Mengzhe Wang, Hui Wang, Crystal Q Niu, Tao Zhang, Zhanhong Wu, Zibo Li
Targeted imaging via peptides has been extensively investigated for both diagnostic and therapeutic applications. However, peptides can be cleared out from the blood circulation quickly, leading to only moderate to low accumulation in regions of interest. Previously, 18F-sTCO-DiPhTz-RGDyK demonstrated relatively high blood retention with increased tumor uptake at the late time point (5.3 ± 0.4 and 8.9 ± 0.5 %ID/g tumor uptake at 1h p.i. and 4h p.i., respectively). In this study, we aim to develop a novel platform based on TCO/tetrazine ligation that could not only be used to label the peptides with F-18 for PET but also to lead to increased or persistent tumor uptake potentially due to enhanced blood circulation of the labeled peptides...
June 3, 2020: Bioconjugate Chemistry
Zijun Chen, Hao Fu, Hua Wu, Jinxiong Huang, Lanlin Yao, Xianzhong Zhang, Yesen Li
PURPOSE: Tumor Necrosis Factor Receptor 1 (TNFR1) and integrin αvβ3 receptor are overexpressed in breast cancer. We hypothesized that a peptide ligand recognizing both receptors in a single receptor-binding probe would be advantageous. Here, we developed a novel 18F-labeled fusion peptide probe [18F]-NOTA-Gly3-E(2PEG4-RGD-WH701) targeting dual receptors (TNFR1 and αvβ3) and evaluated the diagnostic efficacy of this radioactive probe in both MDA-MB-231 and MCF-7 xenograft models in mice...
April 23, 2020: Anti-cancer Agents in Medicinal Chemistry
Silvi Telo, Letizia Calderoni, Sara Vichi, Federico Zagni, Paolo Castellucci, Stefano Fanti
BACKGROUND: FDG PET/CT imaging has an established role in lung cancer (LC) management. Whilst is a sensitive technique, FDG PET/CT has a limited specificity in the differentiation between LC and benign conditions and is not capable of defining LC heterogeneity since FDG uptake varies between hystotypes. OBJECTIVE: To get an overview about new radiopharmaceuticals for the study of cancer biology features beyond glucose metabolism in LC. METHODS: A comprehensive literature review of PubMed/Medline was performed using a combination of the following keywords: "positron emission tomography", "lung neoplasms", "non-FDG", "radiopharmaceuticals", "tracers"...
December 23, 2019: Current Radiopharmaceuticals
Najme Karamzade-Ziarati, Reyhaneh Manafi-Farid, Bahar Ataeinia, Werner Langsteger, Christian Pirich, Felix M Mottaghy, Mohsen Beheshti
Bone metastasis is a disastrous manifestation of most malignancies, especially in breast, prostate and lung cancers. Since asymptomatic bone metastases are not uncommon, early detection, precise assessment, and localization of them are very important. Various imaging modalities have been employed in the setting of diagnosis of bone metastasis, from plain radiography and bone scintigraphy to SPECT, SPECT/CT, PET/CT, MRI. However, each modality showed its own limitation providing accurate diagnostic performance...
June 2019: Quarterly Journal of Nuclear Medicine and Molecular Imaging
Anne-Margaux Collignon, Julie Lesieur, Nadège Anizan, Rana Ben Azzouna, Anne Poliard, Caroline Gorin, Didier Letourneur, Catherine Chaussain, Francois Rouzet, Gael Y Rochefort
Therapies using stem cells may be applicable to all fields of regenerative medicine, including craniomaxillofacial surgery. Dental pulp stem cells (DPSCs) have demonstrated in vitro and in vivo osteogenic and proangiogenic properties. The aim of the study was to evaluate whether early angiogenesis investigated by nuclear imaging can predict bone formation within a mouse critical bone defect. Two symmetrical calvarial critical-sized defects were created. Defects were left empty or filled with i) DPSC-containing dense collagen scaffold, ii) 5% hypoxia-primed DPSC-containing dense collagen scaffold, iii) acellular dense collagen scaffold, or iv) left empty...
October 10, 2018: Acta Biomaterialia
Deling Li, Jingjing Zhang, Nan Ji, Xiaobin Zhao, Kun Zheng, Zhen Qiao, Fang Li, Lixin Lang, Andrei Iagaru, Gang Niu, Zhaohui Zhu, Xiaoyuan Chen
OBJECTIVES: Uncommon pathological subtypes of meningioma may present with severe peritumoral brain edema and mimic high-grade glioma (HGG). In a prospective cohort study of Ga-NOTA-PRGD2 PET/CT to evaluate glioma, we occasionally observed that a combination of Ga-NOTA-PRGD2 and F-FDG was able to differentiate these 2 lesion types. METHODS: From 2013 to 2016, 21 patients suspected of HGG by MRI were recruited for evaluation using Ga-NOTA-PRGD2 PET/CT. Brain F-FDG PET/CT was performed within 3 days for comparison, and the tumor was surgically removed...
September 2018: Clinical Nuclear Medicine
Chunhui Jin, Bao-Nan Zhang, Zhipeng Wei, Bo Ma, Qi Pan, Pingping Hu
Activation of the vitronectin receptor αvβ3 and the phosphorylation of extracellular signal‑regulated kinase (ERK)1/2 are critical events during tumor development and progression. The aim of the present study was to investigate the effects of WD‑3, a formula used in traditional Chinese medicine, on integrin αvβ3 and ERK1/2 expression in vivo using a nude mouse‑human gastric cancer xenograft model combined with non‑invasive, real‑time 18F‑Arg‑Gly‑Asp (RGD) positron emission tomography (PET)/computerized tomography (CT) imaging methods...
December 2017: Molecular Medicine Reports
Monica Piras, Andrea Testa, Ian N Fleming, Sergio Dall'Angelo, Alexandra Andriu, Sergio Menta, Mattia Mori, Gavin D Brown, Duncan Forster, Kaye J Williams, Matteo Zanda
Nonpeptidic Arg-Gly-Asp (RGD)-mimic ligands were designed and synthesized by click chemistry between an arginine-azide mimic and an aspartic acid-alkyne mimic. Some of these molecules combine excellent in vitro properties (high αv β3 affinity, selectivity, drug-like logD, high metabolic stability) with a variety of radiolabeling options (e.g., tritium and fluorine-18, plus compatibility with radio-iodination), not requiring the use of chelators or prosthetic groups. The binding mode of the resulting triazole RGD mimics to αv β3 or αIIb β3 receptors was investigated by molecular modeling simulations...
July 20, 2017: ChemMedChem
Mohammad B Haskali, Delphine Denoyer, Wayne Noonan, Carleen Culinane, Christine Rangger, Normand Pouliot, Roland Haubner, Peter D Roselt, Rodney J Hicks, Craig A Hutton
Control of the biodistribution of radiolabeled peptides has proven to be a major challenge in their application as imaging agents for positron emission tomography (PET). Modification of peptide hydrophilicity in order to increase renal clearance has been a common endeavor to improve overall biodistribution. Herein, we examine the effect of site-specific sulfonation of tyrosine moieties in cyclic(RGDyK) peptides as a means to enhance their hydrophilicity and improve their biodistribution. The novel sulfonated cyclic(RGDyK) peptides were conjugated directly to 4-nitrophenyl 2-[18 F]fluoropropionate, and the biodistribution of the radiolabeled peptides was compared with that of their nonsulfonated, clinically relevant counterparts, [18 F]GalactoRGD and [18 F]FPPRGD2...
April 3, 2017: Molecular Pharmaceutics
Ambros J Beer, Sarah M Schwarzenböck, Niko Zantl, Michael Souvatzoglou, Tobias Maurer, Petra Watzlowik, Horst Kessler, Hans-Jürgen Wester, Markus Schwaiger, Bernd Joachim Krause
PURPOSE: Due to the high expression of the integrin αvβ3 not only on endothelial cells, but also on mature osteoclasts and prostate cancer cells, imaging of osseous metastases with αvβ3-targeted tracers seems promising. However, little is known about the patterns of αvβ3-expression in metastasized prostate cancer lesions in-vivo. Thus we evaluated the uptake of the αvβ3-specific PET tracer [18F]Galacto-RGD for assessment of bone metastases in prostate cancer patients. RESULTS: [18F]Galacto-RGD PET identified 58/74 bone-lesions (detection rate of 78...
May 10, 2016: Oncotarget
Yanfen Cui, Huanhuan Liu, Sheng Liang, Caiyuan Zhang, Weiwei Cheng, Wangxi Hai, Bing Yin, Dengbin Wang
PURPOSE: Radiolabeled arginine-glycine-aspartic acid (RGD) peptides have been developed for PET imaging of integrin avβ3 in the tumor vasculature, leading to great potential for noninvasively evaluating tumor angiogenesis and monitoring antiangiogenic treatment. The aim of this study was to investigate a novel one-step labeled integrin-targeted tracer, 18F-AlF-NOTA-PRGD2, for PET/CT for detecting tumor angiogenesis and monitoring the early therapeutic efficacy of antiangiogenic agent Endostar in human nasopharyngeal carcinoma (NPC) xenograft model...
May 10, 2016: Oncotarget
Rohini Sharma, Kumar G Kallur, Jin S Ryu, Ramanathapuram V Parameswaran, Henrik Lindman, Norbert Avril, Fergus V Gleeson, Jong D Lee, Kyung-Han Lee, Michael J O'Doherty, Ashley M Groves, Matthew P Miller, Edward J Somer, Charles R Coombes, Eric O Aboagye
UNLABELLED: Integrins are upregulated on both tumor cells and associated vasculature, where they play an important role in angiogenesis and metastasis. Fluciclatide is an arginine-glycine-aspartic acid peptide with high affinity for αvβ3/αvβ5 integrin, which can be radiolabeled for PET imaging of angiogenesis. Thus, (18)F-fluciclatide is a potential biomarker of therapeutic response to antiangiogenic inhibitors. The aim of this study was to evaluate the reproducibility of (18)F-fluciclatide in multiple solid-tumor types...
December 2015: Journal of Nuclear Medicine
Rubel Chakravarty, Sudipta Chakraborty, Ashutosh Dash
Breast cancer is the leading cause of cancer deaths among women of all ages worldwide. With advances in molecular imaging procedures, it has been possible to detect breast cancer in its early stage, determine the extent of the disease to administer appropriate therapeutic protocol and also monitor the effects of treatment. By accurately characterizing the tumor properties and biological processes involved, molecular imaging can play a crucial role in minimizing the morbidity and mortality associated with breast cancer...
2015: Mini Reviews in Medicinal Chemistry
Shuang Liu
Angiogenesis is a requirement for tumor growth and metastasis. The angiogenic process depends on vascular endothelial cell migration and invasion, and is regulated by various cell adhesion receptors. Integrins are such a family of receptors that facilitate the cellular adhesion to and migration on extracellular matrix proteins in the intercellular spaces and basement membranes. Among 24 members of the integrin family, αvβ3 is studied most extensively for its role in tumor angiogenesis and metastasis. The αvβ3 is expressed at relatively low levels on epithelial cells and mature endothelial cells, but it is highly expressed on the activated endothelial cells of tumor neovasculature and some tumor cells...
August 19, 2015: Bioconjugate Chemistry
Orit Jacobson, Xuefeng Yan, Ying Ma, Gang Niu, Dale O Kiesewetter, Xiaoyuan Chen
Hexafluorobenzene (HFB) reacts with free thiols to produce a unique and selective perfluoroaromatic linkage between two sulfurs. We modified this chemical reaction to produce dimeric (18)F-RGD-tetrafluorobenzene (TFB)-RGD, an integrin αvβ3 receptor ligand. (18)F-HFB was prepared by a fluorine exchange reaction using K(18)F/K2.2.2 at room temperature. The automated radiofluorination was optimized to minimize the amount of HFB precursor and, thus, maximize the specific activity. (18)F-HFB was isolated by distillation and subsequently reacted with thiolated c(RGDfk) peptide under basic and reducing conditions...
October 21, 2015: Bioconjugate Chemistry
Zhuzhong Cheng, Renbo Wei, Changqiang Wu, Haomiao Qing, Xiao Jiang, Hao Lu, Shirong Chen, Xinping Li, Guohui Xu, Hua Ai
OBJECTIVE: (18)F-Fluorodeoxyglucose ((18)F-FDG), (18)F-fluoro-3'-deoxy-3'-L-fluorothymidine ((18)F-FLT), (18)F-fluoromisonidazole ((18)F-FMISO), and (18)F-AlF-NOTA-PRGD2 ((18)F-RGD) are all commonly used PET tracers for tumor diagnosis based on different mechanisms of tissue uptake. This study compared the ex-vivo biodistribution and PET/computed tomography (CT) imaging studies of these four PET tracers in a xenograft prostate tumor-bearing mouse model. MATERIALS AND METHODS: Nude mice were inoculated with 5 × 10 PC-3 cells in the right armpit...
September 2015: Nuclear Medicine Communications
Reza Golestani, Leila Mirfeizi, Clark J Zeebregts, Johanna Westra, Hans J de Haas, Andor W J M Glaudemans, Michel Koole, Gert Luurtsema, René A Tio, Rudi A J O Dierckx, Hendrikus H Boersma, Philip H Elsinga, Riemer H J A Slart
BACKGROUND: Inflammation and angiogenesis play an important role in atherosclerotic plaque rupture. Therefore, molecular imaging of these processes could be used for determination of rupture-prone atherosclerotic plaques. αvβ3 integrin is involved in the process of angiogenesis. Targeted imaging of αvβ3 integrin has been shown to be possible in previous studies on tumor models, using radiolabeled arginine-glycine-aspartate (RGD). Our aim was to investigate feasibility of ex vivo detection of αvβ3 integrin in carotid endarterectomy (CEA) specimens...
December 2015: Journal of Nuclear Cardiology
Ramajeyam Selvaraj, Benjamin Giglio, Shuanglong Liu, Hui Wang, Mengzhe Wang, Hong Yuan, Srinivasa R Chintala, Li-Peng Yap, Peter S Conti, Joseph M Fox, Zibo Li
The fast kinetics and bioorthogonal nature of the tetrazine trans-cyclooctene (TCO) ligation makes it a unique tool for PET probe construction. In this study, we report the development of an (18)F-labeling system based on a CF3-substituted diphenyl-s-tetrazine derivative with the aim of maintaining high reactivity while increasing in vivo stability. c(RGDyK) was tagged by a CF3-substituted diphenyl-s-tetrazine derivative via EDC-mediated coupling. The resulting tetrazine-RGD conjugate was combined with a (19)F-labeled TCO derivative to give HPLC standards...
March 18, 2015: Bioconjugate Chemistry
Edwin Chang, Hongguang Liu, Kerstin Unterschemmann, Peter Ellinghaus, Shuanglong Liu, Volker Gekeler, Zhen Cheng, Dietmar Berndorff, Sanjiv S Gambhir
PURPOSE: We describe a noninvasive PET imaging method that monitors early therapeutic efficacy of BAY 87-2243, a novel small-molecule inhibitor of mitochondrial complex I as a function of hypoxia-inducible factor-1α (HIF1α) activity. EXPERIMENTAL DESIGN: Four PET tracers [(18)F-FDG, (18)F-Fpp(RGD)2, (18)F-FLT, and (18)F-FAZA] were assessed for uptake into tumor xenografts of drug-responsive (H460, PC3) or drug-resistant (786-0) carcinoma cells. Mice were treated with BAY 87-2243 or vehicle...
January 15, 2015: Clinical Cancer Research
Andrea Vilchis-Juárez, Guillermina Ferro-Flores, Clara Santos-Cuevas, Enrique Morales-Avila, Blanca Ocampo-García, Lorenza Díaz-Nieto, Myrna Luna-Gutiérrez, Nallely Jiménez-Mancilla, Martha Pedraza-López, Leobardo Gómez-Oliván
Peptides based on the cyclic Arg-Gly-Asp (RGD) sequence have been designed to antagonize the function of alpha(v)beta(3) integrin, thereby inhibiting angiogenesis. The conjugation of RGD peptides to radiolabeled gold nanoparticles (AuNP) produces biocompatible and stable multimeric systems with target-specific molecular recognition. The aim of this research was to evaluate the therapeutic response of 177Lu-AuNP-RGD in athymic mice bearing alpha(v)beta(3)-integrin-positive C6 gliomas and compare it with that of 177Lu-AuNP or 177Lu-RGD...
March 2014: Journal of Biomedical Nanotechnology
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