68Ga somatostatin analog radiolabelling: The radiopharmacist's point of view

Lamesa, Chloé; Rauscher, A.; Lacoeuille, Franck; Desruet, Marie-Dominique; Guillet, Benjamin; Faivre-Chauvet, Alain

doi:10.1016/j.mednuc.2015.01.003

Cited by 2 publications

(1 citation statement)

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“…68 Ga decays into a stable isotope, 68 Zn, through positron emission (89%) and electron capture (11%) processes . A tremendous advantage of 68 Ga is its low cost and facile production by a 68 Ge/ 68 Ga generator, and radiotracers for PET can be synthesized from 68 Ga in the laboratory . A Lewis acid, Ga is classified as a hard acid; it strongly binds ligands or chelators containing Lewis basic N and O donor atoms to form stable complexes .…”

Section: Introductionmentioning

confidence: 99%

Synthesis and evaluation of ⁶⁸Ga‐HBED‐CC‐EDBE‐folate for positron‐emission tomography imaging of overexpressed folate receptors on CT26 tumor cells

Choi

Lee

Park

et al. 2017

Labelled Comp Radiopharmac

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The Ga is a positron-emitting radionuclide that can be combined with bifunctional chelating agents and bioactive substances for use as positron-emission tomography (PET) diagnostic agents. The HBED-CC is an acyclic chelating agent that is rapidly labeled with Ga under mild conditions. To target cancer cells, bioactive substances can be conjugated to the carboxyl terminus of HBED-CC. Because folic acid strongly binds to folate receptors that are overexpressed on the surfaces of many types of cancer cells, it was coupled with HBED-CC through a small polyethylene glycol-based linker (EDBE) to generate an active, receptor-selective targeting system. The HBED-CC-EDBE-folate (HCEF) precursor was readily labeled with Ga in 5 minutes at room temperature (98% radiochemical yield; 99% radiochemical purity after isolation). In cellular uptake tests, higher uptakes of Ga-HCEF were observed for the CT26 and KB cell lines (which express folate receptors) than for the A549 cell line (which does not). Finally, in vivo micro-PET measurements over 2 hours of binding in BALB/c mice into which CT26 tumors had been transplanted showed the selective accumulation of Ga-HCEF in the folate receptor-expressing CT26 tumors. These results confirmed the potential of Ga-HCEF as a PET diagnostic agent for tumors that express folate receptors.

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Section: Introductionmentioning

confidence: 99%

Synthesis and evaluation of ⁶⁸Ga‐HBED‐CC‐EDBE‐folate for positron‐emission tomography imaging of overexpressed folate receptors on CT26 tumor cells

Choi

Lee

Park

et al. 2017

Labelled Comp Radiopharmac

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Acid resistant zirconium phosphate for the long term application of 68Ge/68Ga generator system

Lee

Vyas

Kim

et al. 2016

Applied Radiation and Isotopes

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68Ga somatostatin analog radiolabelling: The radiopharmacist's point of view

Cited by 2 publications

References 46 publications

Synthesis and evaluation of ⁶⁸Ga‐HBED‐CC‐EDBE‐folate for positron‐emission tomography imaging of overexpressed folate receptors on CT26 tumor cells

Synthesis and evaluation of ⁶⁸Ga‐HBED‐CC‐EDBE‐folate for positron‐emission tomography imaging of overexpressed folate receptors on CT26 tumor cells

Acid resistant zirconium phosphate for the long term application of 68Ge/68Ga generator system

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68Ga somatostatin analog radiolabelling: The radiopharmacist's point of view

Cited by 2 publications

References 46 publications

Synthesis and evaluation of 68Ga‐HBED‐CC‐EDBE‐folate for positron‐emission tomography imaging of overexpressed folate receptors on CT26 tumor cells

Synthesis and evaluation of 68Ga‐HBED‐CC‐EDBE‐folate for positron‐emission tomography imaging of overexpressed folate receptors on CT26 tumor cells

Acid resistant zirconium phosphate for the long term application of 68Ge/68Ga generator system

Contact Info

Product

Resources

About

Synthesis and evaluation of ⁶⁸Ga‐HBED‐CC‐EDBE‐folate for positron‐emission tomography imaging of overexpressed folate receptors on CT26 tumor cells

Synthesis and evaluation of ⁶⁸Ga‐HBED‐CC‐EDBE‐folate for positron‐emission tomography imaging of overexpressed folate receptors on CT26 tumor cells