Linker Effects on Biological Properties of <sup>111</sup>In-Labeled DTPA Conjugates of a Cyclic RGDfK Dimer

Jia, Bing; Liu, Zhaofei; Shi, Jiyun; Yu, Zilin; Liu, Yang; Zhao, Hang; He, Zhengjie; Liu, Shuang; Wang, Fan

doi:10.1021/bc7002988

Cited by 46 publications

(48 citation statements)

References 45 publications

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“…105 The RGD-BBN was conjugated with 1,4,7-triazacyclononanetriacetic acid (NOTA) for 68 Ga radiolabeling and preclinical PET imaging of human PC3 and MDA-MB-435 melanoma xenograft mice. The authors investigated dual tumor targeting because binding affinity might be lower with monomeric peptides 106 ; however, they also compared the radiolabeled heterodimer 68 Ga-NOTA-RGD-BBN with the corresponding monomers 68 Ga-NOTA-RGD, 68 Ga-NOTA-BBN. The competitive radioligands 125 I-c[RGDyK] (integrin expressing U87MG glioma cells) and 125 I[Tyr 4 ] (PC3 cells) were used to characterize in vitro intregrin α v β 3 and GRPr binding and specificity of RGD-BBN, NOTA-RGD-BBN, BBN, and RGD.…”

Section: Radiogallium Labeled Compoundsmentioning

confidence: 99%

The Next Generation of Positron Emission Tomography Radiopharmaceuticals in Oncology

Rice

Roney

Daumar

et al. 2011

Seminars in Nuclear Medicine

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Although 18F-fluorodeoxyglucose (18F-FDG) is still the most widely used positron emission tomography (PET) radiotracer, there are a few well-known limitations to its use. The last decade has seen the development of new PET probes for in vivo visualization of specific molecular targets, along with important technical advances in the production of positron-emitting radionuclides and their related labeling methods. As such, a broad range of new PET tracers are in preclinical development or have recently entered clinical trials. The topics covered in this review include labeling methods, biological targets, and the most recent preclinical or clinical data of some of the next generation of PET radiopharmaceuticals. This review, which is by no means exhaustive, has been separated into sections related to the PET radionuclide used for radiolabeling: fluorine-18, for the labeling of agents such as FACBC, FDHT, choline, and Galacto-RGD; carbon-11, for the labeling of choline; gallium-68, for the labeling of peptides such as DOTATOC and bombesin analogs; and the long-lived radionuclides iodine-124 and zirconium-89 for the labeling of monoclonal antibodies cG250, and J591 and trastuzumab, respectively.

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Section: Radiogallium Labeled Compoundsmentioning

confidence: 99%

The Next Generation of Positron Emission Tomography Radiopharmaceuticals in Oncology

Rice

Roney

Daumar

et al. 2011

Seminars in Nuclear Medicine

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“…They have been extensively used in the study of tumor angiogenesis, growth and metastasis (1). A decade ago, a series of RGD peptides attached to different radionuclides were developed for positron emission tomography (PET) (2) and single-photon emission computed tomography (SPECT) (3) imaging. Although nuclear imaging modalities have high sensitivity and allow accurate quantification of tracer distribution in the body, they are associated with ionizing radiation, high-cost, and comparatively poor spatial and temporal resolution.…”

Section: Introductionmentioning

confidence: 99%

Integrin αvβ3-Targeted IRDye 800CW Near-Infrared Imaging of Glioblastoma

Huang

Vider

Kovar

et al. 2012

Clinical Cancer Research

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Purpose Integrin αvβ3 plays an important role in tumor angiogenesis, growth and metastasis. We have tested a targeted probe to visualize integrin receptor expression in glioblastomas using near-infrared fluorescent (NIRF) imaging. Experimental design A transgenic glioblastoma mouse model (RCAS-PDGF-driven/tv-a glioblastoma, which mimics the infiltrative growth pattern of human glioblastomas), and two human orthotopic glioblastoma models, (U-87 MG with high integrin β3 expression and TS543 with low integrin β3 expression), were studied. An integrin-targeting NIRF probe, IRDye 800CW-cyclic-RGD peptide (IRDye 800CW-RGD), was tested by in vivo and ex vivo NIRF imaging. Results We demonstrate that the IRDye 800CW-RGD peptide: 1) specifically binds to integrin receptors, 2) is selectively localized to glioblastoma tissue with overexpressed integrin receptors and is retained over prolonged periods of time, 3) is associated with minimal autofluorescence and photobleaching due to imaging at 800 nm, 4) provides delineation of tumor tissue with high precision due to a high tumor-to-normal brain fluorescence ratio (79.7±6.9, 31.2±2.8, and 16.3±1.3) in the U-87 MG, RCAS-PDGF, and TS543 models, respectively; p<0.01) and 5) enables fluorescence-guided glioblastoma resection. Importantly, small foci of residual fluorescence were observed after resection was completed using white light imaging alone, and these fluorescent foci were shown to represent residual tumor tissue by histology. Conclusions NIRF imaging with the IRDye 800CW-RGD probe provides a simple, rapid, low-cost, non-radioactive and highly translatable approach for improved intraoperative glioblastoma visualization and resection. It also has the potential to serve as an imaging platform for noninvasive cancer detection and drug efficacy evaluation studies.

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“…Second, the binding affinity of the monomeric peptide for the targeted receptors is relatively low, which may result in a low tumor uptake and rapid dissociation form the tumor targets . For example, the binding affinity of RGD monomers is about fivefold to tenfold lower than that of the dimeric RGD peptide analogs . Third, the in vivo pharmacokinetics of the monomeric peptides may be suboptimal.…”

Section: Introductionmentioning

confidence: 99%

¹⁸F labeled RGD‐A7R peptide for dual integrin and VEGF‐targeted tumor imaging in mice bearing U87MG tumors

Liang

Guo

et al. 2014

Labelled Comp Radiopharmac

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The aim of this study is to develop a novel Arg-Gly-Asp acid (RGD) and Ala-Thr-Trp-Leu-Pro-Pro-Arg (ATWLPPR A7R) peptide-containing ligand for (18) F labeling as αvβ3 and vascular endothelial growth factor receptor-targeted imaging agent. (18) F-RGD-A7R was prepared by conjugation with (18) F-SFB. The final product was purified by high-performance liquid chromatography and tested in vitro and in vivo. Cell-binding assays of RGD-A7R, RGD and RGD-A7R, A7R were tested in U87MG cells ((125) I-RGDyK and (125) I-A7RY as radioligand, respectively). Preliminary biodistribution of the (18) F-RGD-A7R was also evaluated. The RGD-A7R had good integrin binding affinity (50% inhibitory concentration (IC50 ) = 21.67 and 23.68 nM, slightly lower than unmodified RGD (40.02 nM) and A7R (50.18 nM)). The radiotracer had receptor-mediated activity accumulation in U87MG tumor (1.90 ± 0.34 percentage of injected dose per gram (%ID/g) at 0.5 h postinjection), which is known to be integrin positive. After blocking with RGD-A7R, the tumor uptake was reduced to 0.47 ± 0.06 %ID/g at 0.5 h postinjection. (18) F-RGD-A7R exhibited dual receptor targeting properties both in vitro and in vivo. The favorable characterizations of (18) F-RGD-A7RY, such as convenient synthesis, high specific activity, and high tumor uptake, warrant its further investigation for clinical cancer imaging.

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Linker Effects on Biological Properties of ¹¹¹In-Labeled DTPA Conjugates of a Cyclic RGDfK Dimer

Cited by 46 publications

References 45 publications

The Next Generation of Positron Emission Tomography Radiopharmaceuticals in Oncology

The Next Generation of Positron Emission Tomography Radiopharmaceuticals in Oncology

Integrin αvβ3-Targeted IRDye 800CW Near-Infrared Imaging of Glioblastoma

¹⁸F labeled RGD‐A7R peptide for dual integrin and VEGF‐targeted tumor imaging in mice bearing U87MG tumors

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Linker Effects on Biological Properties of 111In-Labeled DTPA Conjugates of a Cyclic RGDfK Dimer

Cited by 46 publications

References 45 publications

The Next Generation of Positron Emission Tomography Radiopharmaceuticals in Oncology

The Next Generation of Positron Emission Tomography Radiopharmaceuticals in Oncology

Integrin αvβ3-Targeted IRDye 800CW Near-Infrared Imaging of Glioblastoma

18F labeled RGD‐A7R peptide for dual integrin and VEGF‐targeted tumor imaging in mice bearing U87MG tumors

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Linker Effects on Biological Properties of ¹¹¹In-Labeled DTPA Conjugates of a Cyclic RGDfK Dimer

¹⁸F labeled RGD‐A7R peptide for dual integrin and VEGF‐targeted tumor imaging in mice bearing U87MG tumors