Synthesis and evaluation of Tc-99m-labeled RRL-containing peptide as a non-invasive tumor imaging agent in a mouse fibrosarcoma model

Kim, Dae‐Weung; Kim, Woo Hyoung; Kim, Myoung Hyoun; Kim, Chang Guhn

doi:10.1007/s12149-015-1002-6

Cited by 13 publications

(16 citation statements)

References 22 publications

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“…Tc-99 m TAMRA-GHEG-ECG-SDV only expression of β 3 integrin, as a potential target of the SDVcontaining peptide on HT-1080 tumor. The ECG ligand of TAMRA-GHEG-ECG-SDV, a tripeptide including multiple nitrogen and a single sulfur atom, showed strong and stable chelation with Tc-99 m, and is considered as a good candidate for the Tc-99 m chelating ligand in our previous and the present studies (6,19,20). Tc-99 m is the most widely used radioisotope for SPECT imaging.…”

Section: Mean %Id/g (Sd)mentioning

confidence: 62%

A novel Tc‐99 m and fluorescence labeled peptide as a multimodal imaging agent for targeting angiogenesis in a murine tumor model

Kim

et al. 2016

Contrast Media & Molecular

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The serine-aspartic acid-valine (SDV) peptide binds specifically to integrin α β . In the present study, we successfully developed a TAMRA-GHEG-ECG-SDV peptide labeled with both Tc-99 m and TAMRA to target the integrin α β of tumor cells; furthermore, we evaluated the diagnostic performance of Tc-99 m TAMRA-GHEG-ECG-SDV as a dual-modality imaging agent for tumor of the murine model. TAMRA-GHEG-ECG-SDV was synthesized using Fmoc solid-phase peptide synthesis. Radiolabeling of TAMRA-GHEG-ECG-SDV with Tc-99 m was done using ligand exchange methods. Labeling stability and cytotoxicity studies were performed. Gamma camera imaging, biodistribution and ex vivo imaging studies were performed in murine models with HT-1080 and HT-29 tumors. A tumor tissue slide was prepared and analyzed using confocal microscopy. After radiolabeling procedures with Tc-99 m, the Tc-99 m TAMRA-GHEG-ECG-SDV complexes were prepared in high yield (>99%). In the gamma camera imaging study, a substantial uptake of Tc-99 m TAMRA-GHEG-ECG-SDV into HT-1080 tumor (integrin α β positive) and low uptake of Tc-99 m TAMRA-GHEG-ECG-SDV into HT-29 tumor (integrin α β negative) were demonstrated. A competition study revealed that HT-1080 tumor uptake was effectively blocked by the co-injection of an excess concentration of SDV. Specific uptake of Tc-99 m TAMRA-GHEG-ECG-SDV was confirmed by biodistribution, ex vivo imaging and confocal microscopy studies. Our in vivo and in vitro studies revealed substantial uptake of Tc-99 m TAMRA-GHEG-ECG-SDV in the integrin α β -positive tumor. Tc-99 m TAMRA-GHEG-ECG-SDV could be a good candidate for a dual-modality imaging agent targeting tumor angiogenesis. Copyright © 2016 John Wiley & Sons, Ltd.

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Section: Mean %Id/g (Sd)mentioning

confidence: 62%

A novel Tc‐99 m and fluorescence labeled peptide as a multimodal imaging agent for targeting angiogenesis in a murine tumor model

Kim

et al. 2016

Contrast Media & Molecular

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“…The ECG ligand of the TAMRA‐GHEG‐ECG‐VAPG tripeptide including multiple nitrogen and single sulfur atoms showed strong and stable chelation with Tc‐99m and is considered as a good candidate for the Tc‐99m chelating ligand . Tc‐99m is the most widely used radioisotope for single‐photon emission computed tomography imaging.…”

Section: Discussionmentioning

confidence: 99%

“…Radiolabeling of TAMRA‐GHEG‐ECG‐VAPG and TAMRA‐GHEG‐ECG‐PGVA with Tc‐99m was done as described previously . Briefly, 300 μL of peptide solution (0.005 mg/mL in nitrogen‐purged water) and 300 μL of sodium tartrate (100 mg/mL in nitrogen‐purged water) were added and mixed in a microcentrifuge tube.…”

Section: Methodsmentioning

confidence: 99%

“…Radiolabeling of TAMRA-GHEG-ECG-VAPG and TAMRA-GHEG-ECG-PGVA with Tc-99m was done as described previously. 16,17 Briefly, 300 μL of peptide solution (0.005 mg/mL in nitrogen-purged water) and 300 μL of sodium tartrate (100 mg/mL in nitrogen-purged water) were added and mixed in a microcentrifuge tube. The peptide-containing tartrate solution was supplemented with 1.0 mL of Tc-99m pertechnetate (about 1110 MBq) and 30 μL SnCl 2 (1 mg/mL in nitrogen-purged 0.01 M HCl).…”

Section: Radiolabeling With Tc-99mmentioning

confidence: 99%

“…The ECG ligand of the TAMRA-GHEG-ECG-VAPG tripeptide including multiple nitrogen and single sulfur atoms showed strong and stable chelation with Tc-99m and is considered as a good candidate for the Tc-99m chelating ligand. 16,17,22 Tc-99m is the most widely used radioisotope for single-photon emission computed tomography imaging. The radionuclide has excellent physical characteristics for in vivo imaging, and Tc-99m-based imaging is very sensitive and highly quantitative.…”

Section: Figurementioning

confidence: 99%

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Synthesis and evaluation of Tc‐99m and fluorescence‐labeled elastin‐derived peptide, VAPG for multimodal tumor imaging in murine tumor model

Kim

et al. 2017

Labelled Comp Radiopharmac

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We developed a Tc-99m and fluorescence-labeled peptide, Tc-99m TAMRA-GHEG-ECG-VAPG to target tumor cells and evaluated the diagnostic performance as a dual-modality imaging agent for tumor in a murine model. TAMRA-GHEG-ECG-VAPG was synthesized by using Fmoc solid-phase peptide synthesis. Radiolabeling of TAMRA-GHEG-ECG-VAPG with Tc-99m was done by using ligand exchange via tartrate. Binding affinity and in vitro cellular uptake studies were performed. Gamma camera imaging, biodistribution, and ex vivo imaging studies were performed in murine models with SW620 tumors. Tumor tissue slides were prepared and analyzed with immunohistochemistry by using confocal microscopy. After radiolabeling procedures with Tc-99m, Tc-99m TAMRA-GHEG-ECG-VAPG complexes were prepared in high yield (>96%). The K of Tc-99m TAMRA-GHEG-ECG-VAPG determined by saturation binding was 16.8 ± 3.6 nM. Confocal microscopy images of SW620 cells incubated with TAMRA-GHEG-ECG-VAPG showed strong fluorescence in the cytoplasm. Gamma camera imaging revealed substantial uptake of Tc-99m TAMRA-GHEG-ECG-VAPG in tumors. Tumor uptake was effectively blocked by the coinjection of an excess concentration of VAPG. Specific uptake of Tc-99m TAMRA-GHEG-ECG-VAPG was confirmed by biodistribution, ex vivo imaging, and immunohistochemistry stain studies. In vivo and in vitro studies revealed substantial uptake of Tc-99m TAMRA-GHEG-ECG-VAPG in tumor cells. Tc-99m TAMRA-GHEG-ECG-VAPG has potential as a dual-modality tumor imaging agent.

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Diffusion‐induced anisotropic cancer invasion: A novel experimental method based on tumor spheroids

et al. 2022

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Tumour invasion is strongly influenced by microenvironment and, among other parameters, chemical stimuli play an important role. An innovative methodology for the quantitative investigation of chemotaxis in vitro by live imaging of morphology of cell spheroids, in 3D collagen gel, is presented here. The assay was performed by using a chemotactic chamber to impose a controlled gradients of nutrients (glucose) on spheroids, mimicking the chemotactic stimuli naturally occurring in the proximity of blood vessels. Different tumoral cell lines (PANC-1 and HT-1080) are compared to non-tumoral ones (NIH/3T3). Morphology response is observed by means a Time-lapse workstation equipped with an incubating system and quantified by image analysis techniques. Description of invasion phenomena was based on an engineering approach, based on transport phenomena concepts. As expected, NIH/3T3 spheroids are characterized by a limited tendency of cells to invade the surrounding tissue, unlike PANC-1 and HT-1080 that show relatively stronger response to gradients.

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Synthesis and evaluation of Tc-99m-labeled RRL-containing peptide as a non-invasive tumor imaging agent in a mouse fibrosarcoma model

Cited by 13 publications

References 22 publications

A novel Tc‐99 m and fluorescence labeled peptide as a multimodal imaging agent for targeting angiogenesis in a murine tumor model

A novel Tc‐99 m and fluorescence labeled peptide as a multimodal imaging agent for targeting angiogenesis in a murine tumor model

Synthesis and evaluation of Tc‐99m and fluorescence‐labeled elastin‐derived peptide, VAPG for multimodal tumor imaging in murine tumor model

Diffusion‐induced anisotropic cancer invasion: A novel experimental method based on tumor spheroids

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