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Gallium RGD

Claire Provost, Aurélie Prignon, Laura Rozenblum-Beddok, Quentin Bruyer, Sylvie Dumont, Fatiha Merabtene, Valérie Nataf, Cédric Bouteiller, Jean-Noël Talbot
The aim of this study was to evaluate two RGD radiotracers radiolabelled with fluorine-18 or gallium-68, in detecting angiogenesis in grafted human tumours and monitoring their treatment with the anti-angiogenic agent bevacizumab. Sixteen mice bearing an U87MG tumour in one flank and a contralateral A549 tumour were treated with intravenous injections of bevacizumab twice a week for 3 weeks. PET images with 18 F-RGD-K5 and 68 Ga-RGD were acquired before treatment (baseline), after three bevacizumab injections (t1) and after seven bevacizumab injections (t2)...
April 10, 2018: Oncotarget
Akintunde Orunmuyi, Moshe Modiselle, Thabo Lengana, Thomas Ebenhan, Mariza Vorster, Mike Sathekge
We report the case of a 32 year-old male with Chondroblastic Osteosarcoma of the skull, which was imaged with both (18)[F]fluorodeoxyglucose ((18)F-FDG) positron emission tomography/computed tomography (PET/CT) and (68)Gallium-arginine-glycine-aspartic acid ((68)Ga-RGD) PET/CT. The (18)F-FDG PET/CT did not demonstrate the tumour, whereas the (68)Ga-RGD PET/CT clearly depicted a left-sided frontal tumour. (68)Ga-RGD PET/CT may be a clinically useful imaging modality for early detection of recurrent osteosarcoma, considering the limitations of (18)F-FDG PET in a setting of low glycolytic activity...
September 2017: Nuclear Medicine and Molecular Imaging
Dominik Summer, Leo Grossrubatscher, Milos Petrik, Tereza Michalcikova, Zbynek Novy, Christine Rangger, Maximilian Klingler, Hubertus Haas, Piriya Kaeopookum, Elisabeth von Guggenberg, Roland Haubner, Clemens Decristoforo
Positron emission tomography (PET) as well as optical imaging (OI) with peptide receptor targeting probes have proven their value for oncological applications but also show restrictions depending on the clinical field of interest. Therefore, the combination of both methods, particularly in a single molecule, could improve versatility in clinical routine. This proof of principle study aims to show that a chelator, Fusarinine C (FSC), can be utilized as scaffold for novel dimeric dual-modality imaging agents...
June 21, 2017: Bioconjugate Chemistry
Johannes Notni, Dominik Reich, Oleg V Maltsev, Tobias G Kapp, Katja Steiger, Frauke Hoffmann, Irene Esposito, Wilko Weichert, Horst Kessler, Hans-Jürgen Wester
Expression of the cellular transmembrane receptor αvβ6 integrin is essentially restricted to malignant epithelial cells in carcinomas of a broad variety of lineages, whereas it is virtually absent in normal adult tissues. Thus, it is a highly attractive target for tumor imaging and therapy. Furthermore, αvβ6 integrin plays an important role for the epithelial-mesenchymal interaction and the development of fibrosis. Methods: On the basis of the68 Ga chelators TRAP (triazacyclononane-triphosphinate) and NODAGA, we synthesized mono-, di-, and trimeric conjugates of the αvβ6 integrin-selective peptide cyclo(FRGDLAFp( N Me)K) via click chemistry...
April 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
Cinzia Imberti, Samantha Y A Terry, Carleen Cullinane, Fiona Clarke, Georgina H Cornish, Nisha K Ramakrishnan, Peter Roselt, Andrew P Cope, Rodney J Hicks, Philip J Blower, Michelle T Ma
Tris(hydroxypyridinone) chelators conjugated to peptides can rapidly complex the positron-emitting isotope gallium-68 (68 Ga) under mild conditions, and the resulting radiotracers can delineate peptide receptor expression at sites of diseased tissue in vivo. We have synthesized a dendritic bifunctional chelator containing nine 1,6-dimethyl-3-hydroxypyridin-4-one groups (SCN-HP9 ) that can coordinate up to three Ga3+ ions. This derivative has been conjugated to a trimeric peptide (RGD3 ) containing three peptide groups that target the αv β3 integrin receptor...
February 15, 2017: Bioconjugate Chemistry
Thomas Ebenhan, Isabel Schoeman, Daniel D Rossouw, Anne Grobler, Biljana Marjanovic-Painter, Judith Wagener, Hendrik G Kruger, Mike M Sathekge, Jan Rijn Zeevaart
PURPOSE: Radiopharmaceuticals containing the motive tripeptide arginyl-glycyl-asparatic acid (RGD) are known to target ανβ3 integrins during tumor angiogenesis. A more generic kit radiolabeling procedure accommodating Ga-68 from different generators was developed for NOTA-RGD and evaluated for its versatile use and safety in subsequent in vivo applications. The [68 Ga]NOTA-RGD kit was further verified for its expected biodistribution and pharmacokinetics in nonhuman primates and its clinical sensitivity to detect solitary pulmonary nodules (SPN) in cancer patients...
June 2017: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
J R Buscombe
Positron emission tomography (PET) has become widely established in oncology. Subsequently, a whole new “toolbox” of tracers have become available to look at different aspects of cancer cell function and dysfunction, including cell protein production, DNA synthesis, hypoxia and angiogenesis. In the past 5 years, these tools have been used increasingly to look at the other great killer of the developed world: cardiovascular disease. For example, inflammation of the unstable plaque can be imaged with 18-fludeoxyglucose (18F-FDG), and this uptake can be quantified to show the effect that statins have in reducing inflammation and explains how these drugs can reduce the risk of stroke...
September 2015: British Journal of Radiology
Chuangyan Zhai, Dominik Summer, Christine Rangger, Hubertus Haas, Roland Haubner, Clemens Decristoforo
Fusarinine C (FSC), a siderophore-based chelator coupled with the model peptide c(RGDfK) (FSC(succ-RGD)3), revealed excellent targeting properties in vivo using positron emission tomography (PET). Here, we report the details of radiolabeling conditions and specific activity as well as selectivity for (68)Ga. (68)Ga labeling of FSC(succ-RGD)3 was optimized regarding peptide concentration, pH, temperature, reaction time, and buffer system. Specific activity (SA) of [(68)Ga]FSC(succ-RGD)3 was compared with (68)Ga-1,4,7-triazacyclononane, 1-glutaric acid-4,7 acetic acid RGD ([(68)Ga]NODAGA-RGD)...
May 15, 2015: Journal of Labelled Compounds & Radiopharmaceuticals
Peter A Knetsch, Chuangyan Zhai, Christine Rangger, Michael Blatzer, Hubertus Haas, Piriya Kaeopookum, Roland Haubner, Clemens Decristoforo
Over the last years Gallium-68 ((68)Ga) has received tremendous attention for labeling of radiopharmaceuticals for positron emission tomography (PET). (68)Ga labeling of biomolecules is currently based on bifunctional chelators containing aminocarboxylates (mainly DOTA and NOTA). We have recently shown that cyclic peptide siderophores have very good complexing properties for (68)Ga resulting in high specific activities and excellent metabolic stabilities, in particular triacetylfusarinine-C (TAFC). We postulated, that, starting from its deacetylated form (Fusarinine-C (FSC)) trimeric bioconjugates are directly accessible to develop novel targeting peptide based (68)Ga labeled radiopharmaceuticals...
February 2015: Nuclear Medicine and Biology
V Lopez-Rodriguez, R E Gaspar-Carcamo, M Pedraza-Lopez, E L Rojas-Calderon, C Arteaga de Murphy, G Ferro-Flores, M A Avila-Rodriguez
INTRODUCTION: Integrin αvβ3 plays an important role in angiogenesis and is over-expressed in tumoral endothelial cells and some other tumor cells. RGD (Arg-Gly-Asn) peptides labeled with (68)Ga (t1/2=68min) have showed good characteristics for imaging of αvβ3 expression using positron emission tomography (PET). Gallium-66 has been proposed as a PET imaging alternative to (68)Ga and given the unique high energy of its emitted positrons (Emax 4.15MeV) it may also be useful for therapy...
February 2015: Nuclear Medicine and Biology
Svetlana N Rylova, Enikö Barnucz, Melpomeni Fani, Friederike Braun, Martin Werner, Silke Lassmann, Helmut R Maecke, Wolfgang A Weber
UNLABELLED: In recent years, there has been a growing interest in molecular imaging markers of tumor-induced angiogenesis. Several radiolabeled RGD (arginine, glycine, aspartate) peptides have been developed for PET imaging of αvβ3 integrins in the tumor vasculature, but there are only limited data on how angiogenesis inhibitors affect the tumor uptake of these peptides. METHODS: Changes in (68)Ga-NODAGA-c(RGDfK) peptide uptake were measured using PET during bevacizumab therapy of 2 αvβ3-negative squamous cell carcinoma cell lines (A-431 and FaDu) that induce αvβ3-positive neovasculature when transplanted into nude mice...
November 2014: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
Jiyun Shi, Zhongxia Jin, Xujie Liu, Di Fan, Yi Sun, Huiyun Zhao, Zhaohui Zhu, Zhaofei Liu, Bing Jia, Fan Wang
Antiangiogenic therapy is an effective strategy to inhibit tumor growth. Endostar, as an approved antiangiogenesis agent, inhibits the newborn vascular endothelial cells, causing the decrease of integrin αvβ3 expression. Radiolabeled 3PRGD2, a novel PEGlayted RGD dimer probe (PEG4-E[PEG4-c(RGDfK)]2) showed highly specific targeting capability to integrin αvβ3, which could be used for monitoring the efficacy of Endostar antiangiogenic therapy. In this study, (68)Ga-3PRGD2 PET imaging was performed in Endostar treated/untreated Lewis Lung Carcinoma (LLC) mice on days 3, 7, 14, and 21 post-treatment for monitoring the tumor response to Endostar treatment, with the (18)F-FDG imaging as control...
November 3, 2014: Molecular Pharmaceutics
Ute Jungwirth, Johannes Gojo, Theresa Tuder, Gernot Walko, Martin Holcmann, Thomas Schöfl, Karin Nowikovsky, Nastasia Wilfinger, Sushilla Schoonhoven, Christian R Kowol, Rosa Lemmens-Gruber, Petra Heffeter, Bernhard K Keppler, Walter Berger
On the basis of enhanced tumor accumulation and bone affinity, gallium compounds are under development as anticancer and antimetastatic agents. In this study, we analyzed molecular targets of one of the lead anticancer gallium complexes [KP46, Tris(8-quinolinolato)gallium(III)] focusing on colon and lung cancer. Within a few hours, KP46 treatment at low micromolar concentrations induced cell body contraction and loss of adhesion followed by prompt cell decomposition. This rapid KP46-induced cell death lacked classic apoptotic features and was insensitive toward a pan-caspase inhibitor...
October 2014: Molecular Cancer Therapeutics
Yong-il Kim, Ji Hoon Phi, Jin Chul Paeng, Hongyoon Choi, Seung-Ki Kim, Yun-Sang Lee, Keon Wook Kang, Ji Yeoun Lee, Jae Min Jeong, June-Key Chung, Dong Soo Lee, Kyu-Chang Wang
UNLABELLED: Indirect revascularization is the most widely used treatment to induce angiogenesis in pediatric moyamoya disease (MMD). Molecular imaging methods targeted for angiogenesis have recently been developed. We performed angiogenesis imaging in indirect revascularization surgery for MMD to evaluate angiogenic activity and its correlation with treatment efficacy. METHODS: Twelve patients with pediatric MMD were prospectively enrolled. Encephaloduroarteriosynangiosis surgery was conducted, and (68)Ga-Arg-Gly-Asp (RGD) PET was performed 3...
September 2014: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
Jochen Tillmanns, Magdalena Schneider, Daniela Fraccarollo, Jan-Dieter Schmitto, Florian Länger, Dominik Richter, Johann Bauersachs, Samuel Samnick
PURPOSE: Peptides containing the asparagine-glycine-arginine (NGR) motif bind to aminopeptidase N (CD13), which is expressed on inflammatory cells, endothelial cells, and fibroblasts. It is unclear whether radiolabeled NGR-containing tracers could be used for in vivo imaging of the early wound-healing phase after myocardial infarction (MI) using positron emission tomography (PET). PROCEDURES: Uptake of novel tracer [(68)Ga]NGR was assessed together with [(68)Ga]arginine-glycine-aspartic acid ([(68)Ga]RGD) and 2-deoxy-2-[(18) F]fluoro-D-glucose after myocardial ischemia/reperfusion (MI/R) injury using μ-PET and autoradiography, and relative expressions of CD13 and integrin β3 were assessed in fibroblasts, inflammatory cells, and endothelial cells by immunohistochemistry...
February 2015: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
Yahui Shao, Wansheng Liang, Fei Kang, Weidong Yang, Xiaowei Ma, Guiyu Li, Shu Zong, Kai Chen, Jing Wang
Peptides containing asparagine-glycine-arginine (NGR) and arginine-glycine-aspartic acid (RGD) sequence are being developed for tumor angiogenesis-targeted imaging and therapy. The aim of this study was to compare the efficacy of NGR- and RGD-based probes for imaging tumor angiogenesis in HT-1080 tumor xenografts. Two PET probes, (68)Ga-NOTA-G₃-NGR2 and ⁶⁸Ga-NOTA-G₃-RGD2, were successfully prepared. In vitro stability, partition coefficient, tumor cell binding, as well as in vivo biodistribution properties were also analyzed for both PET probes...
October 2014: Amino Acids
Max Kiugel, Ingrid Dijkgraaf, Ville Kytö, Semi Helin, Heidi Liljenbäck, Tiina Saanijoki, Cheng-Bin Yim, Vesa Oikonen, Pekka Saukko, Juhani Knuuti, Anne Roivainen, Antti Saraste
PURPOSE: We evaluated a dimeric RGD-peptide, [(68)Ga]DOTA-E-[c(RGDfK)]2, for positron emission tomography (PET) imaging of myocardial integrin expression associated with extracellular matrix remodeling after myocardial infarction (MI) in rat. PROCEDURES: Male Sprague-Dawley rats were studied at 7 days and 4 weeks after MI induced by permanent ligation of the left coronary artery and compared with sham-operated controls. RESULTS: In vivo imaging revealed higher tracer uptake in the infarcted area than in the remote non-infarcted myocardium of the same rats both at 7 days (MI/remote ratio, 2...
December 2014: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
Ina Israel, Dominik Richter, Jochen Stritzker, Michaela van Ooschot, Ulrike Donat, Andreas K Buck, Samuel Samnick
The α(v)β₃ integrin is highly expressed in prostate cancer (PCa), in which it is a key player in tumour invasion, angiogenesis and metastasis formation. Therefore, α(v)β₃ integrin is considered a very promising target for molecular imaging of PCa. This study tested the potential of the novel α(v)β₃ integrin affine agent [⁶⁸Ga]NOTA-RGD in comparison with the established [¹⁸F]fluoroethylcholine (FEC) and [¹⁸F]fluorodeoxyglucose (FDG) for assessing PCa using positron emission tomography (PET)...
2014: Current Cancer Drug Targets
Johannes Notni, Jakub Šimeček, Hans-Jürgen Wester
Given the wide application of positron emission tomography (PET), positron-emitting metal radionuclides have received much attention recently. Of these, gallium-68 has become particularly popular, as it is the only PET nuclide commercially available from radionuclide generators, therefore allowing local production of PET radiotracers independent of an on-site cyclotron. Hence, interest in optimized bifunctional chelators for the elaboration of (68) Ga-labeled bioconjugates has been rekindled as well, resulting in the development of improved triazacyclononane-triphosphinate (TRAP) ligand structures...
June 2014: ChemMedChem
Jytte Oxboel, Malene Brandt-Larsen, Christina Schjoeth-Eskesen, Rebecca Myschetzky, Henrik H El-Ali, Jacob Madsen, Andreas Kjaer
INTRODUCTION: The aim of this study was to synthesize and perform a side-by-side comparison of two new tumor-angiogenesis PET tracers (68)Ga-NODAGA-E[c(RGDyK)](2) and (64)Cu-NODAGA-E[c(RGDyK)](2) in vivo using human xenograft tumors in mice. Human radiation burden was estimated to evaluate potential for future use as clinical PET tracers for imaging of neo-angiogenesis. METHODS: A (68)Ge/(68)Ga generator was used for the synthesis of (68)Ga-NODAGA-E[c(RGDyK)](2)...
March 2014: Nuclear Medicine and Biology
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