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https://www.readbyqxmd.com/read/28816956/differential-diagnosis-of-posterior-fossa-brain-tumors-multiple-discriminant-analysis-of-tl-spect-and-fdg-pet
#1
Moritaka Yamauchi, Tomohisa Okada, Tsutomu Okada, Akira Yamamoto, Yasutaka Fushimi, Yoshiki Arakawa, Susumu Miyamoto, Kaori Togashi
This study investigated the combined capability of thallium-201 (Tl)-SPECT and fluorine-18-fluoro-deoxy-glucose (FDG)-PET for differential diagnosis of posterior fossa brain tumors using multiple discriminant analysis.This retrospective study was conducted under approval of the institutional review board. In the hospital information system, 27 patients with posterior fossa intra-axial tumor between January 2009 and June 2015 were enrolled and grouped as the following 7 entities: low grade glioma (LGG) 6, anaplastic astrocytoma (AA) 2, glioblastoma (GBM) 3, medulloblastoma (MB) 3, hemangioblastoma (HB) 6, metastatic tumor (Mets) 3, and malignant lymphoma (ML) 4...
August 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28816329/highly-regio-and-stereoselective-trans-iodofluorination-of-ynamides-enabling-the-synthesis-of-e-%C3%AE-fluoro-%C3%AE-iodoenamides
#2
Yang Xi, Guohao Zhu, Luning Tang, Shihan Ma, Dongming Zhang, Rong Zhang, Guangke He, Hongjun Zhu
A highly regio- and stereoselective trans-iodofluorination reaction of ynamides with NIS and Et3N·3HF has been achieved, affording (E)-α-fluoro-β-iodoenamides in moderate to good yields. The reaction proceeds under mild reaction conditions and exhibits good functional group compatibility.
August 17, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28816243/dopamine-synthesis-capacity-is-associated-with-d2-3-receptor-binding-but-not-dopamine-release
#3
Anne S Berry, Vyoma D Shah, Daniella J Furman, Robert L White, Suzanne L Baker, James P O'Neil, Mustafa Janabi, Mark D'Esposito, William J Jagust
Positron Emission Tomography (PET) imaging allows the estimation of multiple aspects of dopamine function including dopamine synthesis capacity, dopamine release, and D2/3 receptor binding. Though dopaminergic dysregulation characterizes a number of neuropsychiatric disorders including schizophrenia and addiction, there has been relatively little investigation into the nature of relationships across dopamine markers within healthy individuals. Here we used PET imaging in 40 healthy adults to compare, within individuals, estimates of dopamine synthesis capacity (Ki) using 6-[(18)F]fluoro-l-m-tyrosine ([(18)F]FMT; a substrate for aromatic amino acid decarboxylase), baseline D2/3 receptor binding potential using [(11)C]raclopride (a weak competitive D2/3 receptor antagonist), and dopamine release using [(11)C]raclopride paired with oral methylphenidate administration...
August 17, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28814238/structural-insights-for-drugs-developed-for-phospholipase-d-enzymes
#4
Kimberly Stieglitz
BACKGROUND: In recent years human phospholipase D enzymes (PLD1 and PLD2 isozymes) have emerged as drug targets for various diseases such as cardiovascular disease, cancer, infectious diseases and neurodegenerative conditions such as Alzheimer's and Parkinson's disease. The interest in PLD as a drug target is due to the fact that PLD enzymes belong to a superfamily of phospholipases that are essential to intracellular and extracellular signaling. Many bioactive lipid signaling molecules are generated by these enzymes including phosphatidic and lysophosphatidic acid, arachidonic acid, and diacylglycerol (DAG)...
August 15, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28812134/elevated-tumor-to-liver-uptake-ratio-tlr-from-18-f-fdg-pet-ct-predicts-poor-prognosis-in-stage-iia-colorectal-cancer-following-curative-resection
#5
Jun Huang, Liang Huang, Jiaming Zhou, Yinghua Duan, Zhanwen Zhang, Xiaoyan Wang, Pinzhu Huang, Shuyun Tan, Ping Hu, Jianping Wang, Meijin Huang
PURPOSE: The prognostic value of the tumor-to-liver uptake ratio (TLR) from 18-fluoro-2-deoxyglucose positron emission tomography/computed tomography ((18)F-FDG-PET/CT) in the early stage of colorectal cancer (CRC) is unclear. Notably, some stage IIA CRC patients experience early recurrence even after curative resection and might benefit from neoadjuvant or adjuvant chemotherapy. This study aims to evaluate whether elevated TLR from (18)F-FDG-PET/CT can predict poor prognosis in stage IIA CRC patients undergoing curative resection...
August 15, 2017: European Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/28809568/combinatorial-nickel-catalyzed-monofluoroalkylation-of-aryl-boronic-acids-with-unactivated-fluoroalkyl-iodides
#6
Jie Sheng, Hui-Qi Ni, Ge Liu, Yan Li, Xi-Sheng Wang
A combinatorial nickel-catalyzed cross-coupling between arylboronic acids and unactived 1-fluoro-1-iodoalkanes has been developed, which demonstrated high efficiency, mild conditions, and excellent functional-group compatibility. Readily available nitrogen and phosphine ligands were combined with a nitrogen source, which in situ generated a variety of easily tunable catalysts to promote the fluoroalkylation for broad scopes of both coupling partners. This new strategy on combinatorial catalysis offers new solutions for nickel-catalyzed cross-coupling reactions...
August 15, 2017: Organic Letters
https://www.readbyqxmd.com/read/28808756/relationship-between-18-f-fluorodeoxyglucose-accumulation-and-the-braf-v600e-mutation-in-papillary-thyroid-cancer
#7
Jae Won Chang, Ki Wan Park, Jae Hyung Heo, Seung-Nam Jung, Lihua Liu, Sung Min Kim, In Sun Kwon, Bon Seok Koo
BACKGROUND: To determine whether (18)F-fluoro-2-deoxyglucose ((18)F-FDG)-PET/CT is useful for predicting the BRAF (V600E) mutation status of a primary papillary thyroid carcinoma (PTC). METHODS: A retrospective analysis was performed in 108 patients who underwent (18)F-FDG positron emission tomography-computed tomography (PET/CT) for staging before thyroidectomy and BRAF analysis in biopsy-confirmed PTC. The maximum standardized uptake value (SUVmax) of the primary tumor was calculated according to FDG accumulation...
August 14, 2017: World Journal of Surgery
https://www.readbyqxmd.com/read/28807572/identification-of-highly-selective-and-potent-orexin-receptor-1-antagonists-derived-from-a-dual-orexin-receptor-1-2-antagonist-based-on-the-structural-framework-of-pyrazoylethylbenzamide
#8
Aya Futamura, Dai Nozawa, Yuko Araki, Yunoshin Tamura, Seiken Tokura, Hiroshi Kawamoto, Yuichi Tokumaru, Sora Kakihara, Takeshi Aoki, Norikazu Ohtake
The design, synthesis, and structure activity relationships of the novel class of pyrazolylethylbenzamide orexin receptor 1-selective antagonists are described. Further derivatization of the prototype dual orexin receptor 1/2 antagonist lead (1) by installing a (S)-methyl group into the ethyl linker moiety between the pyrazole ring and benzamide resulted in an increase of the antagonist potency against orexin receptor 1/2 receptors. Optimization of the benzamide and pyrazole parts of compounds 2 and 9b led to the identification of N-ethyl-5-fluoro-N-{(2S)-1-[5-(4-fluorophenyl)-2H-tetrazol-2-yl]propan-2-yl}-2-(pyrimidin-2-yl)benzamide (24), which exhibited excellent antagonistic activity against orexin receptor 1 with an IC50 of 2...
July 29, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28806782/the-use-of-18f-fluoro-deoxy-glucose-positron-emission-tomography-18f-fdg-pet-as-a-non-invasive-pharmacodynamic-biomarker-to-determine-the-minimally-pharmacologically-active-dose-of-azd8835-a-novel-pi3k%C3%AE-inhibitor
#9
Juliana Maynard, Sally-Ann Emmas, Francois-Xavier Ble, Herve Barjat, Emily Lawrie, Urs Hancox, Urszula M Polanska, Alison Pritchard, Kevin Hudson
BACKGROUND: The phosphatidyl inositol 3 kinase (PI3K), AKT and mammalian target of rapamycin (mTOR) signal transduction pathway is frequently de-regulated and activated in human cancer and is an important therapeutic target. AZD8835 is a PI3K inhibitor, with selectivity against PI3K α and δ isoforms, which is currently in Phase 1 clinical trials. 18F-Fluoro-deoxy-glucose positron emission tomography (18F-FDG PET) is a non-invasive pharmacodynamic imaging biomarker that has become an integral part of drug development...
2017: PloS One
https://www.readbyqxmd.com/read/28805936/characterizing-hypoxia-in-human-glioma-a-simultaneous-multimodal-mri-and-pet-study
#10
Christine Preibisch, Kuangyu Shi, Anne Kluge, Mathias Lukas, Benedikt Wiestler, Jens Göttler, Jens Gempt, Florian Ringel, Mohamed Al Jaberi, Jürgen Schlegel, Bernhard Meyer, Claus Zimmer, Thomas Pyka, Stefan Förster
Hypoxia plays an important role for the prognosis and therapy response of cancer. Thus, hypoxia imaging would be a valuable tool for pre-therapeutic assessment of tumor malignancy. However, there is no standard validated technique for clinical application available yet. Therefore, we performed a study in 12 patients with high-grade glioma, where we directly compared the two currently most promising techniques, namely the MR-based relative oxygen extraction fraction (MR-rOEF) and the PET hypoxia marker H-1-(3-[(18) F]-fluoro-2-hydroxypropyl)-2-nitroimidazole ([(18) F]-FMISO)...
August 14, 2017: NMR in Biomedicine
https://www.readbyqxmd.com/read/28805609/efficacy-of-pet-ct-to-exclude-leiomyoma-in-patients-with-lesions-suspicious-for-uterine-sarcoma-on-mri
#11
Soshi Kusunoki, Yasuhisa Terao, Takafumi Ujihira, Kazunari Fujino, Hiroshi Kaneda, Miki Kimura, Tsuyoshi Ota, Satoru Takeda
OBJECTIVE: To analyze the efficacy of positron emission tomography/computed tomography (PET/CT) for the diagnosis of uterine sarcoma. MATERIALS AND METHODS: Thirty-four patients evaluated between January 2010 and March 2015 were retrospectively enrolled. All patients in whom uterine sarcoma was suspected based on contrast-enhanced magnetic resonance imaging (MRI) findings (heterogeneous, high signal intensity on T2-weighted images and/or high intensity on T1-weighted images) underwent PET/CT for further assessment...
August 2017: Taiwanese Journal of Obstetrics & Gynecology
https://www.readbyqxmd.com/read/28805211/all-atom-md-indicates-ion-dependent-behavior-of-therapeutic-dna-polymer
#12
Ryan L Melvin, William H Gmeiner, Freddie R Salsbury
Understanding the efficacy of and creating delivery mechanisms for therapeutic nucleic acids requires understanding structural and kinetic properties which allow these polymers to promote the death of cancerous cells. One molecule of interest is a 10 mer of FdUMP (5-fluoro-2'-deoxyuridine-5'-O-monophosphate) - also called F10. Here we investigate the structural and kinetic behavior of F10 in intracellular and extracellular solvent conditions along with non-biological conditions that may be efficacious in in vitro preparations of F10 delivery systems...
August 14, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28804446/induction-of-mir-155-after-brain-injury-promotes-type-1-interferon-and-has-a-neuroprotective-effect
#13
Emily B Harrison, Katy Emanuel, Benjamin G Lamberty, Brenda M Morsey, Min Li, Matthew L Kelso, Sowmya V Yelamanchili, Howard S Fox
Traumatic brain injury (TBI) produces profound and lasting neuroinflammation that has both beneficial and detrimental effects. Recent evidence has implicated microRNAs (miRNAs) in the regulation of inflammation both in the periphery and the CNS. We examined the expression of inflammation associated miRNAs in the context of TBI using a mouse controlled cortical impact (CCI) model and found increased levels of miR-21, miR-223 and miR-155 in the hippocampus after CCI. The expression of miR-155 was elevated 9-fold after CCI, an increase confirmed by in situ hybridization (ISH)...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28798032/improved-estrogen-receptor-assessment-by-pet-using-the-novel-radiotracer-4fmfes-in-er-breast-cancer-patients-an-ongoing-phase-ii-clinical-trial
#14
Michel Paquette, Éric Lavallée, Serge Phoenix, René Ouellet, Helena Senta, Johan E van Lier, Brigitte Guérin, Roger Lecomte, Éric E Turcotte
Following encouraging preclinical and human dosimetry results for the novel estrogen receptor (ER) positron emission tomography (PET) radiotracer 4-fluoro-11β-methoxy-16α-[(18)F]fluoroestradiol (4FMFES), a phase II clinical trial was initiated to compare the PET imaging diagnostic potential of 4FMFES to 16α-[(18)F]fluoroestradiol (FES) in ER positive (ER+) breast cancer patients. Methods: Patients diagnosed with ER+ breast cancer (n = 31) were recruited for this study, including six patients that undertook mastectomy and/or axillary node dissection...
August 10, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28796496/discovery-of-clinical-candidate-n-1s-1-3-fluoro-4-trifluoromethoxy-phenyl-2-methoxyethyl-7-methoxy-2-oxo-2-3-dihydropyrido-2-3-b-pyrazine-4-1h-carboxamide-tak-915-a-highly-potent-selective-and-brain-penetrating-phosphodiesterase-2a-inhibitor-for-the-treatment
#15
Satoshi Mikami, Shinji Nakamura, Tomoko Ashizawa, Izumi Nomura, Masanori Kawasaki, Shigekazu Sasaki, Hideyuki Oki, Hironori Kokubo, Isaac D Hoffman, Hua Zou, Noriko Uchiyama, Kosuke Nakashima, Naomi Kamiguchi, Haruka Imada, Noriko Suzuki, Hiroki Iwashita, Takahiko Taniguchi
Phosphodiesterase (PDE) 2A inhibitors have emerged as a novel mechanism with potential therapeutic option to ameliorate cognitive dysfunction in schizophrenia or Alzheimer's disease through upregulation of cyclic nucleotides in the brain, and thereby achieve potentiation of cyclic nucleotide signaling pathways. This article details the expedited optimization of our recently disclosed pyrazolo[1,5-a]pyrimidine lead compound 4b, leading to the discovery of clinical candidate 36 (TAK-915), which demonstrates an appropriate combination of potency, PDE selectivity, and favorable pharmacokinetic (PK) properties, including brain penetration...
August 10, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28796066/a-new-diagnostic-marker-for-differentiating-multicentric-gliomas-from-multiple-intracranial-diffuse-large-b-cell-lymphomas-on-18f-fdg-pet-images
#16
Kai Wang, Xiaobin Zhao, Qian Chen, Di Fan, Zhen Qiao, Song Lin, Tao Jiang, Jianping Dai, Lin Ai
Intracranial gliomas and lymphomas may share similar radiological manifestations, while the treatment strategies for them are different. The aim of the study was to investigate the diagnostic value of fluorine-18-fluoro-2-deoxy-D-glucose (F-FDG) positron emission computed tomography (PET) for differentiation of multicentric gliomas and intracranial multiple diffuse large B-cell lymphomas (DLBCLs) as a study of diagnostic accuracy.A total of 32 patients with multiple intracranial tumors visualized on contrast-enhanced magnetic resonance imaging (MRI) were retrospectively evaluated...
August 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28795715/spin-dynamics-of-light-induced-charge-separation-in-composites-of-semiconducting-polymers-and-pc60bm-revealed-using-q-band-pulse-epr
#17
E A Lukina, E Suturina, E Reijerse, W Lubitz, L V Kulik
Light-induced processes in composites of semiconducting polymers and fullerene derivatives have been widely studied due to their usage as active layers of organic solar cells. However the process of charge separation under light illumination - the key process of an organic solar cell is not well understood yet. Here we report a Q-band pulse electron paramagnetic resonance study of composites of the fullerene derivative PC60BM ([6,6]-phenyl-C61-butyric acid methyl ester) with different p-type semiconducting polymers regioregular and regiorandom P3HT (poly(3-hexylthiophene-2,5-diyl), MEH-PPV (poly[2-methoxy-5-(2-ethylhexyloxy)-1,4-phenylenevinylene]), PCDTBT (poly[N-9'-heptadecanyl-2,7-carbazole-alt-5,5-(4',7'-di-2-thienyl-2',1',3'-benzothiadiazole)]), PTB7 (poly({4,8-bis[(2-ethylhexyl)oxy]benzo[1,2-b:4,5-b']dithiophene-2,6-diyl}{3-fluoro-2-[(2-ethylhexyl)carbonyl]thieno[3,4-b]thiophenediyl}))), resulting in a detailed description of the in-phase laser flash-induced electron spin echo (ESE) signal...
August 10, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28795272/pet-imaging-on-dynamic-metabolic-changes-after-combination-therapy-of-paclitaxel-and-the-traditional-chinese-medicine-in-breast-cancer-bearing-mice
#18
Yao Chen, Ling Wang, Hao Liu, Fahuan Song, Caiyun Xu, Kai Zhang, Qing Chen, Shuang Wu, Yunqi Zhu, Ying Dong, Min Zhou, Hong Zhang, Mei Tian
PURPOSE: The aim of the study was to non-invasively evaluate the anticancer activity of a traditional Chinese medicine-Huaier, combined with paclitaxel (PTX) in breast cancer bearing mice by detecting dynamic metabolic changes with positron emission tomography (PET). PROCEDURES: Balb/c nude mice were randomly divided into one of the four groups: Huaier, PTX, PTX + Huaier, or the control. PET imaging with 2-deoxy-2-[(18)F]fluoro-D-glucose ([(18)F]FDG) was performed to monitor the metabolic changes in BT474 (luminal B) and MDA-MB-231 (triple-negative) breast cancer xenografts...
August 9, 2017: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://www.readbyqxmd.com/read/28793277/o-2-18-f-fluoroethyl-l-tyrosine-18-f-fet-uptake-in-insulinoma-first-results-from-a-xenograft-mouse-model-and-from-human
#19
Alessio Imperiale, Frédéric Boisson, Guillaume Kreutter, Bernard Goichot, Izzie Jacques Namer, Philippe Bachellier, Patrice Laquerriere, Laurence Kessler, Patrice Marchand, David Brasse
INTRODUCTION: Herein we have evaluated the uptake of O-(2-(18)F-fluoroethyl)-l-tyrosine ((18)F-FET) in insulinoma in comparison with those of 6-(18)F-fluoro-3,4-dihydroxy-l-phenylalanine ((18)F-FDOPA) providing first data from both murine xenograft model and one patient with proved endogenous hyperinsulinemic hypoglycemia. METHODS: Dynamic (18)F-FET and carbidopa-assisted (18)F-FDOPA PET were performed on tumor-bearing nude mice after subcutaneous injection of RIN-m5F murine beta cells and on a 30-year-old man with type-1 multiple endocrine neoplasia and hyperinsulinemic hypoglycemia defined by a positive fasting test...
July 12, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28782435/rufinamide-pretreatment-attenuates-ischemia-reperfusion-injury-in-the-gerbil-hippocampus
#20
Chan Woo Park, Tae-Kyeong Lee, Jeong Hwi Cho, In Hye Kim, Jae-Chul Lee, Bich-Na Shin, Ji Hyeon Ahn, Sung Koo Kim, Myoung Cheol Shin, Taek Geun Ohk, Jun Hwi Cho, Moo-Ho Won, Young Joo Lee, Jeong Yeol Seo, Joon Ha Park
OBJECTIVES: Rufinamide, a voltage-gated sodium channel (VGSC) blocker, is widely used for the clinical treatment of seizures associated with Lennox-Gastaut syndrome. Previous studies have demonstrated that VGSC blockers have neuroprotective properties against ischemic damage following experimental cerebral ischemia. However, protective effects of rufinamide against cerebral ischemic insults have not been addressed. Therefore, in the present study, we firstly examined neuroprotective effects of rufinamide using a gerbil model of transient global cerebral ischemia...
August 7, 2017: Neurological Research
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