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https://www.readbyqxmd.com/read/28105289/development-of-4-heteroarylamino-1-azaspiro-oxazole-5-3-bicyclo-2-2-2-octanes-as-%C3%AE-7-nicotinic-receptor-agonists
#1
Matthew D Hill, Haiquan Fang, H Dalton King, Christiana I Iwuagwu, Ivar M McDonald, James Cook, F Christopher Zusi, Robert A Mate, Ronald J Knox, Debra Post-Munson, Amy Easton, Regina Miller, Kimberley Lentz, Wendy Clarke, Yulia Benitex, Nicholas Lodge, Robert Zaczek, Rex Denton, Daniel Morgan, Linda Bristow, John E Macor, Richard Olson
We describe the synthesis of quinuclidine-containing spiroimidates and their utility as α7 nicotinic acetylcholine receptor (nAChR) partial agonists. A convergent synthetic route allowed for rapid SAR investigation and provided a diverse set of fused 6,5-heteroaryl analogs. Two potent and selective α7 nAChR partial agonists, (1'S,3'R,4'S)-N-(7-bromopyrrolo[2,1-f][1,2,4]triazin-4-yl)-4H-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octan]-2-amine (20) and (1'S,3'R,4'S)-N-(7-chloropyrrolo[2,1-f][1,2,4]triazin-4-yl)-4H-1'-azaspiro[oxazole-5,3'-bicyclo[2...
January 12, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28099902/anthelmintic-mebendazole-enhances-cisplatin-s-effect-on-suppressing-cell-proliferation-and-promotes-differentiation-of-head-and-neck-squamous-cell-carcinoma-hnscc
#2
Fugui Zhang, Yong Li, Hongmei Zhang, Enyi Huang, Lina Gao, Wenping Luo, Qiang Wei, Jiaming Fan, Dongzhe Song, Junyi Liao, Yulong Zou, Feng Liu, Jianxiang Liu, Jiayi Huang, Dan Guo, Chao Ma, Xue Hu, Li Li, Xiangyang Qu, Liqun Chen, Xinyi Yu, Zhicai Zhang, Tingting Wu, Hue H Luu, Rex C Haydon, Jinlin Song, Tong-Chuan He, Ping Ji
Head and neck squamous cell carcinoma (HNSCC) is one of the most common and aggressive types of human cancers worldwide. Nearly a half of HNSCC patients experience recurrence within five years of treatment and develop resistance to chemotherapy. Thus, there is an urgent clinical need to develop safe and novel anticancer therapies for HNSCC. Here, we investigate the possibility of repurposing the anthelmintic drug mebendazole (MBZ) as an anti-HNSCC agent. Using the two commonly-used human HNSCC lines CAL27 and SCC15, we demonstrate MBZ exerts more potent anti-proliferation activity than cisplatin in human HNSCC cells...
January 16, 2017: Oncotarget
https://www.readbyqxmd.com/read/28092267/cryo-em-structure-of-the-atp-sensitive-potassium-channel-illuminates-mechanisms-of-assembly-and-gating
#3
Gregory M Martin, Craig Yoshioka, Emily A Rex, Jonathan F Fay, Qing Xie, Matthew R Whorton, James Z Chen, Show-Ling Shyng
KATP channels are metabolic sensors that couple cell energetics to membrane excitability. In pancreatic β-cells, channels formed by SUR1 and Kir6.2 regulate insulin secretion and are the targets of antidiabetic sulfonylureas. Here, we used cryo-EM to elucidate structural basis of channel assembly and gating. The structure, determined in the presence of ATP and the sulfonylurea glibenclamide, at ~6Å resolution reveals a closed Kir6.2 tetrameric core with four peripheral SUR1s each anchored to a Kir6.2 by its N-terminal transmembrane domain (TMD0)...
January 16, 2017: ELife
https://www.readbyqxmd.com/read/28086825/toxicity-and-quality-of-life-report-of-a-phase-ii-study-of-stereotactic-body-radiotherapy-sbrt-for-low-and-intermediate-risk-prostate-cancer
#4
Matthew J Boyer, Michael A Papagikos, Rex Kiteley, Zeljko Vujaskovic, Jackie Wu, W Robert Lee
BACKGROUND: Clinical data indicates that delivery of larger daily doses of radiation may improve the therapeutic ratio for prostate cancer compared to conventional fractionation. A phase II study of stereotactic body radiotherapy with real-time motion management and daily plan re-optimization for low to intermediate risk prostate cancer was undertaken to evaluate this hypothesis. This report details the toxicity and quality of life following treatment. METHODS: From 2009 to 2013, 60 patients with T1-T2c prostate cancer with a Gleason score of 6 and PSA ≤ 15 or Gleason score of 7 and PSA ≤ 10 were enrolled...
January 13, 2017: Radiation Oncology
https://www.readbyqxmd.com/read/28073562/a-new-gambierdiscus-species-dinophyceae-from-rarotonga-cook-islands-gambierdiscus-cheloniae-sp-nov
#5
Kirsty F Smith, Lesley Rhodes, Arjun Verma, Belinda G Curley, D Tim Harwood, Gurjeet S Kohli, Dorothy Solomona, Teina Rongo, Rex Munday, Shauna A Murray
Ciguatera fish poisoning (CFP) has been reported for many years in Rarotonga, Cook Islands, and has had the world's highest reported incidence of this illness for the last 20 years. Following intensive sampling to understand the distribution of the causative organisms of CFP, an undescribed Gambierdiscus species was isolated from the Rarotongan lagoon. Gambierdiscus cheloniae sp. nov. has the common Gambierdiscus Kofoidian plate formula (except for a variability in the number of precingular plates in aberrant cells): Po, 3', 6″ (7″), 6C?, 6 or 7S, 5'″, 1p and 2″″...
December 2016: Harmful Algae
https://www.readbyqxmd.com/read/28073543/corrigendum-to-production-of-ciguatoxin-and-maitotoxin-by-strains-of-gambierdiscus-australes-g-pacificus-and-g-polynesiensis-dinophyceae-isolated-from-rarotonga-cook-islands-harmful-algae-39-2014-185-190
#6
https://www.readbyqxmd.com/read/28071653/prophylactic-orthosteric-inhibition-of-leukocyte-integrin-cd11b-cd18-prevents-long-term-fibrotic-kidney-failure-in-cynomolgus-monkeys
#7
Abbas Dehnadi, A Benedict Cosimi, Rex Neal Smith, Xiangen Li, José L Alonso, Terry K Means, M Amin Arnaout
Ischaemic acute kidney injury (AKI), an inflammatory disease process, often progresses to chronic kidney disease (CKD), with no available effective prophylaxis. This is in part due to lack of clinically relevant CKD models in non-human primates. Here we demonstrate that inhibition of the archetypal innate immune receptor CD11b/CD18 prevents progression of AKI to CKD in cynomolgus monkeys. Severe ischaemia-reperfusion injury of the right kidney, with subsequent periods of the left ureter ligation, causes irreversible right kidney failure 3, 6 or 9 months after AKI...
January 10, 2017: Nature Communications
https://www.readbyqxmd.com/read/28070874/infection-of-defective-human-t-lymphotropic-virus-type-1
#8
Yuuki Hashikura, Kazumi Umeki, Kunihiko Umekita, Hajime Nomura, Akiteru Yamada, Ikuo Yamamoto, Hiroo Hasegawa, Katsunori Yanagihara, Akihiko Okayama
In a previous study, we reported that an identical defective provirus had integrated into multiple sites of the genome of a representative human T-lymphotropic virus type 1 (HTLV-1) cell line, MT-2. A possible explanation for this may be the repeated infection of this defective provirus to a cell. Therefore, we attempted to determine whether a defective provirus could transmit during the co-culture of HTLV-1 uninfected human T-cell line, Jurkat, with MT-2 cells treated with mitomycin C. As a result, we established not only a cell line with the integration of one complete provirus, but also a cell line with the integration of one defective provirus...
January 9, 2017: Human Cell
https://www.readbyqxmd.com/read/28066944/the-effect-of-lactobacillus-isolates-on-growth-performance-immune-response-intestinal-bacterial-community-composition-of-growing-rex-rabbits
#9
REVIEW
C Wang, Y Zhu, F Li, L Huang
The objective of this experiment was to investigate the effect of Lactobacillus isolates on intestinal bacterial community composition of growing Rex Rabbits. A total of 120 weaned Rex Rabbits (30 days old, 30 per group) were used for the experiment, which started after an adaptation period of 7 days. The control group was fed with basal diet only, while the treatment I, II and III groups were fed with basal diet adding antibiotics, Lactobacillus zeae (LB1) and Lactobacillus casei (L3) respectively. Growth performance, immune response and intestinal flora have been examined...
January 8, 2017: Journal of Animal Physiology and Animal Nutrition
https://www.readbyqxmd.com/read/28066798/an-ngago-tool-for-genome-editing-did-crispr-cas9-just-find-a-competitor
#10
Qiang Wei, Junyi Liao, Xinyi Yu, Eric J Wang, Claire Wang, Hue H Luu, Rex C Haydon, Michael J Lee, Tong-Chuan He
While CRISPR/Cas9-mediated genome editing technology has been experiencing a rapid transformation during the past few years, a recent report on NgAgo-mediated single-stranded DNA-guided genome editing may offer an attractive alternative for genome manipulation. While it's too early to predict whether NgAgo will be able to compete with or be superior to CRISPR/Cas9, the scientific community is anxiously waiting for further optimization and broader applications of the NgAgo genome editing technology.
September 2016: Genes & Diseases
https://www.readbyqxmd.com/read/28066604/shifted-focus-of-bronchoalveolar-lavage-in-patients-with-suspected-thoracic-malignancy-an-analysis-of-224-patients
#11
Xin Zhang, Yukun Kuang, Yuan Zhang, Kai He, Noah Lechtzin, Mingying Zeng, Rex C Yung, Canmao Xie
BACKGROUND: Bronchoscopies are extensively adopted for diagnosing and staging thoracic malignancies, but studies are missing as how to keep the process streamlined and more efficient. To evaluate current role of bronchoalveolar lavage (BAL) for cancer and possible infection diagnosis when practicing comprehensive bronchoscopy for patients suspected with thoracic malignancy, and provide foundation for possible practice modification. METHODS: We retrospectively analyzed a prospectively kept database of immunocompetent patients undergoing bronchoscopy for suspected non-hematologic malignancies...
November 2016: Journal of Thoracic Disease
https://www.readbyqxmd.com/read/28064413/journal-of-clinical-monitoring-and-computing-2016-end-of-year-summary-cardiovascular-and-hemodynamic-monitoring
#12
REVIEW
Bernd Saugel, Karim Bendjelid, Lester A Critchley, Steffen Rex, Thomas W L Scheeren
The assessment and optimization of cardiovascular and hemodynamic variables is a mainstay of patient management in the care for critically ill patients in the intensive care unit (ICU) or the operating room (OR). It is, therefore, of outstanding importance to meticulously validate technologies for hemodynamic monitoring and to study their applicability in clinical practice and, finally, their impact on treatment decisions and on patient outcome. In this regard, the Journal of Clinical Monitoring and Computing (JCMC) is an ideal platform for publishing research in the field of cardiovascular and hemodynamic monitoring...
February 2017: Journal of Clinical Monitoring and Computing
https://www.readbyqxmd.com/read/28063319/quantitative-analysis-of-the-extent-of-heavy-metal-contamination-in-soils-near-picher-oklahoma-within-the-tar-creek-superfund-site
#13
Rachelle E Beattie, Wyatt Henke, Conor Davis, M Abdul Mottaleb, James H Campbell, L Rex McAliley
The Tri-State Mining District of Missouri, Kansas and Oklahoma was the site of large-scale mining operations primarily for lead and zinc until the mid-1950s. Although mining across the area has ceased, high concentrations of heavy metals remain in the region's soil and water systems. The town of Picher, Ottawa County, OK, lies within this district and was included in the Tar Creek Superfund Site by the U.S. Environmental Protection Agency in 1980 due to extensive contamination. To elucidate the extent of heavy-metal contamination, a soil-chemistry survey of the town of Picher was conducted...
December 31, 2016: Chemosphere
https://www.readbyqxmd.com/read/28058609/ontogenetic-and-evolutionary-trends-in-the-tooth-enamel-features-in-craseomys-voles-arvicolinae-rodentia
#14
M A Fominykh, S V Zykov, A V Borodin
In Craseomys rufocanus and Craseomys rex, the age-related and species differences in thickness and microstructure of the first lower molars (ml) have been identified and studied. The results suggest that the enamel dimensional and microstructural features may serve as additional indicators of the vole tooth evolutionary stage within a single phyletic lineage.
November 2016: Doklady Biological Sciences: Proceedings of the Academy of Sciences of the USSR, Biological Sciences Sections
https://www.readbyqxmd.com/read/28058518/father-participation-in-child-psychopathology-research
#15
Justin Parent, Rex Forehand, Hayley Pomerantz, Virginia Peisch, Martin Seehuus
The purpose of the current study was two-fold: (1) To examine time trends of the inclusion of fathers in child psychopathology research from 2005 to 2015; and (2) to examine online crowdsourcing as a method to recruit and study fathers. In study 1, findings indicated that, relative to two earlier reviews of father participation from 1984 to 1991 and 1992-2004, there has been limited progress in the inclusion of fathers in child psychopathology research over the last decade. In study 2, without explicit efforts to recruit fathers, almost 40% of a sample of 564 parents recruited from online crowdsourcing (Amazon's Mechanical Turk) were fathers...
January 5, 2017: Journal of Abnormal Child Psychology
https://www.readbyqxmd.com/read/28049197/venous-air-embolism-during-hysteroscopic-myomectomy-an-analysis-of-7-cases
#16
Cédric Van Dijck, Steffen Rex, Jasper Verguts, Dirk Timmerman, Marc Van de Velde, An Teunkens
Venous air embolism (VAE) is a rare but potentially fatal complication of hysteroscopic myomectomy. The symptoms of VAE range from mild and clinically insignificant to complete cardiovascular collapse during surgery. Anesthesiologists and surgeons should be aware of the clinical characteristics and predisposing factors of this possible adverse event. This report analyzes 7 cases of VAE, which occurred at the University Hospitals Leuven, in patients undergoing hysteroscopic myomectomy from April 2009 to April 2011...
January 4, 2017: Gynecologic and Obstetric Investigation
https://www.readbyqxmd.com/read/28048106/su-f-i-78-design-of-diagnostic-multileaf-collimator-based-on-the-monte-carlo-simulation-for-dose-reduction-of-diagnostic-radiography
#17
S Han, Y Ji, K Kim, S Choi, H Jung, S Park
PURPOSE: A diagnostics Multileaf Collimator (MLC) was designed for diagnostic radiography dose reduction. Monte Carlo simulation was used to evaluate efficiency of shielding material for producing leaves of Multileaf collimator. MATERIAL & METHODS: The general radiography unit (Rex-650R, Listem, Korea) was modeling with Monte Carlo simulation (MCNPX, LANL, USA) and we used SRS-78 program to calculate the energy spectrum of tube voltage (80, 100, 120 kVp). The shielding materials was SKD 11 alloy tool steel that is composed of 1...
June 2016: Medical Physics
https://www.readbyqxmd.com/read/28045719/hepatic-histology-and-morphometric-measurements-in-idiopathic-extrahepatic-portal-vein-thrombosis-in-children-correlated-to-clinical-outcome-of-meso-rex-bypass
#18
Niramol Tantemsapya, Riccardo Superina, Deli Wang, Grace Kronauer, Peter F Whitington, Hector Melin-Aldana
OBJECTIVE: The aim of this study was to correlate clinical, histologic, and morphometric features of the liver in children with extrahepatic portal vein thrombosis (EHPVT), with surgical outcome after Meso-Rex bypass (MRB). BACKGROUND: Idiopathic EHPVT, a significant cause of portal hypertension, is surgically corrected by MRB. Correlation of histologic and morphometric features of the liver with outcome has not been reported in children. METHODS: We retrospectively reviewed clinical and intraoperative data of 45 children with idiopathic EHPVT...
December 30, 2016: Annals of Surgery
https://www.readbyqxmd.com/read/28043204/safety-of-gelatin-solutions-for-the-priming-of-cardiopulmonary-bypass-in-cardiac-surgery-a-systematic-review-and-meta-analysis
#19
Idris Ghijselings, Dirk Himpe, Steffen Rex
This systematic review and meta-analysis was conducted to evaluate the safety of gelatin versus hydroxyethyl starches (HES) and crystalloids when used for cardiopulmonary bypass (CPB)-priming in cardiac surgery. MEDLINE (Pubmed), Embase and CENTRAL were searched. We included only randomized, controlled trials comparing CPB-priming with gelatin with either crystalloids or HES-solutions of the newest generation. The primary endpoint was the blood loss during the first 24 hours. Secondary outcomes included perioperative transfusion requirements, postoperative kidney function, postoperative ventilation times and length of stay on the intensive care unit...
December 1, 2016: Perfusion
https://www.readbyqxmd.com/read/28042390/outcomes-of-submucosal-t1b-esophageal-adenocarcinomas-removed-by-endoscopic-mucosal-resection
#20
Darren D Ballard, Neel Choksi, Jingmei Lin, Eun-Young Choi, B Joseph Elmunzer, Henry Appelman, Douglas K Rex, Hala Fatima, William Kessler, John M DeWitt
AIM: To investigate the outcomes and recurrences of pT1b esophageal adenocarcinoma (EAC) following endoscopic mucosal resection (EMR) and associated treatments. METHODS: Patients undergoing EMR with pathologically confirmed T1b EAC at two academic referral centers were retrospectively identified. Patients were divided into 4 groups based on treatment following EMR: Endoscopic therapy alone (group A), endoscopic therapy with either chemotherapy, radiation or both (group B), surgical resection (group C) or no further treatment/lost to follow-up (< 12 mo) (group D)...
December 16, 2016: World Journal of Gastrointestinal Endoscopy
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