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doi:10.13040/ijpsr.0975-8232.4(1).1-18

IJPSR

2013

DOI: 10.13040/ijpsr.0975-8232.4(1).1-18

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Abstract: The treatment of cancer is limited by a number of factors including the low therapeutic index of most chemotherapeutic agents, the emergence of drugand radiation-resistant tumor cells, tumor heterogeneity and the presence of metastatic disease.

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2020

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References 96 publications

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Radiosynthesis, Biological Evaluation, and Preclinical Study of a ⁶⁸Ga-Labeled Cyclic RGD Peptide as an Early Diagnostic Agent for Overexpressed α_vβ₃ Integrin Receptors in Non-Small-Cell Lung Cancer

Pirooznia

Abdi

Beiki

et al. 2020

Contrast Media & Molecular Imaging

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The αvβ3 integrin receptors have high expression on proliferating growing tumor cells of different origins including non-small-cell lung cancer. RGD-containing peptides target the extracellular domain of integrin receptors. This specific targeting makes these short sequences a suitable nominee for theranostic application. DOTA-E(cRGDfK)2 was radiolabeled with 68Ga efficiently. The in vivo and in vitro stability was examined in different buffer systems. Metabolic stability was assessed in mice urine. In vitro specific binding, cellular uptake, and internalization were determined. The tumor-targeting potential of [68Ga]Ga-DOTA-E(cRGDfK)2 in a lung cancer mouse model was studied. Besides, the very early diagnostic potential of the 68Ga-labeled RGD peptide was evaluated. The acquisition and reconstruction of the PET-CT image data were also carried out. Radiochemical and radionuclide purity for [68Ga]Ga-DOTA-E(cRGDfK)2 was >%98 and >%99, respectively. Radiotracer showed high in vivo, in vitro, and metabolic stability which was determined by ITLC. The dissociation constant (Kd) of [68Ga]Ga-DOTA-E(cRGDfK)2 was 15.28 nM. On average, more than 95% of the radioactivity was specific binding (internalized + surface-bound) to A549 cells. Biodistribution data showed that radiolabeled peptides were accumulated significantly in A549 tumor and excreted rapidly by the renal system. Tumor uptake peaks were at 1-hour postinjection for [68Ga]Ga-DOTA-E(cRGDfK)2. The tumor was clearly visualized in all images. [68Ga]Ga-DOTA-E(cRGDfK)2 can be used as a peptide-based imaging agent allowing very early detection of different cancers overexpressing αvβ3 integrin receptors and can be a potential candidate in clinical peptide-based imaging for lung cancer.

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Radiosynthesis, Biological Evaluation, and Preclinical Study of a ⁶⁸Ga-Labeled Cyclic RGD Peptide as an Early Diagnostic Agent for Overexpressed α_vβ₃ Integrin Receptors in Non-Small-Cell Lung Cancer

Pirooznia

Abdi

Beiki

et al. 2020

Contrast Media & Molecular Imaging

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show abstract

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Untitled

Abstract: The treatment of cancer is limited by a number of factors including the low therapeutic index of most chemotherapeutic agents, the emergence of drugand radiation-resistant tumor cells, tumor heterogeneity and the presence of metastatic disease.

Cited by 1 publication

References 96 publications

Radiosynthesis, Biological Evaluation, and Preclinical Study of a ⁶⁸Ga-Labeled Cyclic RGD Peptide as an Early Diagnostic Agent for Overexpressed α_vβ₃ Integrin Receptors in Non-Small-Cell Lung Cancer

Radiosynthesis, Biological Evaluation, and Preclinical Study of a ⁶⁸Ga-Labeled Cyclic RGD Peptide as an Early Diagnostic Agent for Overexpressed α_vβ₃ Integrin Receptors in Non-Small-Cell Lung Cancer

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Untitled

Abstract: The treatment of cancer is limited by a number of factors including the low therapeutic index of most chemotherapeutic agents, the emergence of drugand radiation-resistant tumor cells, tumor heterogeneity and the presence of metastatic disease.

Cited by 1 publication

References 96 publications

Radiosynthesis, Biological Evaluation, and Preclinical Study of a 68Ga-Labeled Cyclic RGD Peptide as an Early Diagnostic Agent for Overexpressed αvβ3 Integrin Receptors in Non-Small-Cell Lung Cancer

Radiosynthesis, Biological Evaluation, and Preclinical Study of a 68Ga-Labeled Cyclic RGD Peptide as an Early Diagnostic Agent for Overexpressed αvβ3 Integrin Receptors in Non-Small-Cell Lung Cancer

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Product

Resources

About

Radiosynthesis, Biological Evaluation, and Preclinical Study of a ⁶⁸Ga-Labeled Cyclic RGD Peptide as an Early Diagnostic Agent for Overexpressed α_vβ₃ Integrin Receptors in Non-Small-Cell Lung Cancer

Radiosynthesis, Biological Evaluation, and Preclinical Study of a ⁶⁸Ga-Labeled Cyclic RGD Peptide as an Early Diagnostic Agent for Overexpressed α_vβ₃ Integrin Receptors in Non-Small-Cell Lung Cancer