scholarly journals Cyclic RGD Peptides Incorporating Cycloalkanes: Synthesis and Evaluation as PET Radiotracers for Tumor Imaging

2014 ◽  
Vol 5 (9) ◽  
pp. 979-982 ◽  
Author(s):  
Ji-Ae Park ◽  
Yong Jin Lee ◽  
Ji Woong Lee ◽  
Kyo Chul Lee ◽  
Gwang il An ◽  
...  
Keyword(s):  
Tumor Imaging ◽  
Rgd Peptides ◽  
Pet Radiotracers

scholarly journals Spectroscopically Well-Characterized RGD Optical Probe as a Prerequisite for Lifetime-Gated Tumor Imaging

2011 ◽  
Vol 10 (6) ◽  
pp. 7290.2011.00018 ◽  
Author(s):  
Julia Eva Mathejczyk ◽  
Jutta Pauli ◽  
Christian Dullin ◽  
Joanna Napp ◽  
Lutz-F. Tietze ◽  
...  
Keyword(s):  
Fluorescence Lifetime ◽  
Nude Mice ◽  
Near Infrared ◽  
Tumor Imaging ◽  
Specific Binding ◽  
Optical Probe ◽  
Detection Sensitivity ◽  
Rgd Peptides ◽  
Emissive Probes

Labeling of RGD peptides with near-infrared fluorophores yields optical probes for noninvasive imaging of tumors overexpressing αvβ3 integrins. An important prerequisite for optimum detection sensitivity in vivo is strongly absorbing and highly emissive probes with a known fluorescence lifetime. The RGD-Cy5.5 optical probe was derived by coupling Cy5.5 to a cyclic arginine–glycine–aspartic acid–d-phenylalanine–lysine (RGDfK) peptide via an aminohexanoic acid spacer. Spectroscopic properties of the probe were studied in different matrices in comparison to Cy5.5. For in vivo imaging, human glioblastoma cells were subcutaneously implanted into nude mice, and in vivo fluorescence intensity and lifetime were measured. The fluorescence quantum yield and lifetime of Cy5.5 were found to be barely affected on RGD conjugation but dramatically changed in the presence of proteins. By time domain fluorescence imaging, we demonstrated specific binding of RGD-Cy5.5 to glioblastoma xenografts in nude mice. Discrimination of unspecific fluorescence by lifetime-gated analysis further enhanced the detection sensitivity of RGD-Cy5.5-derived signals. We characterized RGD-Cy5.5 as a strongly emissive and stable probe adequate for selective targeting of αvβ3 integrins. The specificity and thus the overall detection sensitivity in vivo were optimized with lifetime gating, based on the previous determination of the probes fluorescence lifetime under application-relevant conditions.

68Ga-labeled dimeric and trimeric cyclic RGD peptides as potential PET radiotracers for imaging gliomas

2019 ◽  
Vol 148 ◽  
pp. 168-177 ◽  
Author(s):  
Zuo-Quan Zhao ◽  
Shundong Ji ◽  
Xiao-Yan Li ◽  
Wei Fang ◽  
Shuang Liu
Keyword(s):  
Rgd Peptides ◽  
Pet Radiotracers

scholarly journals Radiolabeled cyclic RGD peptides as radiotracers for tumor imaging

2016 ◽  
Vol 2 (1) ◽  
pp. 1-20 ◽  
Author(s):  
Jiyun Shi ◽  
Fan Wang ◽  
Shuang Liu
Keyword(s):  
Tumor Imaging ◽  
Rgd Peptides

scholarly journals Application of 99mTc-3PRGD2 Imaging for Early Prediction of Pathological Response to Neoadjuvant Chemotherapy in Breast Tumors and Axillary Lymph Nodes

2020 ◽  
Author(s):  
Zhenying Chen ◽  
Fangmeng Fu ◽  
Junyu Lin ◽  
Chao Huang ◽  
Shan Zheng ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Neoadjuvant Chemotherapy ◽  
Tumor Imaging ◽  
Breast Tumors ◽  
Axillary Lymph Nodes ◽  
Axillary Lymph ◽  
Her2 Positive ◽  
Rgd Peptides ◽  
Standardized Uptake Values ◽  
Significant Difference

Abstract Background and PurposeTechnetium 99m-dimeric cyclic RGD peptides with three polyethylene glycol spacers (99mTc-3PRGD2) had a good performance for diagnosing breast cancer. The prospective study was to assess the performance of 99mTc-3PRGD2 tumor imaging for predicting pathological complete response (pCR) outcomes to neoadjuvant chemotherapy (NAC) in breast cancer patients.Materials and MethodsForty-one patients were examined using both 99mTc-3PRGD2 and 18F-fluoro-deoxy-glucose (18F-FDG) imaging before NAC (baseline), and after the first and fifth NAC cycle. The tumor-to-background (T/B) ratios for 99mTc-3PRGD2 imaging and the maximum standardized uptake values (SUVmax) from the 18F-FDG imaging in breast tumors and axillary lymph node (ALN) metastases were separately calculated and analyzed—based on receiver operating characteristic (ROC) analysis. ResultsFinally, pCR was achieved in 13 of 41 patients after NAC. The area under curve (AUC) of T/B changes (ΔT/B) in breast tumors for predicting pCR after first and fifth cycle were 0.827 and 0.687, and 0.859 and 0.778 in ALN metastases, respectively. For SUVmax changes (ΔSUVmax), the ROC-AUC were 0.859 and 0.713, as well as 0.572 and 0.802, respectively. In breast tumors, the AUCs of ΔT/B1 and ΔSUVmax1 had no significant difference (P > 0.05). However, the AUC of ΔT/B1 was significantly higher than for ΔSUVmax1 in ALN metastases (Z = 2.10, P = 0.035). Additionally, the T/B1 trends for breast tumor and ALN in pCR group were higher than for non-pCR group in HER2-positive patients (P﹤0.05). ConclusionsCompared with 18F-FDG imaging, our study shows that use of 99mTc-3PRGD2 imaging offered a similar level of predictive performance for breast cancer pCR to NAC, and early T/B1 trends of ALN showed an higher performance for predicting pCR.Trial RegistrationClinicalTrials.gov ID: NCT02742168.

scholarly journals Preclinical Evaluation of Radiolabeled Peptides for PET Imaging of Glioblastoma Multiforme

Molecules ◽  
2019 ◽  
Vol 24 (13) ◽  
pp. 2496 ◽  
Author(s):  
Zbynek Novy ◽  
Jana Stepankova ◽  
Michaela Hola ◽  
Dominika Flasarova ◽  
Miroslav Popper ◽  
...  
Keyword(s):  
Glioblastoma Multiforme ◽  
Tumor Imaging ◽  
Ex Vivo ◽  
Tumor Model ◽  
Rgd Peptides ◽  
Radiolabeled Peptides ◽  
Biodistribution Studies ◽  
Target Organs

In this study, we have compared four 68Ga-labeled peptides (three Arg-Gly-Asp (RGD) peptides and substance-P) with two 18F-tracers clinically approved for tumor imaging. We have studied in vitro and in vivo characteristics of selected radiolabeled tracers in a glioblastoma multiforme tumor model. The in vitro part of the study was mainly focused on the evaluation of radiotracers stability under various conditions. We have also determined in vivo stability of studied 68Ga-radiotracers by analysis of murine urine collected at various time points after injection. The in vivo behavior of tested 68Ga-peptides was evaluated through ex vivo biodistribution studies and PET/CT imaging. The obtained data were compared with clinically used 18F-tracers. 68Ga-RGD peptides showed better imaging properties compared to 18F-tracers, i.e., higher tumor/background ratios and no accumulation in non-target organs except for excretory organs.

Synthesis and in Vitro and in Vivo Evaluation of SiFA-Tagged Bombesin and RGD Peptides as Tumor Imaging Probes for Positron Emission Tomography

2014 ◽  
Vol 25 (4) ◽  
pp. 738-749 ◽  
Author(s):  
Simon Lindner ◽  
Christina Michler ◽  
Stephanie Leidner ◽  
Christian Rensch ◽  
Carmen Wängler ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Tumor Imaging ◽  
Emission Tomography ◽  
In Vivo Evaluation ◽  
Rgd Peptides ◽  
Positron Emission ◽  
Imaging Probes

Synthesis, Radiolabeling, and Biological Evaluation of 5-Hydroxy-2-[18F]fluoroalkyl-tryptophan Analogues as Potential PET Radiotracers for Tumor Imaging

2016 ◽  
Vol 59 (11) ◽  
pp. 5324-5340 ◽  
Author(s):  
Aristeidis Chiotellis ◽  
Adrienne Müller Herde ◽  
Simon L. Rössler ◽  
Ante Brekalo ◽  
Erika Gedeonova ◽  
...  
Keyword(s):  
Tumor Imaging ◽  
Biological Evaluation ◽  
Pet Radiotracers ◽  
Tryptophan Analogues
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