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Nuclear Medicine and Biology

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https://www.readbyqxmd.com/read/28636973/amide-to-triazole-switch-vs-in-vivo-nep-inhibition-approaches-to-promote-radiopeptide-targeting-of-grpr-positive-tumors
#1
Theodosia Maina, Aikaterini Kaloudi, Ibai E Valverde, Thomas L Mindt, Berthold A Nock
INTRODUCTION: Radiolabeled bombesin (BBN)-analogs have been proposed for diagnosis and therapy of gastrin-releasing peptide receptor (GRPR)-expressing tumors, such as prostate, breast and lung cancer. Metabolic stability represents a crucial factor for the success of this approach by ensuring sufficient delivery of circulating radioligand to tumor sites. The amide-to-triazole switch on the backbone of DOTA-PEG4-[Nle(14)]BBN(7-14) (1) was reported to improve the in vitro stability of resulting (177)Lu-radioligands...
June 10, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28628775/developing-new-pet-tracers-to-image-the-growth-hormone-secretagogue-receptor-1a-ghs-r1a
#2
Kazunori Kawamura, Masayuki Fujinaga, Yoko Shimoda, Tomoteru Yamasaki, Yiding Zhang, Akiko Hatori, Lin Xie, Hidekatsu Wakizaka, Katsushi Kumata, Takayuki Ohkubo, Yusuke Kurihara, Masanao Ogawa, Nobuki Nengaki, Ming-Rong Zhang
INTRODUCTION: `The growth hormone secretagogue receptor 1a (GHS-R1a) is the orphan G-protein-coupled receptor, and its endogenous ligand is ghrelin. GHS-R1a contributes to regulation of glucose homeostasis, memory and learning, food addiction, and neuroprotection. Several PET tracers for GHS-R1a have been developed, but none have been reported to be clinically applicable to GHS-R1a imaging. In this study, we developed three new PET tracers for GHS-R1a: (18)F-labeled 6-(4-chlorophenyl)-3-((1-(2-fluoroethyl)piperidin-3-yl)methyl)-2-(o-tolyl)quinazolin-4(3H)-one (1), (11)C-labeled 6-(4-chlorophenyl)-3-((1-(2-methoxyethyl)piperidin-3-yl)methyl)-2-(o-tolyl)quinazolin-4(3H)-one (2), and (11)C-labeled (S)-(4-(1H-indole-6-carbonyl)-3-methylpiperazin-1-yl)(4'-methoxy-[1,1'-biphenyl]-4-yl)methanone (3)...
June 10, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28599133/dose-on-demand-production-of-diverse-18-f-radiotracers-for-preclinical-applications-using-a-continuous-flow-microfluidic-system
#3
Lidia Matesic, Annukka Kallinen, Ivan Greguric, Giancarlo Pascali
INTRODUCTION: The production of (18)F-radiotracers using continuous flow microfluidics is under-utilized due to perceived equipment limitations. We describe the dose-on-demand principle, whereby the back-to-back production of multiple, diverse (18)F-radiotracers can be prepared on the same day, on the same microfluidic system using the same batch of [(18)F]fluoride, the same microreactor, the same HPLC column and SPE cartridge to obtain a useful production yield. METHODS: [(18)F]MEL050, [(18)F]Fallypride and [(18)F]PBR111 were radiolabeled with [(18)F]fluoride using the Advion NanoTek Microfluidic Synthesis System...
June 2, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28624669/neutron-activatable-radionuclide-cancer-therapy-using-graphene-oxide-nanoplatelets
#4
Junghyun Kim, Michael Jay
Neutron-activation is a promising method of generating radiotherapeutics with minimal handling of radioactive materials. Graphene oxide nanoplatelets (GONs) were examined as a carrier for neutron-activatable holmium with the purpose of exploiting inherent characteristics for theranostic application. GONs were hypothesized to be an ideal candidate for this application owing to their desirable characteristics such as a rigid structure, high metal loading capacity, low density, heat resistance, and the ability to withstand harsh environments associated with the neutron-activation process...
June 1, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28602965/-67-ga-labeled-deferoxamine-derivatives-for-imaging-bacterial-infection-preparation-and-screening-of-functionalized-siderophore-complexes
#5
Joseph A Ioppolo, Deanna Caldwell, Omid Beiraghi, Lisset Llano, Megan Blacker, John F Valliant, Paul J Berti
INTRODUCTION: Deferoxamine (DFO) is a siderophore that bacteria use to scavenge iron and could serve as a targeting vector to image bacterial infection where current techniques have critical limitations. [(67)Ga]-DFO, which is a mimetic of the corresponding iron complex, is taken up by bacteria in culture, however in vivo it clears too rapidly to allow for imaging of infection. In response, we developed several new DFO derivatives to identify those that accumulate in bacteria, and at sites of infection, and that could potentially have improved pharmacokinetics...
June 1, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28578290/-131-i-labeled-chitosan-hydrogels-for-radioembolization-a-preclinical-study-in-small-animals
#6
Hyosook Hwang, Kwang Il Kim, JeongIl Kwon, Byoung Soo Kim, Hwan-Seok Jeong, Su Jin Jang, Phil-Sun Oh, Ho Sung Park, Seok Tae Lim, Myung-Hee Sohn, Hwan-Jeong Jeong
INTRODUCTION: The purpose of the study was to examine potential of (131)I-labeled chitosan hydrogels (Chi) for treatment of liver cancer. METHODS: Orthotopic hepatoma was induced by McA-RH7777-fLuc cells (1×10(7)) that were injected into the left hepatic lobe of rats. Ten days later, tumor-bearing rats evidenced by bioluminescence received (125)I-labeled Chi with left hepatic artery access. Pharmacokinetics and excretion (n=8) and biodistribution (n=6/time point) were studied after injection...
May 25, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28575795/-11-c-erlotinib-pet-cannot-detect-acquired-erlotinib-resistance-in-nsclc-tumor-xenografts-in-mice
#7
Alexander Traxl, Taraneh Beikbaghban, Thomas Wanek, Kushtrim Kryeziu, Christine Pirker, Severin Mairinger, Johann Stanek, Thomas Filip, Michael Sauberer, Claudia Kuntner, Walter Berger, Oliver Langer
INTRODUCTION: [(11)C]Erlotinib PET has shown promise to distinguish non-small cell lung cancer (NSCLC) tumors harboring the activating epidermal growth factor receptor (EGFR) mutation delE746-A750 from tumors with wild-type EGFR. To assess the suitability of [(11)C]erlotinib PET to detect the emergence of acquired erlotinib resistance in initially erlotinib-responsive tumors, we performed in vitro binding and PET experiments in mice bearing tumor xenografts using a range of different cancer cells, which were erlotinib-sensitive or exhibited clinically relevant resistance mechanisms to erlotinib...
May 25, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28575794/-99m-tc-labeled-psma-inhibitor-biokinetics-and-radiation-dosimetry-in-healthy-subjects-and-imaging-of-prostate-cancer-tumors-in-patients
#8
Clara Santos-Cuevas, Jenny Davanzo, Guillermina Ferro-Flores, Francisco O García-Pérez, Blanca Ocampo-García, Eleazar Ignacio-Alvarez, Edgar Gómez-Argumosa, Martha Pedraza-López
The prostate-specific membrane antigen (PSMA) is expressed in epithelial cells of the prostate and highly overexpressed in 95% of advanced prostate cancers. The aims of this study was to estimate the biokinetics and dosimetry of (99m)Tc-EDDA/HYNIC-iPSMA ((99m)Tc-labeled PSMA inhibitor) in eight healthy subjects and evaluate its usefulness as a tumor-imaging agent in eight prostate cancer patients. METHODS: (99m)Tc-EDDA/HYNIC-iPSMA was obtained from a lyophilized formulation with radiochemical purities >98%, determined by reversed-phase HPLC and ITLC-SG analyses...
May 25, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28528264/baseline-and-longitudinal-variability-of-normal-tissue-uptake-values-of-18-f-fluorothymidine-pet-images
#9
Matthijs C F Cysouw, Gerbrand M Kramer, Virginie Frings, Adrianus J De Langen, Mariëlle J Wondergem, Laura M Kenny, Eric O Aboagye, Carsten Kobe, Jürgen Wolf, Otto S Hoekstra, Ronald Boellaard
PURPOSE: [(18)F]-fluorothymidine ([(18)F]-FLT) is a PET-tracer enabling in-vivo visualization and quantification of tumor cell proliferation. For qualitative and quantitative analysis, adequate knowledge of normal tissue uptake is indispensable. This study aimed to quantitatively investigate baseline tracer uptake of blood pool, lung, liver and bone marrow and their precision, and to assess the longitudinal effect of systemic treatment on biodistribution. METHODS: (18)F-FLT-PET(/CT) scans (dynamic or static) of 90 treatment-naïve oncological patients were retrospectively evaluated...
May 10, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28528265/synthesis-radiolabeling-and-preclinical-evaluation-of-a-11-c-gmom-derivative-as-pet-radiotracer-for-the-ion-channel-of-the-n-methyl-d-aspartate-receptor
#10
Pieter J Klein, Robert C Schuit, Athanasios Metaxas, Johannes Am Christiaans, Esther Kooijman, Adriaan A Lammertsma, Bart Nm van Berckel, Albert D Windhorst
INTRODUCTION: Presently available PET ligands for the NMDAr ion channel generally suffer from fast metabolism. The purpose of this study was to develop a metabolically more stable ligand for the NMDAr ion channel, taking [(11)C]GMOM ([(11)C]1) as the lead compound. METHODS: [(11)C]1, its fluoralkyl analogue [(18)F]PK209 ([(18)F]2) and the newly synthesized fluorovinyloxy analogue [(11)C]7b were evaluated ex vivo in male Wistar rats for metabolic stability. In addition, [(11)C]7b was subjected to a biodistribution study and its affinity (Ki) and lipophilicity (logD7...
May 8, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28511073/preparation-and-evaluation-of-l-and-d-5-18-f-fluorotryptophan-as-pet-imaging-probes-for-indoleamine-and-tryptophan-2-3-dioxygenases
#11
Tang Tang, Herman S Gill, Annie Ogasawara, Jeff N Tinianow, Alexander N Vanderbilt, Simon-Peter Williams, Georgia Hatzivassiliou, Sharla White, Wendy Sandoval, Kevin DeMent, Mengling Wong, Jan Marik
Indoleamine and tryptophan 2,3-dioxygenases (IDO1 and TDO2) are pyrrolases catalyzing the oxidative cleavage of the 2,3-double bond of L-tryptophan in kynurenine pathway. In the tumor microenvironment, their increased activity prevents normal immune function, i.e. tumor cell recognition and elimination by cytotoxic T-cells. Consequently, inhibition of the kynurenine pathway may enhance the activity of cancer immunotherapeutics by reversing immune dysfunction. We sought to investigate the properties of radiolabeled 5-[(18)F]fluorotryptophan with respect to its ability for measuring IDO1 and TDO2 activity by positron emission tomography (PET)...
May 5, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28577428/vapc-1-targeted-64-cu-tp3805-kit-preparation-and-its-evaluation
#12
Sushil K Tripathi, Pardeep Kumar, Edouard J Trabulsi, Sung Kim, Peter A McCue, Charles Intenzo, Adam Berger, Leonard Gomella, Mathew L Thakur
INTRODUCTION: Previously, our laboratory has shown that (64)Cu-TP3805 can specifically target VPAC-1 receptors and be used for positron emission tomography (PET) imaging of breast (BC) and prostate cancer (PC) in humans. Present work is aimed at the formulation of a freeze-dried diaminedithiol-peptide (N2S2-TP3805) kit and it's evaluation for the preparation of (64)Cu labeled TP3805. Parameters such as pH, temperature and incubation time were examined that influenced the radiolabeling efficiency and stability of the product...
May 3, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28575696/regiospecific-radiolabelling-of-nanofitin-on-ni-magnetic-beads-with-18-f-fbem-and-in-vivo-pet-studies
#13
Sylvestre Dammicco, Marine Goux, Christian Lemaire, Guillaume Becker, Mohamed Ali Bahri, Alain Plenevaux, Mathieu Cinier, André Luxen
INTRODUCTION: Nanofitins are low molecular weight, single chain and cysteine-free protein scaffolds able to selectively bind a defined biological target. They derive from Sac7d bacterial protein family and are highly stable over a wide range of pH (0-13) and temperature (Tm ~80°C). Their extreme stability, low cost of production and high tolerability for chemical coupling make Nanofitins a very interesting alternative to antibodies and their fragments. Here, a hexahistidine tagged model Nanofitin (H4) directed against hen egg white lysozyme was radiolabelled and injected in mice to provide a baseline biodistribution and pharmacokinetic profiles to support future Nanofitin development programs...
April 27, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28486098/preparation-of-212-pb-labeled-monoclonal-antibody-using-a-novel-224-ra-based-generator-solution
#14
Sara Westrøm, Roman Generalov, Tina B Bønsdorff, Roy H Larsen
INTRODUCTION: Alpha-emitting radionuclides have gained considerable attention as payloads for cancer targeting molecules due to their high cytotoxicity. One attractive radionuclide for this purpose is (212)Pb, which by itself is a β-emitter, but acts as an in vivo generator for its short-lived α-emitting daughters. The standard method of preparing (212)Pb-labeled antibodies requires handling and evaporation of strong acids containing high radioactivity levels by the end user. An operationally easier and more rapid process could be useful since the 10...
April 26, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28575697/pet-ct-with-18-f-choline-physiological-whole-bio-distribution-in-male-and-female-subjects-and-diagnostic-pitfalls-on-1000-prostate-cancer-patients-18-f-choline-pet-ct-bio-distribution-and-pitfalls-a-southern-italian-experience
#15
Ferdinando Calabria, Agostino Chiaravalloti, Carmelo Cicciò, Vincenzo Gangemi, Domenico Gullà, Federico Rocca, Gianpasquale Gallo, Giuseppe Lucio Cascini, Orazio Schillaci
INTRODUCTION: The (11)C/(18)F-choline is a PET/CT radiopharmaceutical useful in detecting tumors with high lipogenesis. (11)C/(18)F-choline uptake can occur in physiological conditions or tumors. The knowledge of its bio-distribution is essential to recognize physiologic variants or diagnostic pitfalls. Moreover, few information are available on the bio-distribution of this tracer in female patients. Our aim was to discuss some documented (18)F-choline PET/CT pitfalls in prostate cancer patients...
April 17, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28426991/clinical-usefulness-of-18-f-fdg-pet-ct-for-initial-staging-and-assessment-of-treatment-efficacy-in-patients-with-lymph-node-tuberculosis
#16
Nicolas Lefebvre, Xavier Argemi, Nicolas Meyer, Joy Mootien, Nawal Douiri, Stefania Sferrazza-Mandala, Frédéric Schramm, Noëlle Weingertner, Daniel Christmann, Yves Hansmann, Alessio Imperiale
INTRODUCTION: Few studies have evaluated the promising role of (18)F-fluoro-2-deoxy-D-glucose positron emission tomography (PET) and PET/computed tomography FDG PET/CT in evaluating and monitoring treatment response in patients with lymph node tuberculosis (LNTB). The aim of this clinical investigation was to assess the clinical usefulness of FDG PET/CT for initial tuberculosis staging and to determine the prognostic value of the decrease of (18)F-FDG uptake during antibiotic treatment in LNTB patients...
April 8, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28456080/radiosynthesis-and-biological-evaluation-of-n-2-18-f-fluoropropionyl-3-4-dihydroxy-l-phenylalanine-as-a-pet-tracer-for-oncologic-imaging
#17
Caihua Tang, Dahong Nie, Ganghua Tang, Siyuan Gao, Shaoyu Liu, Fuhua Wen, Xiaolan Tang
INTRODUCTION: Several (11)C and (18)F labeled 3,4-dihydroxy-l-phenylalanine (l-DOPA) analogues have been used for neurologic and oncologic diseases, especially for brain tumors and neuroendocrine tumors PET imaging. However, (18)F-labeled N-substituted l-DOPA analogues have not been reported so far. In the current study, radiosynthesis and biological evaluation of a new (18)F-labeled l-DOPA analogue, N-(2-[(18)F]fluoropropionyl)-3,4-dihydroxy-l-phenylalanine ([(18)F]FPDOPA) for tumor PET imaging are performed...
April 7, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28433794/detection-of-melanoma-metastases-with-pet-comparison-of-18-f-5-fpn-with-18-f-fdg
#18
Yichun Wang, Mengting Li, Yingying Zhang, Fengzhen Zhang, Chunbao Liu, Yiling Song, Yongxue Zhang, Xiaoli Lan
INTRODUCTION: (18)F-5-fluoro-N-(2-(Diethylamino)ethyl)picolinamide ((18)F-5-FPN) is a new positron-emission tomography (PET) radiopharmaceutical with potential for the detection of lymph node (LN) and pulmonary metastatic lesions of melanoma. We compared its performance with that of (18)F-deoxyglucose ((18)F-FDG). METHODS: Cervical LN and lung melanoma metastasis models were established in C57BL/6 mice. Primary tumors were created by injection of melanoma cells into the pinna, and the resulting cervical LN metastases were evaluated...
April 7, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28432915/proton-induced-production-and-radiochemical-isolation-of-44-ti-from-scandium-metal-targets-for-44-ti-44-sc-generator-development
#19
Valery Radchenko, Jonathan W Engle, Dmitri G Medvedev, Joel M Maassen, Cleo M Naranjo, George A Unc, Catherine A L Meyer, Tara Mastren, Mark Brugh, Leonard Mausner, Cathy S Cutler, Eva R Birnbaum, Kevin D John, F Meiring Nortier, Michael E Fassbender
Scandium-44g (half-life 3.97h) shows promise for application in positron emission tomography (PET), due to favorable decay parameters. One of the sources of (44g)Sc is the (44)Ti/(44g)Sc generator, which can conveniently provide this radioisotope on a daily basis at a diagnostic facility. Titanium-44 (half-life 60.0 a), in turn, can be obtained via proton irradiation of scandium metal targets. A substantial (44)Ti product batch, however, requires high beam currents, long irradiation times and an elaborate chemical procedure for (44)Ti isolation and purification...
April 7, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28438468/clinical-results-and-economic-considerations-of-68-ga-psma-and-radiolabeled-choline-in-prostate-cancer
#20
Laura Evangelista, Maria Giuseppina Bonavina, Emilio Bombardieri
In recent years there was an impressive improvement in the options for the management of patients with prostate cancer. Nuclear Medicine has significantly enriched its diagnostic options, both in radiopharmacy and in instrumentation, in order to accurately target prostatic cancer cells, thus rendering the physicians able to adopt the best therapeutic strategy. In the present analysis, we have evaluated the available published data about 68Ga-PSMA and radio-labeled choline, two radiopharmaceutical agents for positron emission tomography/computed tomography (PET/CT) examination, by reporting clinical information and considering data about legal, economic and organization aspects...
April 5, 2017: Nuclear Medicine and Biology
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