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Gastrin and Cholecystokinin Peptide-based Radiopharmaceuticals: an in Vivo and in Vitro Comparison by Anna Lucia Tornesello; Michela Aurilio; Antonella Accardo; Laura Tarallo; Antonio Barbieri; Claudio Arra; Diego Tesauro; Giancarlo Morelli; Luigi Aloj is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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## Abstract The development of suitable radioligands for targeting CCK‐2 receptor expressing tumors, such as medullary thyroid carcinoma, is of great clinical interest. In the search for the best CCK‐2R binding peptides, we have synthesized, evaluated and compared the CCK8 peptide (Asp‐Tyr‐Met‐Gly‐Trp‐Met‐Asp‐PheNH~2~) and two gastrin analogs commonly referred to as MG0 (DGlu‐Glu(5)‐Ala‐Tyr‐Gly‐Trp‐Met‐Asp‐PheNH~2~) and MG11 (DGlu(1)‐Ala‐Tyr‐Gly‐Trp‐Met‐Asp‐PheNH~2~). The N‐terminal portion of the three peptide sequences was derivatized by introducing the DTPAGlu or DOTA chelators to allow radiolobeling with ^111^In(III) and ^68^Ga(III), respectively. Saturation binding and cellular internalization experiments were performed on A431 cells overexpressing CCK2R (A431‐CCK2R). All compounds showed Kd values in the nM range and were internalized with similar rates in CCK2 receptor overexpressing cells. Biodistribution experiments showed higher specific uptake of both MG0‐based compounds compared to conjugates containing the CCK8 and MG11 peptide sequences. The higher retention levels of MG0‐based peptides were associated with markedly elevated and undesired kidney uptake compared to

Who reads Gastrin and Cholecystokinin Peptide-based Radiopharmaceuticals: an in Vivo and in Vitro Comparison?

Author

Anna Lucia Tornesello; Michela Aurilio; Antonella Accardo; Laura Tarallo; Antonio Barbieri; Claudio Arra; Diego Tesauro; Giancarlo Morelli; Luigi Aloj

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 1075-2617)

Published

2011

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)