3,4-dimethylimidazo[1,5-a]quinoxaline ([(18) F]AQ28A)...
November 29, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/27896807/fdg-pet-ct-imaging-of-therapeutic-response-in-granulomatous-lymphocytic-interstitial-lung-disease-glild-in-common-variable-immunodeficiency-cvid
#13
S Jolles, E Carne, M Brouns, T El-Shanawany, P Williams, C Marshall, P Fielding
Common variable immunodeficiency (CVID) is the most common severe adult primary immunodeficiency and is characterized by a failure to produce antibodies leading to recurrent predominantly sinopulmonary infections. Improvements in the prevention and treatment of infection with immunoglobulin replacement and antibiotics have resulted in malignancy, autoimmune, inflammatory and lymphoproliferative disorders emerging as major clinical challenges in the management of patients who have CVID. In a proportion of CVID patients, inflammation manifests as granulomas that frequently involve the lungs, lymph nodes, spleen and liver and may affect almost any organ...
November 28, 2016: Clinical and Experimental Immunology
https://www.readbyqxmd.com/read/27895731/advantages-and-disadvantages-of-f-18-fluorodeoxyglucose-positron-emission-tomography-computed-tomography-in-carcinoma-of-unknown-primary
#14
Xiaozhou Yu, Xiaofeng Li, Xiuyu Song, Dong Dai, Lei Zhu, Yanjia Zhu, Jian Wang, Huiqin Zhao, Wengui Xu
Carcinoma of unknown primary is a type of malignant disease where the primary carcinoma cannot be identified by conventional examination, which presents challenges in diagnosis and therapy. This study aims to evaluate the detailed clinical value and indications of using fluorine-18-2-fluoro-2-deoxy-D-glucose positron emission tomography/computed tomography (F-18 FDG PET/CT) in a large sample. A total of 449 patients who were selected under strict standards were retrospectively included in this study. F-18 FDG PET/CT accurately detected the primary carcinoma in 115 of 449 patients whose primaries could not be detected by conventional examination (25...
November 2016: Oncology Letters
https://www.readbyqxmd.com/read/27895434/bay-41-2272-treatment-improves-acetylcholine-induced-aortic-relaxation-in-l-name-hypertensive-rats
#15
Shahid Prawez, Azad Ahmad Ahanger, Thakur Uttam Singh, Santosh Kumar Mishra, Souvendra Nath Sarkar, Dinesh Kumar
Hypertension, an emerging problem of recent era, and many pathophysiological factors are participating to produce the disease. Nitric oxide (NO) is an important constituent to ameliorate hypertensive condition. Inhibition of endogenous NO synthase by L-N(G)-Nitroarginine methyl ester (L-NAME) was responsible for generating hypertension in rats. BAY 41-2272 (5-cyclopropyl-2-[1-(2-fluoro-benzyl)-1H-pyrazolo[3,4-b]pyridine-3-yl]-pyrimidin-4-ylamine), a soluble guanylyl cyclase activator, restricts rise of blood pressure and shows cardioprotective activity...
December 2016: International Journal of Angiology: Official Publication of the International College of Angiology, Inc
https://www.readbyqxmd.com/read/27895137/successful-response-to-pegylated-interferon-alpha-in-a-recurrent-paraganglioma
#16
Thibault Bahougne, Alessio Imperiale, Gerlinde Averous, Gerard Chabrier, Nelly Burnichon, Anne-Paule Gimenez-Roqueplo, Nassim Dali-Youcef, Rossella Libé, Eric Baudin, Catherine Roy, Herve Lang, Laurence Kessler
INTRODUCTION: Early and accurate identification of recurrences in patients with aggressive paraganglioma (PGL) poses significant challenges. Moreover, the most appropriate therapeutic strategy for recurrent PGL remains to be established. RESULTS: We report the case of 52-year-old man with a history of recurrent, sporadic, left retroperitoneal PGL that relapsed twice (at eight and nine years after the first surgical intervention). At the time of the second recurrence, 2-deoxy-2-[fluorine-18]fluoro-D-glucose (FDG) positron emission tomography/computed tomography (PET/CT) demonstrated a pathologically increased tracer uptake in multiple nodular lesions (10-15 mm in size) located close to the remnant of the left renal pedicle and in the left lombar paravertebral region...
November 28, 2016: Endocrine-related Cancer
https://www.readbyqxmd.com/read/27889577/brain-uptake-and-metabolism-of-the-endocannabinoid-anandamide-labeled-in-either-the-arachidonoyl-or-ethanolamine-moiety
#17
Kun Hu, Shilpa Sonti, Sherrye T Glaser, Richard I Duclos, Samuel J Gatley
INTRODUCTION: Anandamide (N-arachidonoylethanolamine) is a retrograde neuromodulator that activates cannabinoid receptors. The concentration of anandamide in the brain is controlled by fatty acid amide hydrolase (FAAH), which has been the focus of recent drug discovery efforts. Previous studies in C57BL/6 mice using [(3)H-arachidonoyl]anandamide demonstrated deposition of tritium in thalamus and cortical areas that was blocked by treatment with an FAAH inhibitor and that was not seen in FAAH-knockout mice...
November 9, 2016: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/27889414/changes-in-glucose-induced-plasma-active-glucagon-like-peptide-1-levels-by-co-administration-of-sodium-glucose-cotransporter-inhibitors-with-dipeptidyl-peptidase-4-inhibitors-in-rodents
#18
Takahiro Oguma, Chiaki Kuriyama, Keiko Nakayama, Yasuaki Matsushita, Kumiko Hikida, Minoru Tsuda-Tsukimoto, Akira Saito, Kenji Arakawa, Kiichiro Ueta, Masabumi Minami, Masaharu Shiotani
We investigated whether structurally different sodium-glucose cotransporter (SGLT) 2 inhibitors, when co-administered with dipeptidyl peptidase-4 (DPP4) inhibitors, could enhance glucagon-like peptide-1 (GLP-1) secretion during oral glucose tolerance tests (OGTTs) in rodents. Three different SGLT inhibitors-1-(β-d-Glucopyranosyl)-4-chloro-3-[5-(6-fluoro-2-pyridyl)-2-thienylmethyl]benzene (GTB), TA-1887, and canagliflozin-were examined to assess the effect of chemical structure. Oral treatment with GTB plus a DPP4 inhibitor enhanced glucose-induced plasma active GLP-1 (aGLP-1) elevation and suppressed glucose excursions in both normal and diabetic rodents...
October 28, 2016: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/27889090/focal-nodular-and-diffuse-haematopoietic-marrow-hyperplasia-in-patients-with-underlying-malignancies-a-radiological-mimic-of-malignancy-in-need-of-recognition
#19
L T C Chow, A W H Ng, S K C Wong
AIM: To report the authors' experience of focal nodular haematopoietic marrow hyperplasia (FNHMH) and diffuse haematopoietic marrow hyperplasia (DHMH) clinically masquerading as skip, distant, or disseminated metastasis in seven patients with underlying malignant neoplasms. MATERIALS AND METHODS: Five patients with FNHMH and two with DHMH mistaken radiologically as skip and disseminated metastasis, respectively, were compared and contrasted with four patients with osteosarcomas and two with chondrosarcomas harbouring skip metastasis, noting the temporal relationship with their haematological profile...
November 24, 2016: Clinical Radiology
https://www.readbyqxmd.com/read/27886621/evaluation-of-two-nucleophilic-syntheses-routes-for-the-automated-synthesis-of-6-18-f-fluoro-l-dopa
#20
Marc Pretze, Dominic Franck, Falk Kunkel, Erich Foßhag, Carmen Wängler, Björn Wängler
Two different strategies for the nucleophilic radiosynthesis of [(18)F]F-DOPA were evaluated regarding their applicability for an automated routine production on an Ecker&Ziegler Modular-Lab Standard module. Initially, we evaluated a promising 5-step synthesis based on a chiral, cinchonidine-derived phase-transfer catalyst (cPTC) being described to give the product in high radiochemical yields (RCY), high specific activities (AS) and high enantiomeric excesses (ee). However, the radiosynthesis of [(18)F]F-DOPA based on this strategy showed to be highly complex, giving the intermediate products as well as the final product in insufficient yields for automatization...
October 27, 2016: Nuclear Medicine and Biology
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