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Nuclear Medicine and Biology

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https://www.readbyqxmd.com/read/29929115/matched-pair-86-y-90-y-labeled-bivalent-rgd-bombesin-antagonist-rgd-glu-do3a-6-ahx-rm2-as-a-potential-theranostic-agent-for-prostate-cancer
#1
Nilantha Bandara, Tamila J Stott Reynolds, Rebecca Schehr, Rajendra P Bandari, Philipp J Diebolder, Stephanie Krieger, Jingli Xu, Yubin Miao, Buck E Rogers, Charles J Smith
INTRODUCTION: In this study, we describe development of a true matched-pair theranostic agent that is able to target the αV β3 integrin and the gastrin releasing peptide receptor (GRPR). We herein describe methods to metallate and characterize the new conjugate and to validate its biological efficacy by in vitro and in vivo methods. METHODS: We have previously described the development of [RGD-Glu-6Ahx-RM2] (where RGD: Arg-Gly-Asp; Glu: glutamic acid; 6-Ahx: 6-amino hexanoic acid; RM2: (D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2)) that has been conjugated to a DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) bifunctional chelating agent (BFCA) to afford [RGD-Glu-[DO3A]-6-Ahx-RM2] peptide...
June 8, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29885559/-99m-tc-d-lpr-a-novel-retro-inverso-peptide-for-vegf-receptor-1-targeted-tumor-imaging
#2
Farzaneh Rezazadeh, Nourollah Sadeghzadeh, Seyed Mohammad Abedi, Saeid Abediankenari
INTRODUCTION: The aim of this study was to evaluate the ability of D (LPR), a novel retro-inverso peptidomimetic derivative for imaging colon cancer. METHODS: Two different D (LPR) analogs were designed and compared based on conjugation of HYNIC at peptide's C or N terminal and then labeled with technetium-99m using tricine/EDDA as an exchange coligands. The radiolabeled conjugates were assessed for in vitro stability in saline and serum. The VEGFR-1 and NRP-1 receptors affinity, in vitro internalization and also dissociation Constance was evaluated...
May 31, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29929114/one-pot-synthesis-and-biodistribution-of-fluorine-18-labeled-serum-albumin-for-vascular-imaging
#3
Falguni Basuli, Xiang Zhang, Mark R Williams, Jurgen Seidel, Michael V Green, Peter L Choyke, Rolf E Swenson, Elaine M Jagoda
INTRODUCTION: Equilibrium single-photon radionuclide imaging methods for assessing cardiac function and the integrity of the vascular system have long been in use for both clinical and research purposes. However, positron-emitting blood pool agents that could provide PET equivalents to these (and other) clinical procedures have not yet been adopted despite technical imaging advantages offered by PET. Our goal was to develop a PET blood pool tracer that not only meets necessary in vivo biological requirements but can be produced with an uncomplicated and rapid synthesis method which would facilitate clinical translation...
May 30, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29800797/the-impact-of-age-on-radium-223-distribution-and-an-evaluation-of-molecular-imaging-surrogates
#4
Wen Jiang, David Ulmert, Brian W Simons, Diane S Abou, Daniel L J Thorek
INTRODUCTION: Radium-223 dichloride is the first alpha-particle emitting therapeutic agent approved by FDA and EMA for bone metastatic castration-resistant prostate cancer. We studied its age-dependent biodistribution in mice, and compared it with [99m Tc]Tc-MDP and [18 F]NaF aiming to identify a potential imaging surrogate to predict [223 Ra]RaCl2 whole-body localization. METHODS: Male C57Bl/6 mice dosed with [223 Ra]RaCl2 were sacrificed at different time points to explore [223 Ra]RaCl2 whole-body distribution...
May 8, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29803076/brush-border-enzyme-cleavable-linkers-evaluation-for-reducing-renal-uptake-of-radiolabeled-prostate-specific-membrane-antigen-inhibitors
#5
Ganesan Vaidyanathan, Choong Mo Kang, Darryl McDougald, Il Minn, Mary Brummet, Martin G Pomper, Michael R Zalutsky
INTRODUCTION: Radiolabeled, low-molecular-weight prostate-specific membrane antigen (PSMA) inhibitors based on the Glu-ureido pharmacophore show promise for the detection and treatment of castration-resistant prostate cancer; however, high renal retention of activity, related in part to overexpression of PSMA in kidneys can be problematic. The goal of the current study was to investigate the use of brush border enzyme-cleavable linkers as a strategy for reducing kidney activity levels from radiolabeled PSMA inhibitors...
May 5, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29800798/impact-of-structural-alterations-on-the-radiopharmacological-profile-of-18-f-labeled-pyrimidines-as-cyclooxygenase-2-cox-2-imaging-agents
#6
Ole Tietz, Alison Marshall, Cody Bergman, Melinda Wuest, Frank Wuest
INTRODUCTION: Non-invasive imaging of COX-2 in cancer represents a powerful tool for assessing COX-2-mediated effects on chemoprevention and radiosensitization using potent and selective COX-2 inhibitors as an emerging class of anticancer drugs. Careful assessment of the pharmacokinetic profile of radiolabeled COX-2 inhibitors is of crucial importance for the development of suitable radiotracers for COX-2 imaging in vivo. The delicate balance between the selection of typical COX-2 pharmacophores and the resulting physicochemical characteristics of the COX-2 inhibitor represents a formidable challenge for the search of radiolabeled COX-2 imaging agents...
May 5, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29883883/gallium-68-labeled-ubiquicidin-derived-octapeptide-as-a-potential-infection-imaging-agent
#7
Jyotsna Bhatt, Archana Mukherjee, Ajit Shinto, Kamaleshwaran Koramadai Karuppusamy, Aruna Korde, Mukesh Kumar, Haladhar Dev Sarma, Krishnamohan Repaka, Ashutosh Dash
INTRODUCTION: Gallium-68 based infection imaging agents are in demand to detect infection foci with high spatial resolution and sensitivity. In this study, Ubiquicidin derived octapeptide, UBI (31-38) conjugated with macrocyclic chelator NOTA was radiolabeled with 68 Ga to develop infection imaging agent. METHODS: Circular dichroism (CD) spectroscopy was performed to study conformational changes in UBI (31-38) and its NOTA conjugate in a "membrane like environment"...
May 4, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29807242/what-about-%C3%AE-v-%C3%AE-3-integrins-in-molecular-imaging-in-oncology
#8
REVIEW
Frederic Debordeaux, Lucie Chansel-Debordeaux, Jean-Baptiste Pinaquy, Philippe Fernandez, Jurgen Schulz
Non-invasive investigation of integrin expression is an interesting approach in nuclear medicine department. Indeed, integrins are overexpressed in a wide array of diseases, including tumor neoangiogenesis, cardiovascular pathologies, immune dysfunction, etc. Different targets have been identified in order to be detected and quantified for angiogenesis and vascular remodeling, among them VEGF, matrix metalloproteases, and integrins (αv β3 , but also α5 ß1 and αv β6 ). Their targeting appears of great interest either for early diagnosis, aggressiveness staging of the disease or for selection of responders to new-targeted therapies...
May 4, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29705525/corrigendum-to-212-pb-labeled-b7-h3-targeting-antibody-for-pancreatic-cancer-therapy-in-mouse-models-nucl-med-biol-58-2018-67-73
#9
Benjamin B Kasten, Abhishek Gangrade, Harrison Kim, Jinda Fan, Soldano Ferrone, Cristina R Ferrone, Kurt R Zinn, Donald J Buchsbaum
No abstract text is available yet for this article.
April 25, 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29783202/feasibility-of-myocardial-pet-imaging-using-a-benzylguanidine-analog-meta-3-18-f-fluoropropyl-benzylguanidine-18-f-mfpbg
#10
Sang-Keun Woo, Byung Seok Moon, Bom Sahn Kim, Min Hwan Kim, Yong Jin Lee, Jae Ho Jung, Kyo Chul Lee, Youngho Seo, Wook Kim, Sang Moo Lim, Byung Chul Lee, Sang Eun Kim
INTRODUCTION: Global and regional sympathetic activity in the heart can be evaluated using [123 I]meta-iodobenzylguanidine ([123 I]mIBG) imaging. However, [123 I]mIBG is associated with low image spatial resolution and sensitivity in cardiac imaging. We investigated the capability of an F-18-labeled mIBG derivative, meta-(3-[18 F]fluoropropyl)benzylguanidine ([18 F]mFPBG), for identifying ischemic and viable myocardium in a rat model of myocardial infarction. MATERIALS AND METHODS: The ex vivo biodistribution and in vivo metabolic stability of [18 F]mFPBG were investigated in Sprague-Dawley rats...
June 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29783201/n-4-18-f-fluorobenzyl-cholylglycine-a-novel-tracer-for-pet-of-enterohepatic-circulation-of-bile-acids-radiosynthesis-and-proof-of-concept-studies-in-rats
#11
Kim Frisch, Damion H R Stimson, Taracad Venkatachalam, Gregory K Pierens, Susanne Keiding, David Reutens, Rajiv Bhalla
INTRODUCTION: Enterohepatic circulation (EHC) of conjugated bile acids is an important physiological process crucial for regulation of intracellular concentrations of bile acids and their function as detergents and signal carriers. Only few bile acid-derived imaging agents have been synthesized and hitherto none have been evaluated for studies of EHC. We hypothesized that N-(4-[18 F]fluorobenzyl)cholylglycine ([18 F]FBCGly), a novel fluorine-18 labeled derivative of endogenous cholylglycine, would be a suitable tracer for PET of the EHC of conjugated bile acids, and we report here a radiosynthesis of [18 F]FBCGly and a proof-of-concept study by PET/MR in rats...
June 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29747036/-18-f-ge-179-positron-emission-tomography-pet-tracer-for-n-methyl-d-aspartate-receptors-one-pot-synthesis-and-preliminary-micro-pet-study-in-a-rat-model-of-mcao
#12
Weiyan Zhou, Weiqi Bao, Donglang Jiang, Yanyan Kong, Fengchun Hua, Xiuhong Lu, Yihui Guan
INTRODUCTION: The objective of this study was to synthesize an N-methyl-d-aspartate receptor (NMDAR) radiotracer [18 F]-GE-179 in one-pot and evaluate its in vivo binding for NMDAR activation after brain ischemia reperfusion injury. METHODS: [18 F]-GE-179 was auto-synthesized using a quick one-pot method from a stable disulfide precursor and purified using semi-preparative high-performance liquid chromatography (HPLC) with ethanol/aqueous NaH2 PO4 as the eluent...
June 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29747035/microscale-radiosynthesis-preclinical-imaging-and-dosimetry-study-of-18-f-ambf-3-tate-a-potential-pet-tracer-for-clinical-imaging-of-somatostatin-receptors
#13
Ksenia Lisova, Maxim Sergeev, Susan Evans-Axelsson, Andreea D Stuparu, Seval Beykan, Jeffrey Collins, Jason Jones, Michael Lassmann, Ken Herrmann, David Perrin, Jason T Lee, Roger Slavik, R Michael van Dam
BACKGROUND: Peptides labeled with positron-emitting isotopes are emerging as a versatile class of compounds for the development of highly specific, targeted imaging agents for diagnostic imaging via positron-emission tomography (PET) and for precision medicine via theranostic applications. Despite the success of peptides labeled with gallium-68 (for imaging) or lutetium-177 (for therapy) in the clinical management of patients with neuroendocrine tumors or prostate cancer, there are significant advantages of using fluorine-18 for imaging...
June 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29571068/robust-high-yield-1-tbq-production-of-cyclotron-based-sodium-99m-tc-pertechnetate
#14
J D Andersson, B Thomas, S V Selivanova, E Berthelette, J S Wilson, A J B McEwan, K Gagnon
This paper presents the irradiation and processing of high-current 100 Mo targets at the University of Alberta (UofA) in a GMP compliant setting. For purpose of comparison with a second production facility, additional studies at Centre Hospitalier Universitaire de Sherbrooke (CHUS) are also described. INTRODUCTION: More than 70% of today's diagnostic radiopharmaceuticals are based on 99m Tc, however the conventional supply chain for obtaining 99m Tc is fragile. The aim of this work was to demonstrate reliable high yield production and processing of 99m Tc with medium-energy, high-current, cyclotrons...
May 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29571067/evaluation-of-177-lu-lu-chx-a%C3%A2-dtpa-6a10-fab-as-a-radioimmunotherapy-agent-targeting-carbonic-anhydrase-xii
#15
L Fiedler, M Kellner, A Gosewisch, R Oos, G Böning, S Lindner, N Albert, P Bartenstein, H-J Reulen, R Zeidler, F J Gildehaus
INTRODUCTION: Due to their infiltrative growth behavior, gliomas have, even after surgical resection, a high recurrence tendency. The approach of intracavitary radioimmunotherapy (RIT) is aimed at inhibiting tumor re-growth by directly administering drugs into the resection cavity (RC). Direct application of the radioconjugate into the RC has the advantage of bypassing the blood-brain barrier, which allows the administration of higher radiation doses than systemic application. Carbonic anhydrase XII (CA XII) is highly expressed on glioma cells while being absent from normal brain and thus an attractive target molecule for RIT...
May 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29571066/in-vitro-and-in-vivo-evaluation-of-the-bifunctional-chelator-nodia-me-in-combination-with-a-prostate-specific-membrane-antigen-targeting-vector
#16
Tilman Läppchen, Yvonne Kiefer, Jason P Holland, Mark D Bartholomä
INTRODUCTION: We recently developed a chelating platform based on the macrocycle 1,4,7-triazacyclononane with up to three five-membered azaheterocyclic arms for complexation of the PET nuclides gallium-68 and copper-64. The main objective of this study was to evaluate the stability and pharmacokinetics of 68 Ga- and 64 Cu-complexes of the bifunctional chelator NODIA-Me 1 covalently bound to a PSMA targeting vector in vivo. METHODS: NODIA-Me 1 was conjugated to the PSMA targeting Glu-NH-CO-NH-Lys moiety to give the bioconjugate NODIA-Me-NaI-Ahx-PSMA 4...
May 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29544122/-18-f-rps-544-a-pet-tracer-for-imaging-the-chemokine-receptor-cxcr4
#17
Alejandro Amor-Coarasa, James Kelly, Shashikanth Ponnala, Yogindra Vedvyas, Anastasia Nikolopoulou, Clarence Williams, Moonsoo M Jin, J David Warren, John W Babich
INTRODUCTION: CXCR4 specific [18 F]-labeled positron emission tomography (PET) imaging agents are needed which would enable general distribution of the radiotracer for clinical investigation. We sought to synthesize, radiolabel and evaluate [18 F]RPS-544, a novel non-peptide CXCR4 antagonist as a CXCR4 specific probe. We compared [18 F]RPS-544 with the previously published [18 F]-3 ([18 F]RPS-510 in this paper) in a bi-lateral tumor model of differential CXCR4 expression for its ability to selectively target CXCR4 expression...
May 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29529532/a-new-method-measuring-the-interaction-of-radiotracers-with-the-human-p-glycoprotein-p-gp-transporter
#18
Chrysoula Vraka, Monika Dumanic, Teresa Racz, Florian Pichler, Cecile Philippe, Theresa Balber, Eva-Maria Klebermass, Karl-Heinz Wagner, Marcus Hacker, Wolfgang Wadsak, Markus Mitterhauser
In drug development, biomarkers for cerebral applications have a lower success rate compared to cardiovascular drugs or tumor therapeutics. One reason is the missing blood brain barrier penetration, caused by the tracer's interaction with efflux transporters such as the P-gp (MDR1 or ABCB1). Aim of this study was the development of a reliable model to measure the interaction of radiotracers with the human efflux transporter P-gp in parallel to the radiolabeling process. LigandTracer® Technology was used with the wildtype cell line MDCKII and the equivalent cell line overexpressing human P-gp (MDCKII-hMDR1)...
May 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29525446/alanine-and-glycine-conjugates-of-2s-4r-4-18-f-fluoroglutamine-for-tumor-imaging
#19
Zhihao Zha, Karl Ploessl, Brian P Lieberman, Limin Wang, Hank F Kung
INTRODUCTION: Glutamine is an essential source of energy, metabolic substrates, and building block for supporting tumor proliferation. Previously, (2S,4R)-4-[18 F]fluoroglutamine (4F-Gln) was reported as a glutamine-related metabolic imaging agent. To improve the in vivo kinetics of this radiotracer, two new dipeptides, [18 F]Gly-(2S,4R)4-fluoroglutamine (Gly-4F-Gln) and [18 F]Ala-(2S,4R)4-fluoroglutamine (Ala-4F-Gln) were investigated. METHODS: Radiolabeling was performed via 2-steps 18 F-fluorination...
May 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29502008/time-dependent-transcriptional-response-of-got1-human-small-intestine-neuroendocrine-tumor-after-177-lu-lu-octreotate-therapy
#20
Johan Spetz, Nils Rudqvist, Britta Langen, Toshima Z Parris, Johanna Dalmo, Emil Schüler, Bo Wängberg, Ola Nilsson, Khalil Helou, Eva Forssell-Aronsson
INTRODUCTION: Patients with neuroendocrine tumors expressing somatostatin receptors are often treated with 177 Lu[Lu]-octreotate. Despite being highly effective in animal models, 177 Lu[Lu]-octreotate-based therapies in the clinical setting can be optimized further. The aims of the study were to identify and elucidate possible optimization venues for 177 Lu[Lu]-octreotate tumor therapy by characterizing transcriptional responses in the GOT1 small intestine neuroendocrine tumor model in nude mice...
May 2018: Nuclear Medicine and Biology
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