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https://www.readbyqxmd.com/read/28210740/catalyst-free-synthesis-of-%C3%AE-fluoro-%C3%AE-hydroxy-ketones-%C3%AE-fluoro-ynols-via-electrophilic-fluorination-of-tertiary-propargyl-alcohols-using-selectfluor%C3%A2-f-teda-bf4
#1
Naganaboina Naveen, Rengarajan Balamurugan
A facile method for the synthesis of α-fluoro-β-hydroxy ketones/α-fluoro-ynols from tertiary propargyl alcohols under electrophilic fluorination conditions using F-TEDA-BF4 has been presented. The products bear pharmaceutically important α-fluoro ketone, gem-diaryl and fluorohydrin moieties in the same molecule. Interestingly, this catalyst free protocol results in monofluorination.
February 17, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28209720/acquired-expression-of-cbl-q367p-in-mice-induces-dysplastic-myelopoiesis-mimicking-chronic-myelomonocytic-leukemia
#2
Yuichiro Nakata, Takeshi Ueda, Akiko Nagamachi, Norimasa Yamasaki, Ken-Ichiro Ikeda, Yasuyuki Sera, Keiyo Takubo, Akinori Kanai, Hideaki Oda, Masashi Sanada, Seishi Ogawa, Kohichiro Tsuji, Yasuhiro Ebihara, Linda Wolff, Zen-Ichiro Honda, Toshio Suda, Toshiya Inaba, Hiroaki Honda
Chronic myelomonocytic leukemia (CMML) is a hematological malignancy characterized by uncontrolled proliferation of dysplastic myelomonocytes and frequent progression to acute myeloid leukemia (AML). We identified mutations in the Cbl gene, which encodes a negative regulator of cytokine signaling, in a subset of CMML patients. To investigate the contribution of mutant Cbl in CMML pathogenesis, we generated conditional knock-in mice for Cbl that express wild-type Cbl in a steady state and inducibly express Cbl(Q367P) , a CMML-associated Cbl mutant...
February 16, 2017: Blood
https://www.readbyqxmd.com/read/28202750/careers-in-virology-working-at-the-centers-for-disease-control-and-prevention
#3
Jennifer L Konopka-Anstadt, Cara C Burns
As non-academic careers in science have become less and less "alternative," one field that has consistently attracted early-career virologists is public health research. The desire to make tangible contributions towards public health needs and better protect the public from infectious disease often motivate the transition. In this Career Gem, two academically-trained virologists offer insights into pursuing a research career in public health at the Centers for Disease Control and Prevention.
February 15, 2017: Journal of Virology
https://www.readbyqxmd.com/read/28199020/gemfibrozil-food-and-drug-administration-approved-lipid-lowering-drug-increases-longevity-in-mouse-model-of-late-infantile-neuronal-ceroid-lipofuscinosis
#4
Arunava Ghosh, Suresh Babu Rangasamy, Khushbu K Modi, Kalipada Pahan
Late Infantile Neuronal Ceroid Lipofuscinosis (LINCL) is a rare neurodegenerative disease caused by mutations in the Cln2 gene that leads to deficiency or loss of function of the tripeptidyl peptidase 1 (TPP1) enzyme. TPP1 deficiency is known to cause the accumulation of autofluoroscent lipid-protein pigments in brain. Similar to other neurodegenerative disorders, LINCL is also associated with neuroinflammation and neuronal damage. Despite investigations, no effective therapy is currently available for LINCL...
February 15, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28198398/microrna-155-controls-exosome-synthesis-and-promotes-gemcitabine-resistance-in-pancreatic-ductal-adenocarcinoma
#5
Manabu Mikamori, Daisaku Yamada, Hidetoshi Eguchi, Shinichiro Hasegawa, Tomoya Kishimoto, Yoshito Tomimaru, Tadafumi Asaoka, Takehiro Noda, Hiroshi Wada, Koichi Kawamoto, Kunihito Gotoh, Yutaka Takeda, Masahiro Tanemura, Masaki Mori, Yuichiro Doki
The cancer drug gemcitabine (GEM) is a key drug for treating pancreatic ductal adenocarcinoma (PDAC), but PDAC cells develop chemoresistance after long-term administration. Since the tolerance was immediately spread to every PDAC tissue in a patient, it is assumed that some certain efficient mechanisms underlay in the development of chemoresistance. Changes in the levels of particular microRNAs or alterations in intercellular communication play a dominant role in chemoresistance development, and recent data also suggest that exosomes play an important role in this process...
February 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28188072/adjuvant-combination-therapy-with-gemcitabine-and-autologous-%C3%AE-%C3%AE-t-cell-transfer-in-patients-with-curatively-resected-pancreatic-cancer
#6
Taku Aoki, Hirokazu Matsushita, Mayumi Hoshikawa, Kiyoshi Hasegawa, Norihiro Kokudo, Kazuhiro Kakimi
BACKGROUND AIMS: The outcome for pancreatic cancer after surgery remains highly unsatisfactory, and development of more effective therapies is urgently needed. Therefore, we conducted a phase I clinical study of a novel combination of gemcitabine (GEM) and autologous γδ T-cell therapy for patients with curatively resected pancreatic cancer (University Hospital Medical Information Clinical Trials Registry identifier 000000931). METHODS: From July 2008 to December 2012, 56 consenting patients were recruited...
February 7, 2017: Cytotherapy
https://www.readbyqxmd.com/read/28187380/biomimetic-nanoassemblies-of-1-o-octodecyl-2-conjugated-linoleoyl-sn-glycero-3-phosphatidyl-gemcitabine-with-phospholipase-a2-triggered-degradation-for-the-treatment-of-cancer
#7
Jing Zuo, Li Tong, Lina Du, Ming Yang, Yiguang Jin
Phospholipids are important biomolecules with strong self-assembling ability to form biomembranes or liposomes. However, biomimetic prodrugs of phospholipids are not well known, including their self-assembling behavior at the air/water interface or in aqueous media. Here we design and prepare a biomimetic phospholipid-like amphiphilic prodrug, 1-O-octodecyl-2-conjugated linoleoyl-sn-glycero-3-phosphatidyl gemcitabine (OLGPG). After spreading at the air/water interface, it formed Langmuir monolayers. Stable nanoassemblies were obtained based on molecular self-assembly after OLGPG was injected in water...
February 3, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28183260/current-challenges-and-opportunities-for-chemoprevention-of-pancreatic-cancer
#8
Altaf Mohammed, Naveena B Janakiram, Venkateshwar Madka, Min Li, Adam S Asch, Chinthalapally V Rao
The incidence of pancreatic cancer (PC) is rising in parallel with the deaths caused by this malignant disease largely due to limited improvement in current treatment strategies. In spite of aggressive PC research, for the past three decades, there has been no significant improvement in the five-year survival for this cancer. Like many other cancers, it takes several years for normal pancreatic cells to transform into pancreatic precursor lesions and to further progress into invasive carcinoma. Hence there is a scope for development of chemoprevention strategies to inhibit/delay/prevent progression of this disease into an advanced stage cancer...
February 8, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28179351/a-multicenter-phase-ii-study-of-gemcitabine-plus-s-1-chemotherapy-for-advanced-biliary-tract-cancer
#9
Shiho Arima, Kyoko Shimizu, Tomoyoshi Okamoto, Masao Toki, Yutaka Suzuki, Naohiro Okano, Daisuke Naruge, Kirio Kawai, Takaaki Kobayashi, Akiyoshi Kasuga, Hiroshi Kitamura, Atuko Takasu, Fumio Nagashima, Masanori Sugiyama, Junji Furuse
BACKGROUND: Gemcitabine (GEM) plus cisplatin (CDDP) chemotherapy has been used worldwide as the standard first-line treatment for advanced biliary tract cancer (BTC). A phase II trial has also suggested promising activity of GEM plus S-1 chemotherapy against advanced BTC. The aim of this study was to evaluate the efficacy and safety of GEM plus S-1 chemotherapy in patients with advanced BTC. PATIENTS AND METHODS: The eligibility criteria were as follows: histologically-proven BTC, unresectable or recurrent disease, ECOG performance status (PS) 0-1 regardless of previous treatment...
2017: Anticancer Research
https://www.readbyqxmd.com/read/28177234/experimental-and-theoretical-studies-on-rhodium-catalyzed-coupling-of-benzamides-with-2-2-difluorovinyl-tosylate-diverse-synthesis-of-fluorinated-heterocycles
#10
Jia-Qiang Wu, Shang-Shi Zhang, Hui Gao, Zisong Qi, Chu-Jun Zhou, Wei-Wei Ji, Yao Liu, Yunyun Chen, Qingjiang Li, Xingwei Li, Honggen Wang
Fluorinated heterocycles play an important role in pharmaceutical and agrochemical industries. Herein, we report on the synthesis of four types of fluorinated heterocycles via rhodium(III)-catalyzed C-H activation of arenes/alkenes and versatile coupling with 2,2-difluorovinyl tosylate. With N-OMe benzamide being a directing group (DG), the reaction delivered a monofluorinated alkene with the retention of the tosylate functionality. Subsequent one-pot acid treatment allowed the efficient synthesis of 4-fluoroisoquinolin-1(2H)-ones and 5-fluoropyridin-2(1H)-ones...
February 8, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28176879/parp-inhibitor-increases-chemosensitivity-by-upregulating-mir-664b-5p-in-brca1-mutated-triple-negative-breast-cancer
#11
Wei Song, Lin Tang, Yumei Xu, Jing Xu, Wenwen Zhang, Hui Xie, Shui Wang, Xiaoxiang Guan
Emerging evidence has shown that adding poly(ADP-ribose) polymerase (PARP) inhibitors to chemotherapy regimens is superior to the control regimens alone in BRCA1-mutated triple-negative breast cancer (TNBC) patients, but their underlying mechanisms have not been fully elucidated. In this study, using miRNA microarray analysis of two BRCA1-mutated TNBC cell lines, we found that miR-664b-5p expression was increased after adding a PARP inhibitor, olaparib, to a carboplatin (CBP) plus gemcitabine (GEM) therapy regimen...
February 8, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28176365/high-efficacy-of-pazopanib-on-an-undifferentiated-spindle-cell-sarcoma-resistant-to-first-line-therapy-is-identified-with-a-patient-derived-orthotopic-xenograft-pdox-nude-mouse-model
#12
Kentaro Igarashi, Kei Kawaguchi, Takashi Murakami, Tasuku Kiyuna, Kentaro Miyake, Arun S Singh, Scott D Nelson, Sarah Dry, Yunfeng Li, Norio Yamamoto, Katsuhiro Hayashi, Hiroaki Kimura, Shinji Miwa, Hiroyuki Tsuchiya, Fritz C Eilber, Robert M Hoffman
Undifferentiated spindle-cell sarcoma (USCS) is a recalcitrant cancer. Our laboratory pioneered the patient-derived orthotopic xenograft (PDOX) nude mouse model with the technique of surgical orthotopic implantation (SOI). In the present study, we evaluated the efficacy of standard first-line chemistry of doxorubicin (DOX), gemcitabine (GEM) combined with docetaxel (DOC), compared to pazopanib (PAZ), a multi-targeting tyrosine-kinase inhibitor, in an USCS PDOX model. A high-grade USCS from a striated muscle of the patients was grown orthotopically in the right biceps femoris muscle of nude mice to establish the PDOX model...
February 8, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28164512/critical-deviations-of-ionized-calcium-measurements-when-using-blood-gas-analyzers-to-monitor-citrate-dialysis
#13
Thorsten Feldkamp, Norbert Weiler, Michael Marx, Peter B Luppa, Ralf Junker
BACKGROUND: During the course of acute kidney injury (AKI) patients may require renal replacement therapy (RRT). The preferred therapeutic measure for such patients is continuous RRT (CRRT). Anticoagulation is required to prevent clotting of the extracorporeal circuit. The actual KDIGO guidelines recommend citrate as the first line anticoagulant. METHODS: Citrate dose infused into the extracorporeal circuit should achieve an extracorporeal calcium concentration of 0...
October 1, 2016: Clinical Laboratory
https://www.readbyqxmd.com/read/28161047/mercury-species-in-formerly-contaminated-soils-and-released-soil-gases
#14
Jiřina Sysalová, Jan Kučera, Barbora Drtinová, Rostislav Červenka, Ondřej Zvěřina, Josef Komárek, Jan Kameník
Total mercury (T-Hg), elemental mercury (Hg(0)), methylmercury (MeHg(+)), phenylmercury (PhHg(+)), and gaseous elemental mercury (GEM) species were determined in soils formerly contaminated by different processes from two sites in the Czech Republic. Analytical methods involved atomic absorption spectrometry (AAS) using a single-purpose Advanced Mercury Analyser AMA-254 and radiochemical neutron activation analysis (RNAA) for T-Hg determination, a thermal desorption method was used for Hg(0) determination, gas chromatography coupled with atomic fluorescence spectrometry (GC-AFS) was employed for assay of MeHg(+) and PhHg(+), while GEM measurement was carried out using a portable Zeeman-AAS device Lumex RA-915(+)...
February 1, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28152544/exosomes-confer-chemoresistance-to-pancreatic-cancer-cells-by-promoting-ros-detoxification-and-mir-155-mediated-suppression-of-key-gemcitabine-metabolising-enzyme-dck
#15
Girijesh Kumar Patel, Mohammad Aslam Khan, Arun Bhardwaj, Sanjeev K Srivastava, Haseeb Zubair, Mary C Patton, Seema Singh, Moh'd Khushman, Ajay P Singh
BACKGROUND: Chemoresistance is a significant clinical problem in pancreatic cancer (PC) and underlying molecular mechanisms still remain to be completely understood. Here we report a novel exosome-mediated mechanism of drug-induced acquired chemoresistance in PC cells. METHODS: Differential ultracentrifugation was performed to isolate extracellular vesicles (EVs) based on their size from vehicle- or gemcitabine-treated PC cells. Extracellular vesicles size and subtypes were determined by dynamic light scattering and marker profiling, respectively...
February 2, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/28149718/arthroscopic-bone-grafting-for-anteroinferior-glenoid-defect-using-template
#16
Wichan Kanchanatawan, Jatupon Kongtharvonskul, Kaiwan Sriruanthong, Gem Dorjiee
Significant anteroinferior glenoid bone loss is widely accepted as a major pathology of recurrent anterior shoulder dislocation, particularly after failed arthroscopic Bankart repair. Numerous surgical techniques for glenoid bone grafting have been described and have been reported to yield successful outcomes. Both open and arthroscopic approaches have been used, with the coracoid and the iliac crest being commonly used for bone graft. When compared with open surgery, an arthroscopic approach has many advantages...
December 2016: Arthroscopy Techniques
https://www.readbyqxmd.com/read/28142123/plasmonic-nanocarrier-grid-enhanced-raman-sensor-for-studies-of-anticancer-drug-delivery
#17
Katarzyna Kurzątkowska, Ty Santiago, Maria Hepel
Targeted drug delivery systems using nanoparticle nanocarriers offer remarkable promise for cancer therapy by discriminating against devastating cytotoxicity of chemotherapeutic drugs to healthy cells. To aid in the development of new drug nanocarriers, we propose a novel plasmonic nanocarrier grid-enhanced Raman sensor which can be applied for studies and testing of drug loading onto the nanocarriers, attachment of targeting ligands, dynamics of drug release, assessment of nanocarrier stability in biological environment, and general capabilities of the nanocarrier...
January 24, 2017: Biosensors & Bioelectronics
https://www.readbyqxmd.com/read/28142120/nanotechnology-for-delivery-of-gemcitabine-to-treat-pancreatic-cancer
#18
REVIEW
Gebremariam Birhanu, Hamid Akbari Javar, Ehsan Seyedjafari, Ali Zandi-Karimi
Pancreatic cancer (PC) is one of the most deadly and quickly fatal human cancers with a 5-year mortality rate close to 100%. Its prognosis is very poor, mainly because of its hostile biological behavior and late onset of symptoms for clinical diagnosis; these bring limitations on therapeutic interventions. Factors contributing for the difficulties in treating PC include: high rate of drug resistance, fast metastasis to different organs, poor prognosis and relapse of the tumor after therapy. After being approved by US FDA 1997, Gemcitabine (Gem) is the first line and the gold standard drug for all stages of advanced PC till now...
January 28, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28139930/synthesis-of-gem-difluoroallylboronates-via-fecl2-catalyzed-boration-%C3%AE-fluorine-elimination-of-trifluoromethyl-alkenes
#19
Yang Liu, Yuhan Zhou, Yilong Zhao, Jingping Qu
The first ferrous chloride catalyzed boration/β-fluorine elimination of trifluoromethyl alkenes is described. Thus, a full range of gem-difluoroallylboronates were obtained in high yield under mild conditions. As an important fluorinated building block, gem-difluoroallylboronate can be readily converted into diverse difluoro-substituted species.
January 31, 2017: Organic Letters
https://www.readbyqxmd.com/read/28139322/the-local-impact-of-a-coal-fired-power-plant-on-inorganic-mercury-and-methyl-mercury-distribution-in-rice-oryza-sativa-l
#20
Xiaohang Xu, Bo Meng, Chao Zhang, Xinbin Feng, Chunhao Gu, Jianyang Guo, Kevin Bishop, Zhidong Xu, Sensen Zhang, Guangle Qiu
Emission from coal-fired power plants is one of the major anthropogenic sources of mercury (Hg) in the environment, because emitted Hg can be quickly deposited nearby the source, attention is paid to the effects of coal-burning facilities on levels of toxic methyl-mercury (MeHg) in biota near such sources. Since rice is an agricultural crop that can bio-accumulate MeHg, the potential effects of a large Hg-emitting coal-fired power plant in Hunan Province, China on both inorganic Hg (Hg(II)) and MeHg distributions in rice was investigated...
January 27, 2017: Environmental Pollution
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