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https://www.readbyqxmd.com/read/28333959/fnc-efficiently-inhibits-mantle-cell-lymphoma-growth
#1
Yan Zhang, Rong Zhang, Xixi Ding, Bangan Peng, Ning Wang, Fang Ma, Youmei Peng, Qingduan Wang, Junbiao Chang
FNC, 2'-deoxy-2'-β-fluoro-4'-azidocytidine, is a novel cytidine analogue, that has shown strong antiproliferative activity in human lymphoma, lung adenocarcinoma and acute myeloid leukemia. In this study, we investigated the effects of FNC on mantle cell lymphoma (MCL) and the underlying mechanisms. In in vitro experiments, cell viability was detected by the CCK8 assay, and cell cycle progression and apoptosis were assessed by flow cytometry, and the expression of relative apoptosis proteins were detected by Western Blot...
2017: PloS One
https://www.readbyqxmd.com/read/28332824/indole-substituted-benzothiazoles-and-benzoxazoles-as-selective-and-reversible-mao-b-inhibitors-for-treatment-of-parkinson-s-disease
#2
Min-Ho Nam, Moosung Park, Hyeri Park, Youngjae Kim, Seulki Yoon, Vikram Shahaji Sawant, Ji Won Choi, Jong-Hyun Park, Ki Duk Park, Sun-Joon Min, Changjoon Justin Lee, Hyunah Choo
To develop a novel, selective, and reversible MAO-B inhibitors for safer treatment of Parkinson's disease, benzothiazole and benzoxazole derivatives with indole moiety were designed and synthesized. Most of the synthesized compounds showed inhibitory activities against MAO-B and selectivity over MAO-A. The most active compound was Compound 5b, 6-fluoro-2-(1-methyl-1H-indol-5-yl)benzo[d]thiazole with an IC50 value of 29 nM with no apparent effect on MAO-A activity at 10 M. Based on the reversibility assay, Compound 5b turned out to be a fully reversible with over 95% of recovery of enzyme activity after washout of the compound...
March 23, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28331985/one-month-assessment-of-renal-cell-carcinoma-treated-by-everolimus-using-fdg-pet-ct-predicts-progression-free-and-overall-survival
#3
Hiroki Ito, Keiichi Kondo, Takashi Kawahara, Tomohiro Kaneta, Ukihide Tateishi, Daiki Ueno, Kazuhiro Namura, Kazuki Kobayashi, Yasuhide Miyoshi, Yasushi Yumura, Kazuhide Makiyama, Narihiko Hayashi, Hisashi Hasumi, Kimito Osaka, Yumiko Yokomizo, Jun-Ichi Teranishi, Yusuke Hattori, Tomio Inoue, Hiroji Uemura, Masahiro Yao, Noboru Nakaigawa
PURPOSE: We evaluated (18)F-2-fluoro-2-deoxyglucose positron emission tomography/computed tomography (FDG PET/CT) results as outcome predictors for patients with metastatic renal cell carcinoma (RCC) treated by everolimus (EVL), an inhibitor of mammalian target of rapamycin. METHODS: We retrospectively reviewed 30 patients who were treated with EVL for metastatic RCC between May 2010 and March 2015, by evaluating their FDG PET/CT result before and 1 month after starting EVL treatment...
March 22, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28331883/practical-no-gold-standard-evaluation-framework-for-quantitative-imaging-methods-application-to-lesion-segmentation-in-positron-emission-tomography
#4
Abhinav K Jha, Esther Mena, Brian Caffo, Saeed Ashrafinia, Arman Rahmim, Eric Frey, Rathan M Subramaniam
Recently, a class of no-gold-standard (NGS) techniques have been proposed to evaluate quantitative imaging methods using patient data. These techniques provide figures of merit (FoMs) quantifying the precision of the estimated quantitative value without requiring repeated measurements and without requiring a gold standard. However, applying these techniques to patient data presents several practical difficulties including assessing the underlying assumptions, accounting for patient-sampling-related uncertainty, and assessing the reliability of the estimated FoMs...
January 2017: Journal of Medical Imaging
https://www.readbyqxmd.com/read/28331132/orbital-malt-lymphoma-after-autologous-stem-cell-transplantation-for-follicular-lymphoma-as-relapse-of-diffuse-large-b-cell-lymphoma
#5
Toshihiko Matsuo, Takehiro Tanaka, Nobuharu Fujii
We report a patient who developed orbital MALT lymphoma after autologous peripheral blood stem cell transplantation for follicular lymphoma as relapse of diffuse large B-cell lymphoma. A 54-year-old woman with systemic lymphadenopathy was diagnosed with diffuse large B-cell lymphoma by left supraclavicular lymph node biopsy, and underwent 6 courses of R-CHOP chemotherapy with rituximab, cyclophosphamide, doxorubicin, vincristine, and prednisolone, leading to complete response. Five years later in the follow-up, an abdominal mass with abnormal uptake was found by whole-body 2-[(18)F]fluoro-2-deoxy-D-glucose positron emission tomography, and computed tomography-guided biopsy demonstrated follicular lymphoma...
2017: Journal of Clinical and Experimental Hematopathology: JCEH
https://www.readbyqxmd.com/read/28327308/chalcone-benzoxaborole-hybrids-as-novel-anticancer-agents
#6
Jiong Zhang, Fei Yang, Zhitao Qiao, Mingyan Zhu, Huchen Zhou
In this study, we report the synthesis of a series of chalcone-benzoxaborole hybrid molecules and the evaluation of their anticancer activity. Their anticancer potency and toxicity were tested on three human cancer cell lines and two normal cell lines. The 4-fluoro compound 15 was found to be the most potent compound with an IC50 value of 1.4μM on SKOV3 cells. The 4-iodo compound 18 and 3-methyloxy-4-amino compound 47 showed good potency on SKOV3 cells while exhibiting low toxicity on normal cells. This work extended the application of benzoxaboroles to the field of anticancer research...
December 1, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28326060/microbial-neuraminidase-induces-a-moderate-and-transient-myelin-vacuolation-independent-of-complement-system-activation
#7
Pablo Granados-Durán, María Dolores López-Ávalos, Manuel Cifuentes, Margarita Pérez-Martín, María Del Mar Fernández-Arjona, Timothy R Hughes, Krista Johnson, B Paul Morgan, Pedro Fernández-Llebrez, Jesús M Grondona
AIMS: Some central nervous system pathogens express neuraminidase (NA) on their surfaces. In the rat brain, a single intracerebroventricular (ICV) injection of NA induces myelin vacuolation in axonal tracts. Here, we explore the nature, the time course, and the role of the complement system in this damage. METHODS: The spatiotemporal analysis of myelin vacuolation was performed by optical and electron microscopy. Myelin basic protein-positive area and oligodendrocyte transcription factor (Olig2)-positive cells were quantified in the damaged bundles...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28323942/incretin-therapies-do-not-expand-%C3%AE-cell-mass-or-alter-pancreatic-histology-in-young-male-mice
#8
Aaron R Cox, Carol J Lam, Matthew M Rankin, Jacqueline S Rios, Julia Chavez, Claire W Bonnyman, Kourtney B King, Roger A Wells, Deepti Anthony, Justin X Tu, Jenny J Kim, Changhong Li, Jake A Kushner
The impact of incretins upon pancreatic β-cell expansion remains extremely controversial. Multiple studies indicate that incretin-based therapies can increase β-cell proliferation, and incretins have been hypothesized to expand β-cell mass. However, considerable disagreement exists on whether incretins actually increase β-cell mass. Moreover, some reports indicate that incretins may cause metaplastic changes in pancreatic histology. To resolve these questions we treated a large cohort of mice with incretin-based therapies and carried out a rigorous analysis of β-cell turnover and pancreatic histology using high-throughput imaging...
March 8, 2017: Endocrinology
https://www.readbyqxmd.com/read/28322043/-sup-18-sup-f-fluoro-hydroxyphenethylguanidines-efficient-synthesis-and-comparison-of-two-structural-isomers-as-radiotracers-of-cardiac-sympathetic-innervation
#9
Yong-Woon Jung, Keun Sam Jang, Guie Gu, Robert A Koeppe, Phillip S Sherman, Carole A Quesada, David M Raffel
Fluorine-18 labeled phenethylguanidines are currently under development in our laboratory as radiotracers for quantifying regional cardiac sympathetic nerve density using PET imaging techniques. In this study, we report an efficient synthesis of <sup>18</sup>F-hydroxyphenethylguanidines consisting of nucleophilic aromatic [<sup>18</sup>F]fluorination of a protected diaryliodonium salt precursor followed by a single deprotection step to afford the desired radiolabeled compound. This approach has been shown to reliably produce 4-[<sup>18</sup>F]fluoro-<i>m</I>-hydroxyphenethylguanidine ([<sup>18</sup>F]4F-MHPG, [<sup>18</sup>F]<b>1</b>) and its structural isomer 3-[<sup>18</sup>F]fluoro-<i>p</i>-hydroxyphenethylguanidine ([<sup>18</sup>F]3F-PHPG, [<sup>18</sup>F]<b>2</b>) with good radiochemical yields...
March 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28322026/objective-3d-surface-evaluation-of-intracranial-electrophysiologic-correlates-of-cerebral-glucose-metabolic-abnormalities-in-children-with-focal-epilepsy
#10
Jeong-Won Jeong, Eishi Asano, Vinod Kumar Pilli, Yasuo Nakai, Harry T Chugani, Csaba Juhász
To determine the spatial relationship between 2-deoxy-2[(18) F]fluoro-D-glucose (FDG) metabolic and intracranial electrophysiological abnormalities in children undergoing two-stage epilepsy surgery, statistical parametric mapping (SPM) was used to correlate hypo- and hypermetabolic cortical regions with ictal and interictal electrocorticography (ECoG) changes mapped onto the brain surface. Preoperative FDG-PET scans of 37 children with intractable epilepsy (31 with non-localizing MRI) were compared with age-matched pseudo-normal pediatric control PET data...
March 21, 2017: Human Brain Mapping
https://www.readbyqxmd.com/read/28318229/tracing-effects-of-fluorine-substitutions-on-g-quadruplex-conformational-changes
#11
Jonathan Dickerhoff, Linn Haase, Walter Langel, Klaus Weisz
A human telomere sequence that folds into an intramolecular (3+1)-hybrid G-quadruplex was modified by the incorporation of 2'-fluoro-2'-deoxyriboguanosines ((F)G) into syn positions of its outer tetrad. A circular dichroism and NMR spectral analysis reveals a nearly quantitative switch of the G-tetrad polarity with concerted syn↔anti transitions of all four G residues. These observations follow findings on a (F)G-substituted (3+1)-hybrid quadruplex with a different fold, suggesting a more general propensity of hybrid-type quadruplexes to undergo a tetrad polarity reversal...
March 20, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28316823/a-new-solvate-of-afatinib-a-specific-inhibitor-of-the-erbb-family-of-tyrosine-kinases
#12
Matthias Zeller, Gabriel Lima Barros de Araujo, Trev Parker, Amrinder Singh Rai, Stephen R Byrn
Afatinib (systematic name: N-{4-(3-chloro-4-fluoro-anilino)-7-[(tetra-hydro-furan-3-yl)-oxy]quinazolin-6-yl}-4-(di-methyl-amino)-but-2-enamide), is a specific in-hibitor of the ErbB family of tyrosine kinases. The free base form crystallizes from aceto-nitrile as a mixed water-aceto-nitrile solvent, C24H25ClFN5O3·0.25C2H3N·2H2O. It crystallizes with two independent mol-ecules (A and B) in the asymmetric unit of the chiral space group P4212, but exhibits close to perfect pseudo-inversion symmetry, emulating P4/ncc that relates the two mol-ecules to each other...
March 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28316809/crystal-structure-and-hydrogen-bonding-patterns-in-5-fluoro-cytosinium-picrate
#13
Marimuthu Mohana, Packianathan Thomas Muthiah, Colin D McMillen
In the crystal structure of the title compound, 5-fluoro-cytosinium picrate, C4H5FN3O(+)·C6H2N3O7(-), one N heteroatom of the 5-fluoro-cytosine (5FC) ring is protonated. The 5FC ring forms a dihedral angle of 19.97 (11)° with the ring of the picrate (PA(-)) anion. In the crystal, the 5FC(+) cation inter-acts with the PA(-) anion through three-centre N-H⋯O hydrogen bonds, forming two conjoined rings having R2(1)(6) and R1(2)(6) motifs, and is extended by N-H⋯O hydrogen bonds and C-H⋯O inter-actions into a two-dimensional sheet structure lying parallel to (001)...
March 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28315919/a-rare-adult-renal-neuroblastoma-better-imaged-by-18-f-fdg-than-by-68-ga-dotanoc-in-the-pet-ct-scan
#14
Tarun Kumar Jain, Sharwan Kumar Singh, Ashwani Sood, Abhiram Gj Ashwathanarayama, Rajender Kumar Basher, Jaya Shukla, Bhagwant Rai Mittal
Primary renal neuroblastoma is an uncommon tumor in children and extremely rare in adults. We present a case of a middle aged female having a large retroperitoneal mass involving the right kidney with features of neuroblastoma on pre-operative histopathology. Whole-body fluorine-18-fluoro-deoxyglucose positron emission tomography ((18)F-FDG PET/CT) and (68)Ga-dotanoc PET/CT scans performed for staging and therapeutic potential revealed a tracer avid mass replacing the right kidney and also pelvic lymph nodes...
March 20, 2017: Hellenic Journal of Nuclear Medicine
https://www.readbyqxmd.com/read/28314510/t-butyl-pyridine-and-phenyl-c-region-analogues-of-2-3-fluoro-4-methylsulfonylaminophenyl-propanamides-as-potent-trpv1-antagonists
#15
Sunho Lee, Dong Wook Kang, HyungChul Ryu, Changhoon Kim, Jihyae Ann, Hobin Lee, Eunhye Kim, Sunhye Hong, Sun Choi, Peter M Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph, Jeewoo Lee
A series of 2-substituted 6-t-butylpyridine and 4-t-butylphenyl C-region analogues of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides were investigated for hTRPV1 antagonism. The analysis of structure activity relationships indicated that the pyridine derivatives generally exhibited a little better antagonism than did the corresponding phenyl surrogates for most of the series. Among the compounds, compound 7 showed excellent antagonism toward capsaicin activation with Ki=0.1nM and compound 60S demonstrated a strong antiallodynic effect with 83% MPE at 10mg/kg in the neuropathic pain model...
March 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28300727/in%C3%A2-vivo-transport-of-three-radioactive-18-f-fluorinated-deoxysucrose-analogs-by-the-maize-sucrose-transporter-zmsut1
#16
Thu M Tran, Carissa S Hampton, Tom W Brossard, Michael Harmata, J David Robertson, Silvia S Jurisson, David M Braun
Sucrose transporter (SUT) proteins translocate sucrose across cell membranes; however, mechanistic aspects of sucrose binding by SUTs are not well resolved. Specific hydroxyl groups in sucrose participate in hydrogen bonding with SUT proteins. We previously reported that substituting a radioactive fluorine-18 [(18)F] at the C-6' position within the fructosyl moiety of sucrose did not affect sucrose transport by the maize (Zea mays) ZmSUT1 protein. To determine how (18)F substitution of hydroxyl groups at two other positions within sucrose, the C-1' in the fructosyl moiety or the C-6 in the glucosyl moiety, impact sucrose transport, we synthesized 1'-[F(18)]fluoro-1'-deoxysucrose and 6-[F(18)]fluoro-6-deoxysucrose ([(18)F]FDS) analogs...
March 8, 2017: Plant Physiology and Biochemistry: PPB
https://www.readbyqxmd.com/read/28298962/evaluation-of-response-to-immune-checkpoint-inhibitors-is-there-a-role-for-positron-emission-tomography
#17
EDITORIAL
Matteo Bauckneht, Roberta Piva, Gianmario Sambuceti, Francesco Grossi, Silvia Morbelli
Strategies targeting intracellular negative regulators such as immune checkpoint inhibitors (ICPIs) have demonstrated significant antitumor activity across a wide range of solid tumors. In the clinical practice, the radiological effect of immunotherapeutic agents has raised several more relevant and complex challenges for the determination of their imaging-based response at single patient level. Accordingly, it has been suggested that the conventional Response Evaluation Criteria in Solid Tumors assessment alone, based on dimensional evaluation provided by computed tomography (CT), tends to underestimate the benefit of ICPIs at least in a subset of patients, supporting the need of immune-related response criteria...
February 28, 2017: World Journal of Radiology
https://www.readbyqxmd.com/read/28294334/comparative-assessment-of-6-18-f-fluoro-l-m-tyrosine-and-6-18-f-fluoro-l-dopa-to-evaluate-dopaminergic-presynaptic-integrity-in-a-parkinson-s-disease-rat-model
#18
REVIEW
Guillaume Becker, Bahri Mohamed Ali, Anne Michel, Fabian Hustadt, Gaëtan Garraux, André Luxen, Christian Lemaire, Alain Plenevaux
Because of the progressive loss of nigro-striatal dopaminergic terminals in Parkinson's disease (PD), in vivo quantitative imaging of dopamine (DA) containing neurons in animal models of PD is of critical importance in the pre-clinical evaluation of highly awaited disease-modifying therapies. Among existing methods, the high sensitivity of positron emission tomography (PET) is attractive to achieve that goal. The aim of this study was to perform a quantitative comparison of brain images obtained in 6-hydroxydopamine (6-OHDA) lesioned rats using two dopaminergic PET radiotracers, namely [(18) F]fluoro-3,4-dihydroxyphenyl-L-alanine ([(18) F]FDOPA) and 6-[(18) F]fluoro-L-m-tyrosine ([(18) F]FMT)...
March 10, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28294075/%C3%AE-18f-fluoro-azomycin-arabinoside-%C3%AE-18f-faza-synthesis-radiofluorination-and-preliminary-pet-imaging-of-murine-a431-tumors
#19
Piyush Kumar, Peter Roselt, Gerald Reischl, Carlene Cullinane, Davood Beiki, Walter Ehrlichmann, David Binns, Ebrahim Naimi, Jennifer Yang, Rodney Hicks, Hans-Juergen Machulla, Leonard I Wiebe
BACKGROUND: 1-α-D-(5-Deoxy-5-[18F]fluoroarabinofuranosyl)-2-nitroimidazole ([18F]FAZA) is a PET radiotracer that demonstrates excellent potential in imaging regional hypoxia, and is clinically used in diagnosing a wide range of solid tumors in cancer patients. [18F]FAZA, however, is radiofluorinated in only moderate recovered radiochemical yield (rRCY, ~12%). It is postulated that the relative stability of the C1' β-anomeric bond at C5' will make 1-β-D-(5-fluoro-5-deoxyarabinofuranosyl)-2-nitroimidazole (β-FAZA), the β-conformer of FAZA, an attractive candidate for clinical hypoxia imaging...
March 13, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28293004/-granuloma-by-foreign-body-reaction-to-the-stapler-used-for-partial-resection-of-the-lung
#20
Shintaro Hashimoto, Naoya Yamasaki, Ryoichiro Doi, Go Hatachi, Ryoutaro Kamohara, Takuro Miyazaki, Keitaro Matsumoto, Tomoshi Tsuchiya, Mikiko Hashisako, Kazuhiro Tabata, Takeshi Nagayasu
A 66-year-old woman underwent right lower lobectomy and partial resection of the middle lobe for Stage I A double lung cancer. Five years after the operation, a routine computed tomography (CT) scan showed a mass on the staple line at the middle lobe. The mass was enlarged on CT scan after 6 months. A definitive diagnosis could not be made by bronchoscopic examination and fluoro-2-deoxy-glucose(FDG)/positron emission tomography( PET)-CT showed FDG uptake in the mass( early phase:SUVmax=3.24, late phase:SUVmax=4...
March 2017: Kyobu Geka. the Japanese Journal of Thoracic Surgery
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