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https://www.readbyqxmd.com/read/28816108/editorial-radiopharmaceuticals-for-cancer-therapy-and-diagnosis
#1
EDITORIAL
Ralph Santos-Oliveira
No abstract text is available yet for this article.
2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28815804/octadentate-picolinic-acid-based-bispidine-ligand-for-radiometal-ions
#2
Peter Comba, Una Jermilova, Chris Orvig, Brian O Patrick, Caterina F Ramogida, Katharina Rück, Christina Schneider, Miriam Starke
The synthesis of the octadentate bispidine ligand H2bispa2 bearing two picolinic acid pendant arms and its coordination chemistry with metal ions with radionuclides relevant for nuclear medicine, i.e. indium(III) (111In), lutetium(III) (177Lu) and lanthanum(III) (as surrogate for 225Ac), are reported. The non-radioactive metal complexes of the N6O2-type bispa ligand were characterized by 1H and 13C nuclear magnetic resonance spectroscopy, elemental analysis, mass spectrometry and single crystal X-ray analysis...
August 16, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28814251/the-role-of-radiopharmaceuticals-in-amiodarone-induced-thyroid-pathology
#3
Doina Piciu, Alexandru Irimie
Amiodarone is a di-iodinated benzofuran derivative and is classified as a class III antiarrhythmic agent. It is one of the most powerful and effective antiarrhythmics, being a first-line agent due to its ability to treat ventricular and supraventricular dysrhythmias; since 1960 the drug has become one of the most frequently prescribed antiarrhythmics, despite its potentially serious, side effects. By far, one of the most challenging condition is the thyroid pathology induced by this drug. Each 200 mg tablet of amiodarone contains approximately 75 mg of iodine, 3-10% from each tablet being released as free iodine...
August 16, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28810154/synthesis-and-evaluation-of-a-99m-tc-labeled-chemokine-receptor-antagonist-peptide-for-imaging-of-chemokine-receptor-expressing-tumors
#4
Azadeh Mikaeili, Mostafa Erfani, Omid Sabzevari
OBJECTIVE: The chemokine receptor CXCR4 is highly expressed in tumor cells and plays an important role in tumor metastasis. In the present study, we report on the evaluation of a new radiopharmaceutical peptide for its potential to visualization for CXCR4-expressing tumors in vivo. METHODS: A CXCR4 antagonist analogue was synthesized using a standard Fmoc solid phase strategy and labeled with (99m)Tc via HYNIC and EDDA/tricine as coligands. In addition, stability in human serum, receptor binding internalization, in vivo tumor uptake, and tissue biodistribution were evaluated...
July 12, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28801560/imaging-active-infection-in-vivo-using-d-amino-acid-derived-pet-radiotracers
#5
Kiel D Neumann, Javier E Villanueva-Meyer, Christopher A Mutch, Robert R Flavell, Joseph E Blecha, Tiffany Kwak, Renuka Sriram, Henry F VanBrocklin, Oren S Rosenberg, Michael A Ohliger, David M Wilson
Occult bacterial infections represent a worldwide health problem. Differentiating active bacterial infection from sterile inflammation can be difficult using current imaging tools. Present clinically viable methodologies either detect morphologic changes (CT/ MR), recruitment of immune cells ((111)In-WBC SPECT), or enhanced glycolytic flux seen in inflammatory cells ((18)F-FDG PET). However, these strategies are often inadequate to detect bacterial infection and are not specific for living bacteria. Recent approaches have taken advantage of key metabolic differences between prokaryotic and eukaryotic organisms, allowing easier distinction between bacteria and their host...
August 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28800462/imaging-biodistribution-and-in-vitro-study-of-smart-99m-tc-pamam-g4-dendrimer-as-novel-nano-complex
#6
Asghar Narmani, Kamal Yavari, Javad Mohammadnejad
Overexpression of folic acid receptor in various human tumors cells makes it as good candidate for targeting delivery of chemotherapeutic and radiopharmaceutical agents. In this research, FA used for functionalization of PEG modified PAMAM G4 dendrimer as a smart delivery of 5-FU and (99m)Tc for the breast carcinoma in order to chemotherapeutic and imaging goals. One aim of this research was assess the FA-mediated cell viability assay of PEG-PAMAM G4-FA-5FU-(99m)Tc and in vitro uptake of PEG-PAMAM G4-FA-(99m)Tc as the novel nano-complex determined on C2Cl2 (normal cell) and MCF-7 (breast cancer cell) cell lines...
August 1, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28797482/-principles-modalities-and-indications-of-the-administration-of-radium-in-cancers-focus-on-metastatic-prostate-cancer-state-of-arts
#7
REVIEW
Pauline Bertolaso, Laura Leroy, Marine Gross-Goupil, Olivier Aupee, Alain Ravaud, Guilhem Roubaud, Anne-Laure Cazeau, Sylvestre Le Moulec
Prostate cancer is the first cancer in men and has a specific tropism to bones. This tropism provided the rationale to develop bone targeting radiopharmaceutical agents, such as strontium, samarium and more recently the Radium-223, an alpha-emitter. In a phase III trial, ALSYMPCA, Radium-223 not only improved pain relief, but also impacted on overall survival. Despite an approval by both FDA and EMA, prescription of this agent remains limited by the lack of refund, especially in France. Radium-223 is currently evaluated in several clinical trials (combination with chemotherapy, radiotherapy or hormone therapy) in order to optimize the therapeutic sequences in metastatic bone prostate cancer and argues for being incorporated into the current therapeutic arsenal...
August 7, 2017: Bulletin du Cancer
https://www.readbyqxmd.com/read/28781122/dosimetry-of-99m-tc-dtpa-dmsa-and-mag3-used-in-renal-function-studies-of-newborns-and-children
#8
Marcial Vásquez Arteaga, Víctor Murillo Caballero, Kelman Marín Rengifo
The dose to kidneys of newborns and 1-year old children was calculated using the MIRD methodology. In order to perform renal studies radiopharmaceutical like (99m)Tc-DTPA, (99m) Tc-MAG3 and (99m)Tc-DMSA are used. Here, besides the anatomic and structure information of kidneys another data are provided in benefit of patient, however during the radioisotope decay emitted radiations delivers, totally or partially, their energy. Therefore is important to estimate the internal radiation dose of the organs. The largest dose to kidneys comes from the self-dose and it is due to the charged particles emitted during (99m)Tc decay...
July 28, 2017: Applied Radiation and Isotopes
https://www.readbyqxmd.com/read/28775270/a-sustainable-nanocomposite-au-salen-cc-for-catalytic-degradation-of-eosin-y-and-chromotrope-2r-dyes
#9
Vishal J Mayani, Suranjana V Mayani, Sang Wook Kim
Up to now, a very few catalysts have been developed approaching the heterogeneous catalytic degradation of Eosin Y and Chromotrope 2R dyes (Acid Red 29). The present study provides a complete perspective of recyclable nanocomposite Au(Salen)@CC for catalytic degradation of hazardous water pollutant dyes viz., Eosin Y & Chromotrope 2R using mild reaction conditions. New gold Salen complex doped carbon nanocomposite Au(Salen)@CC was developed by easy methodology using nano carbon cage (CC) prepared from low-priced Pyrolysis fuel oil (PFO) residue based Pitch...
August 3, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28758574/personalized-and-precision-medicine-in-cancer-a-theragnostic-approach
#10
Partha S Choudhury, Manoj Gupta
Background & objectives: There are many challenges in the execution of targeted therapy in cancer due to tumor heterogeneity between individuals. In case of solid tumors this is one of the reasons as to why genomic analysis from single tumor biopsy specimens underestimate the mutational burdens in such heterogenous tumors thus contributing to treatment failure and drug resistance. Molecular characteristics redefine tumor classification for molecular targeted therapies ensuring the best patient specific therapies with better specificity and cost effective ratio...
July 27, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28750494/brain-pet-and-functional-mri-why-simultaneously-using-hybrid-pet-mr-systems
#11
Diego Cecchin, Alessandro Palombit, Marco Castellaro, Erica Silvestri, Franco Bui, Henryk Barthel, Osama Sabri, Maurizio Corbetta, Alessandra Bertoldo
INTRODUCTION: In the last 20 years growing attention has been devoted to multimodal imaging. The recent literature is rich of clinical and research studies that have been performed using different imaging modalities on both separate and integrated Positron Emission Tomography (PET) and Magnetic Resonance (MR) scanners. However, today, hybrid PET/MR systems measure signals related to brain structure, metabolism, neurochemistry, perfusion, and neuronal activity simultaneously, i.e. in the same physiological conditions...
July 27, 2017: Quarterly Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/28742337/gallium-complexation-stability-and-bioconjugation-of-1-4-7-triazacyclononane-derived-chelators-with-azaheterocyclic-arms
#12
Alexander Schmidtke, Tilman Läppchen, Christian Weinmann, Lorenz Bier-Schorr, Manfred Keller, Yvonne Kiefer, Jason P Holland, Mark D Bartholomä
We have recently introduced a 1,4,7-triazacyclononane (TACN) based chelating system with additional five-membered azaheterocyclic substituents for complexation of radioactive Cu(2+) ions. In this work, we investigated the complexation properties of these novel chelators with Ga(3+). In labeling experiments, we could show that the penta- and hexadentate imidazole derivatives NODIA-Me 4 and NOTI-Me 1 can be labeled with (68)Ga in specific activities up to ∼30 MBq nmol(-1), while the corresponding thiazole derivative NOTThia 2 did not label satisfactorily under identical conditions...
August 7, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28737945/preliminary-pet-study-of-18-f-fc119s-in-normal-and-alzheimer-s-disease-models
#13
Se Jong Oh, Min Hwan Kim, Sang Jin Han, Kyung Jun Kang, In Ok Ko, YoungSoo Kim, Ji-Ae Park, Jae Yong Choi, Kyo Chul Lee, Dae Yoon Chi, Yong Jin Lee, Kyeong Min Kim
To evaluate the efficacy of (18)F-FC119S as a positron emission tomography (PET) radiopharmaceutical for the imaging of Alzheimer's disease (AD), we studied the drug absorption characteristics and distribution of (18)F-FC119S in normal mice. In addition, we evaluated the specificity of (18)F-FC119S for β-amyloid (Aβ) in the AD group of an APP/PS1 mouse model and compared it with that in the wild-type (WT) group. The behavior of (18)F-FC119S in the normal mice was characteristic of rapid brain uptake and washout patterns...
August 2, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28737914/density-functional-theory-study-on-the-complexation-of-nota-as-a-bifunctional-chelator-with-radiometal-ions
#14
F Y Adeowo, B Honarparvar, A A Skelton
1,4,7-Triazacyclononane-1,4,7-triacetic acid (NOTA) is a key bifunctional chelator utilized for the complexation of metal ions in radiopharmaceutical applications; the ability of these chelators depends on the strength of their binding with ions. The focus of the present work is to evaluate the complexation of Cu(2+), Ga(3+), Sc(3+), and In(3+) radiometal ions with NOTA using density functional theory (B3LYP functional) and 6-311+G(2d,2p)/DGDZVP basis sets. The significant role of ion-water interactions in the chelation interaction energies in solution reflects the competition between ion-water and NOTA-ion interaction in the chelation process...
August 7, 2017: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/28736283/multicellular-dosimetric-chain-for-molecular-radiotherapy-exemplified-with-dose-simulations-on-3d-cell-spheroids
#15
Vappu Reijonen, Liisa K Kanninen, Eero Hippeläinen, Yan-Ru Lou, Eero Salli, Alexey Sofiev, Melina Malinen, Timo Paasonen, Marjo Yliperttula, Antti Kuronen, Sauli Savolainen
PURPOSE: Absorbed radiation dose-response relationships are not clear in molecular radiotherapy (MRT). Here, we propose a voxel-based dose calculation system for multicellular dosimetry in MRT. We applied confocal microscope images of a spherical cell aggregate i.e. a spheroid, to examine the computation of dose distribution within a tissue from the distribution of radiopharmaceuticals. METHODS: A confocal microscope Z-stack of a human hepatocellular carcinoma HepG2 spheroid was segmented using a support-vector machine algorithm and a watershed function...
July 20, 2017: Physica Medica: PM
https://www.readbyqxmd.com/read/28721305/fully-automated-gmp-production-of-68-ga-ga-do3a-vs-cys-40-exendin-4-for-clinical-use
#16
Irina Velikyan, Ulrika Rosenstrom, Olof Eriksson
[(68)Ga]Ga-DO3A-VS-Cys(40)-Exendin-4/PET-CT targeting glucagon like peptide-1 receptor (GLP-1R) has previously demonstrated its potential clinical value for the detection of insulinomas. The production and accessibility of this radiopharmaceutical is one of the critical factors in realization of clinical trials and routine clinical examinations. Previously, the radiopharmaceutical was prepared manually, however larger scale of clinical trials and healthcare requires automation of the production process in order to limit the operator radiation dose as well as improve tracer manufacturing robustness and on-line documentation for enhanced good manufacturing practice (GMP) compliance...
2017: American Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/28719177/classics-in-neuroimaging-imaging-the-dopaminergic-pathway-with-pet
#17
Meghna Kanthan, Paul Cumming, Jacob M Hooker, Neil Vasdev
The success of positron emission tomography (PET) for observing molecular processes underlying brain function and disease is underpinned by radiotracer chemistry. From the earliest applications of PET to measure dopamine synthesis capacity and the abundance of neuroreceptors and transporters, to the more recent topic of dynamic neurochemical imaging, interrogation of brain dopamine in conditions such as neurodegenerative diseases, schizophrenia, mood disorders, and addictions has been a driving force that challenges the ingenuity of radiopharmaceutical scientists...
July 18, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28714296/-68-ga-somatostatin-analogue-pet-ct-analysis-of-costs-and-benefits-in-a-public-hospital-setting
#18
Tatiana Segard, Laurence Mja Morandeau, Elizabeth A Geelhoed, Roslyn J Francis
INTRODUCTION: Between 2009 and 2012, (68) Ga-somatostatin analogue PET-CT progressively replaced (111) In-octreotide scintigraphy for imaging neuroendocrine tumours in WA public hospitals due to published literature demonstrating improved diagnostic accuracy and increased availability. Despite significantly improved sensitivity and specificity, (68) Ga-somatostatin analogue PET is currently unfunded in Australia. This study sought to undertake cost analysis of the two modalities in a public hospital setting and to compare them with regard to patient factors such as imaging time and radiation dose...
July 17, 2017: Journal of Medical Imaging and Radiation Oncology
https://www.readbyqxmd.com/read/28711759/dft-study-of-the-interaction-between-dota-chelator-and-competitive-alkali-metal-ions
#19
E Frimpong, A A Skelton, B Honarparvar
1, 4, 7, 10-tetraazacyclododecane-1, 4, 7, 10-tetracetic acid (DOTA) is an important chelator for radiolabeling of pharmaceuticals. The ability of alkali metals found in the body to complex with DOTA and compete with radio metal ions can alter the radiolabeling process. Non-covalent interactions between DOTA complexed with alkali metals Li(+), Na(+), K(+) and Rb(+), are investigated with density functional theory using B3LYP and ωB97XD functionals. Conformational possibilities of DOTA were explored with a varying number of carboxylic pendant arms of DOTA in close proximity to the ions...
June 29, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28711565/new-aspects-of-molecular-imaging-in-prostate-cancer
#20
Francesco Ceci, Paolo Castellucci, Juliano J Cerci, Stefano Fanti
Nowadays several new imaging modalities are available for investigating prostate cancer (PCa) such as magnet resonance imaging (MRI) in the form of whole body MRI and pelvic multiparametric MRI and positron emission tomography (PET) using choline as radiotracers. Nevertheless, these modalities proved sub-optimal accuracy for detecting PCa metastases, particularly in the recurrence setting. A new molecular probe targeting the prostate specific membrane antigen (PSMA) has been recently developed for PET imaging...
July 12, 2017: Methods: a Companion to Methods in Enzymology
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