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https://www.readbyqxmd.com/read/28616954/surface-charge-and-particle-size-determine-the-metabolic-fate-of-dendritic-polyglycerols
#1
Kritee Pant, Johanna Pufe, Kristof Zarschler, Ralf Bergmann, Jörg Steinbach, Sabine Reimann, Rainer Haag, Jens Pietzsch, Holger Stephan
Dendritic polyglycerols (dPG) are water soluble, polyether-based nanomaterials which hold great potential in diagnostic as well as therapeutic applications. In order to translate them for in vivo applications, a systematic assessment regarding their cell and tissue interactions as well as their metabolic fate in vivo is a crucial step. Herein, we explore the structure-activity relationship of three different sizes (ca. 3, 5, and 10 nm) of neutral dendritic polyglycerol (dPG) and their corresponding negatively charged sulfate analogs (dPGS) on their in vitro and in vivo characteristics...
June 15, 2017: Nanoscale
https://www.readbyqxmd.com/read/28598691/development-of-68-ga-scn-dota-capsaicin-as-an-imaging-agent-targeting-apoptosis-and-cell-cycle-arrest-in-breast-cancer
#2
Jun Young Lee, Sang-Yeun Lee, Gun Gyun Kim, Min Goo Hur, Seung Dae Yang, Jeong-Hoon Park, Sang Wook Kim
(68)Ga-labeled capsaicin using a DOTA (1,4,7,10-tetraazocyclododecane-N,N',N″,N'″-tetraacetic acid) derivative [(68)Ga-SCN-Benzyl(Bn)-DOTA-capsaicin] was studied for the diagnosis of breast cancers, such as MCF-7 and SK-BR-3. The standard compound, (69)Ga-SCN-Bn-DOTA-capsaicin, was also prepared and characterized by spectroscopic analysis. The binding affinity of (68)Ga-SCN-Bn-DOTA-capsaicin was evaluated by using breast cancer cell lines (MCF-7, SK-BR-3) and colon cancer cell (CT-26); the biodistribution was carried out by using MCF-7-bearing nude mice, after which the positron emission tomography (PET) images were obtained at different time intervals (15-120 minutes)...
June 2017: Cancer Biotherapy & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28591728/generation-and-evaluation-of-antibody-agents-for-molecular-imaging-of-cd44v6-expressing-cancers
#3
Anna-Karin Haylock, Johan Nilvebrant, Anja Mortensen, Irina Velikyan, Marika Nestor, Ronny Falk
AIM: The aim of this study was to generate and characterize scFv antibodies directed to human CD44v6, as well as to radiolabel and evaluate top candidates in vitro and in vivo for their potential use in CD44v6-targeted molecular imaging in cancer patients. MATERIALS AND METHODS: Phage display selections were used to isolate CD44v6-specific scFvs. A chain shuffling strategy was employed for affinity maturation based on a set of CD44v6-specific first-generation clones...
May 18, 2017: Oncotarget
https://www.readbyqxmd.com/read/28570736/preclinical-pet-study-of-intravitreal-injections
#4
Anxo Fernández-Ferreiro, Andrea Luaces-Rodríguez, Pablo Aguiar, Juan Pardo-Montero, Miguel González-Barcia, Lara García-Varela, Michel Herranz, Jesús Silva-Rodríguez, María Gil-Martínez, María A Bermúdez, Alba Vieites-Prado, José Blanco-Méndez, María Jesús Lamas, Francisco Gómez-Ulla, Álvaro Ruibal, Francisco Javier Otero-Espinar, Francisco González
Purpose: This work aimed at describing the time course of vitreous clearance through the use of positron emission tomography (PET) as a noninvasive tool for pharmacokinetic studies of intravitreal injection. Methods: The pharmacokinetic profile of intravitreal injections of molecules labeled with 18Fluorine (18F) was evaluated in adult Sprague Dawley rats by using a dedicated small-animal PET/computed tomography scanner. Different conditions were studied: three molecules radiolabeled with 18F (18F-FDG, 18F-NaF, and 18F-Choline), three volumes of intravitreal injections (7, 4, and 2 μL), and absence or presence of eye inflammation (uveitis)...
June 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28566692/pilot-study-of-64-cu-i-for-pet-imaging-of-melanoma
#5
Lei Jiang, Yingfeng Tu, Xiang Hu, Ande Bao, Hao Chen, Xiaowei Ma, Tim Doyle, Hongcheng Shi, Zhen Cheng
At present, (64)Cu(II) labeled tracers including (64)CuCl2 have been widely applied in the research of molecular imaging and therapy. Human copper transporter 1 (hCTR1) is the major high affinity copper influx transporter in mammalian cells, and specially responsible for the transportation of Cu(I) not Cu(II). Thus, we investigated the feasible application of (64)Cu(I) for PET imaging. (64)Cu(II) was reduced to (64)Cu(I) with the existence of sodium L-ascorbate, DL-Dithiothreitol or cysteine. Cell uptake and efflux assay was investigated using B16F10 and A375 cell lines, respectively...
May 31, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28562337/il13ra2-targeted-alpha-particle-therapy-against-glioblastomas
#6
Anirudh Sattiraju, Kiran Kumar Solingapuram Sai, Ang Xuan, Darpan N Pandya, Frankis G Almaguel, Thaddeus J Wadas, Denise M Herpai, Waldemar Debinski, Akiva Mintz
Glioblastoma (GBM) is the most aggressive primary malignant brain cancer that invariably results in a dismal prognosis. Chemotherapy and radiotherapy have not been completely effective as standard treatment options for patients due to recurrent disease. We and others have therefore developed molecular strategies to specifically target interleukin 13 receptor alpha 2 (IL13RA2), a GBM restricted receptor expressed abundantly on over 75% of GBM patients. In this work, we evaluated the potential of Pep-1L, a novel IL13RA2 targeted peptide, as a platform to deliver targeted lethal therapies to GBM...
May 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28516169/hybrid-pixel-waveform-hpwf-enabled-cdte-detectors-for-small-animal-gamma-ray-imaging-applications
#7
A Groll, K Kim, H Bhatia, J C Zhang, J H Wang, Z M Shen, L Cai, J Dutta, Q Li, L J Meng
This paper presents the design and preliminary evaluation of small-pixel CdTe gamma ray detectors equipped with a hybrid pixel-waveform (HPWF) readout system for gamma ray imaging applications with additional discussion on CZT due to its similarity. The HPWF readout system utilizes a pixelated anode readout circuitry which is designed to only provide the pixel address. This readout circuitry works in coincidence with a high-speed digitizer to sample the cathode waveform which provides the energy, timing, and depth-of-interaction (DOI) information...
January 2017: IEEE transactions on radiation and plasma medical sciences
https://www.readbyqxmd.com/read/28468949/identification-of-a-novel-the-itg%C3%AE-v%C3%AE-6-binding-peptide-using-protein-separation-and-phage-display
#8
Uwe Haberkorn, Annette Altmann, Max Sauter, Saskia Roesch, Walter Mier, Rolf Warta, Juergen Debus, Gerhard Dyckhoff, Christel Herold-Mende
PURPOSE: Targeted therapies are regarded as promising approaches to increase 5-year survival rate of head and neck squamous cell carcinoma (HNSCC) patients. EXPERIMENTAL DESIGN: For the selection of carcinoma-specific peptides membrane proteome of HNO97 tumor cells fractionated by the ProteomeLab™ PF2D system and corresponding HNO97 cells were deployed for an alternating biopanning using a sunflower trypsin inhibitor1-based phage display (SFTI8Ph) library. Stability, binding properties and affinity of novel candidates were assessed in vitro using radio-HPLC, binding experiments and surface plasmon resonance assay (SPR), respectively...
May 3, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28412013/investigation-of-the-imaging-characteristics-of-the-albira-ii-small-animal-pet-system-for-18-f-68-ga-and-64-cu
#9
Ali Asgar Attarwala, Yvonne Wanjiku Karanja, Deni Hardiansyah, Chiara Romanó, Mareike Roscher, Björn Wängler, Gerhard Glatting
AIM: In this study the performance characteristics of the Albira II PET sub-system and the response of the system for the following radionuclides (18)F, (68)Ga and (64)Cu was analyzed. MATERIALS AND METHODS: The Albira II tri-modal system (Bruker BioSpin MRI GmbH, Ettlingen, Germany) is a pre-clinical device for PET, SPECT and CT. The PET sub-system uses single continuous crystal detectors of lutetium yttrium orthosilicate (LYSO). The detector assembly consists of three rings of 8 detector modules...
April 12, 2017: Zeitschrift Für Medizinische Physik
https://www.readbyqxmd.com/read/28382139/in-vivo-imaging-of-experimental-melanoma-tumors-using-the-novel-radiotracer-68-ga-nodaga-procainamide-pca
#10
István Kertész, András Vida, Gábor Nagy, Miklós Emri, Antal Farkas, Adrienn Kis, János Angyal, Noémi Dénes, Judit P Szabó, Tünde Kovács, Péter Bai, György Trencsényi
PURPOSE: The most aggressive form of skin cancer is the malignant melanoma. Because of its high metastatic potential the early detection of primary melanoma tumors and metastases using non-invasive PET imaging determines the outcome of the disease. Previous studies have already shown that benzamide derivatives, such as procainamide (PCA) specifically bind to melanin pigment. The aim of this study was to synthesize and investigate the melanin specificity of the novel (68)Ga-labeled NODAGA-PCA molecule in vitro and in vivo using PET techniques...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/28361250/influence-of-co-57-and-ct-transmission-measurements-on-the-quantification-accuracy-and-partial-volume-effect-of-a-small-animal-pet-scanner
#11
Julia G Mannheim, Andreas M Schmid, Bernd J Pichler
PURPOSE: Non-invasive in vivo positron emission tomography (PET) provides high detection sensitivity in the nano- to picomolar range and in addition to other advantages, the possibility to absolutely quantify the acquired data. The present study focuses on the comparison of transmission data acquired with an X-ray computed tomography (CT) scanner or a Co-57 source for the Inveon small animal PET scanner (Siemens Healthcare, Knoxville, TN, USA), as well as determines their influences on the quantification accuracy and partial volume effect (PVE)...
March 30, 2017: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://www.readbyqxmd.com/read/28301817/simple-and-rapid-radiosynthesis-of-n-18-f-labeled-glutamic-acid-as-a-hepatocellular-carcinoma-pet-tracer
#12
Aixia Sun, Shaoyu Liu, Xiaolan Tang, Dahong Nie, Ganghua Tang, Zhanwen Zhang, Fuhua Wen, Xiaoyan Wang
INTRODUCTION: We have reported that N-(2-(18)F-fluoropropionyl)-L-glutamate ((18)F-FPGLU) showed good tumor-to-background contrast and (18)F-FPGLU was prepared via complex multi-step reaction sequence; here, it is synthesized by a facile two-step reaction sequence. The objectives of this study are to synthesize (18)F-FPGLU via a two-step reaction sequence and to evaluate the value of (18)F-FPGLU in nude mice bearing human hepatocellular carcinoma SMCC-7721 (HCC SMCC-7721). METHODS: (18)F-FPGLU was synthetized from the precursor (2S)-dimethyl 2-(2-bromopropanamido)pentanedioate via the two-step on-column hydrolysis using a modified commercial FDG synthesizer...
June 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28219717/effects-of-tetrahydrocannabinol-on-glucose-uptake-in-the-rat-brain
#13
I Miederer, K Uebbing, J Röhrich, S Maus, N Bausbacher, K Krauter, V Weyer-Elberich, B Lutz, M Schreckenberger, R Urban
Δ(9)-Tetrahydrocannabinol (THC) is the psychoactive component of the plant Cannabis sativa and acts as a partial agonist at cannabinoid type 1 and type 2 receptors in the brain. The goal of this study was to assess the effect of THC on the cerebral glucose uptake in the rat brain. 21 male Sprague Dawley rats (12-13 w) were examined and received five different doses of THC ranging from 0.01 to 1 mg/kg. For data acquisition a Focus 120 small animal PET scanner was used and 24.1-28.0 MBq of [(18)F]-fluoro-2-deoxy-d-glucose were injected...
February 20, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28146242/positron-emission-tomography-for-the-development-and-characterization-of-corneal-permanence-of-ophthalmic-pharmaceutical-formulations
#14
Anxo Fernández-Ferreiro, Jesús Silva-Rodríguez, Francisco Javier Otero-Espinar, Miguel González-Barcia, María Jesús Lamas, Alvaro Ruibal, Andrea Luaces-Rodriguez, Alba Vieites-Prado, Tomas Sobrino, Michel Herranz, Lara García-Varela, José Blanco-Mendez, María Gil-Martínez, María Pardo, Alexis Moscoso, Santiago Medín-Aguerre, Juan Pardo-Montero, Pablo Aguiar
Purpose: This work is aimed at describing the utility of positron emission tomography/computed tomography (PET/CT) as a noninvasive tool for pharmacokinetic studies of biopermanence of topical ocular formulations. Methods: The corneal biopermanence of a topical ophthalmic formulation containing gellan gum and kappa carragenan (0.82% wt/vol) labeled with 18Fluorine (18F) radiotracers (18F-FDG and 18F-NaF) was evaluated by using a dedicated small-animal PET/CT, and compared with the biopermanence of an aqueous solution labeled with the same compounds...
February 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28097210/preclinical-positron-emission-tomography-scanner-based-on-a-monolithic-annulus-of-scintillator-initial-design-study
#15
Alexander V Stolin, Peter F Martone, Gangadhar Jaliparthi, Raymond R Raylman
Positron emission tomography (PET) scanners designed for imaging of small animals have transformed translational research by reducing the necessity to invasively monitor physiology and disease progression. Virtually all of these scanners are based on the use of pixelated detector modules arranged in rings. This design, while generally successful, has some limitations. Specifically, use of discrete detector modules to construct PET scanners reduces detection sensitivity and can introduce artifacts in reconstructed images, requiring the use of correction methods...
January 2017: Journal of Medical Imaging
https://www.readbyqxmd.com/read/28049619/synthesis-and-evaluation-of-1-cyclopropylmethyl-4-4-11-c-methoxyphenyl-piperidin-1-yl-2-oxo-1-2-dihydropyridine-3-carbonitrile-11-c-cmdc-for-pet-imaging-of-metabotropic-glutamate-receptor-2-in-the-rat-brain
#16
Yufei Ma, Katsushi Kumata, Joji Yui, Yiding Zhang, Tomoteru Yamasaki, Akiko Hatori, Masayuki Fujinaga, Nobuki Nengaki, Lin Xie, Hui Wang, Ming-Rong Zhang
Brain metabotropic glutamate receptor 2 (mGluR2) has been proposed as a therapeutic target for the treatment of schizophrenia-like symptoms arising from increased glutamate transmission in the forebrain. However, there does not exist a reliable tool for the study of mGluR2 in human neuroimaging. The purpose of this study was to radiosynthesize 1-(cyclopropylmethyl)-4-(4-[(11)C]methoxyphenyl)piperidin-1-yl-2-oxo-1,2-dihydropyridine-3-carbonitrile ([(11)C]CMDC) and evaluate its potential as a positron emission tomography (PET) radiotracer for imaging mGluR2 in the rat brain...
December 23, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28034351/synthesis-and-preliminary-evaluation-of-5-18f-fluoroleucine
#17
Bennett B Chin, Darryl McDougald, Douglas Weitzel, Thomas Hawk, Robert E Reiman, Michael R Zalutsky, Ganesan Vaidyanathan
BACKGROUND: Amino acid transporters, such as LAT1, are overexpressed in aggressive prostate and breast carcinomas, directly influencing pathways of growth and proliferation. OBJECTIVE: The purpose of this study is to synthesize and characterize a novel 18F labeled leucine analog, 5-[18F]fluoroleucine, as a potential imaging agent for aggressive tumors which may not be amenable to imaging by FDG PET. METHODS: 5-fluoroleucine was synthesized and characterized, and its 18F-labeled analog was synthesized from a mesylate precursor...
December 30, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27995432/investigation-of-image-reconstruction-parameters-of-the-mediso-nanoscan-pc-small-animal-pet-ct-scanner-for-two-different-positron-emitters-under-nema-nu-4-2008-standards
#18
Anastasios Gaitanis, George A Kastis, Elena Vlastou, Penelope Bouziotis, Panayotis Verginis, Constantinos D Anagnostopoulos
PURPOSE: The Tera-Tomo 3D image reconstruction algorithm (a version of OSEM), provided with the Mediso nanoScan® PC (PET8/2) small-animal positron emission tomograph (PET)/x-ray computed tomography (CT) scanner, has various parameter options such as total level of regularization, subsets, and iterations. Also, the acquisition time in PET plays an important role. This study aims to assess the performance of this new small-animal PET/CT scanner for different acquisition times and reconstruction parameters, for 2-deoxy-2-[(18)F]fluoro-D-glucose ([(18)F]FDG) and Ga-68, under the NEMA NU 4-2008 standards...
December 19, 2016: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://www.readbyqxmd.com/read/27992512/68ga-trap-rgd-3-hybrid-imaging-for-the-in-vivo-monitoring-of-%C3%AE-v%C3%A3-3-integrin-expression-as-biomarker-of-anti-angiogenic-therapy-effects-in-experimental-breast-cancer
#19
Philipp M Kazmierczak, Andrei Todica, Franz-Josef Gildehaus, Heidrun Hirner-Eppeneder, Matthias Brendel, Ralf S Eschbach, Magdalena Hellmann, Konstantin Nikolaou, Maximilian F Reiser, Hans-Jürgen Wester, Saskia Kropf, Axel Rominger, Clemens C Cyran
OBJECTIVES: To investigate 68Ga-TRAP-(RGD)3 hybrid imaging for the in vivo monitoring of αvß3-integrin expression as biomarker of anti-angiogenic therapy effects in experimental breast cancer. MATERIALS AND METHODS: Human breast cancer (MDA-MB-231) xenografts were implanted orthotopically into the mammary fat pads of n = 25 SCID mice. Transmission/emission scans (53 min to 90 min after i.v. injection of 20 MBq 68Ga-TRAP-(RGD)3) were performed on a dedicated small animal PET before (day 0, baseline) and after (day 7, follow-up) a 1-week therapy with the VEGF antibody bevacizumab or placebo (imaging cohort n = 13; therapy n = 7, control n = 6)...
2016: PloS One
https://www.readbyqxmd.com/read/27957722/dynamic-pet-evaluation-of-elevated-flt-level-after-sorafenib-treatment-in-mice-bearing-human-renal-cell-carcinoma-xenograft
#20
Naoyuki Ukon, Songji Zhao, Wenwen Yu, Yoichi Shimizu, Ken-Ichi Nishijima, Naoki Kubo, Yoshimasa Kitagawa, Nagara Tamaki, Kei Higashikawa, Hironobu Yasui, Yuji Kuge
BACKGROUND: Sorafenib, an oral multikinase inhibitor, has anti-proliferative and anti-angiogenic activities and is therapeutically effective against renal cell carcinoma (RCC). Recently, we have evaluated the tumor responses to sorafenib treatment in a RCC xenograft using [Methyl-(3)H(N)]-3'-fluoro-3'-deoxythythymidine ([(3)H]FLT). Contrary to our expectation, the FLT level in the tumor significantly increased after the treatment. In this study, to clarify the reason for the elevated FLT level, dynamic 3'-[(18)F]fluoro-3'-deoxythymidine ([(18)F]FLT) positron emission tomography (PET) and kinetic studies were performed in mice bearing a RCC xenograft (A498)...
December 2016: EJNMMI Research
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