Gallium-68: Chemistry and Radiolabeled Peptides Exploring Different Oncogenic Pathways

Clément Morgat, Elif Hindié, Anil K. Mishra, Michèle Allard, Philippe Fernandez
Cancer Biotherapy and Radiopharmaceuticals. 2013-03-01; 28(2): 85-97
DOI: 10.1089/cbr.2012.1244

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1. Cancer Biother Radiopharm. 2013 Mar;28(2):85-97. doi: 10.1089/cbr.2012.1244.

Gallium-68: chemistry and radiolabeled peptides exploring different oncogenic

Morgat C(1), Hindié E, Mishra AK, Allard M, Fernandez P.

Author information:
(1)INCIA, UMR 5287, Univ. Bordeaux, Talence, France.

Abstract Early and specific tumor detection and also therapy selection and
response evaluation are some challenges of personalized medicine. This calls for
high sensitive and specific molecular imaging such as positron emission
tomography (PET). The use of peptides for PET molecular imaging has undeniable
advantages: possibility of targeting through peptide-receptor interaction, small
size and low-molecular weight conferring good penetration in the tissue or at
cellular level, low toxicity, no antigenicity, and possibility of wide choice for
radiolabeling. Among β(+)-emitter radioelements, Gallium-68 is a very attractive
positron-emitter compared with carbon-11 or fluorine-18 taking into account its
easy production via a (68)Ge/(68)Ga generator and well established
radiochemistry. Gallium-68 chemistry is based on well-defined coordination
complexes with macrocycle or chelates having strong binding properties,
particularly suitable for linking peptides that allow resistance to in vivo
transchelation of the metal ion. Understanding specific and nonspecific molecular
mechanisms involved in oncogenesis is one major key to develop new molecular
imaging tools. The present review focuses on peptide signaling involved in
different oncogenic pathways. This peptide signalization might be common for
tumoral and non-tumoral processes or could be specific of an oncological process.
This review describes gallium chemistry and different (68)Ga-radiolabeled
peptides already in use or under development aiming at developing molecular PET
imaging of different oncological processes.

DOI: 10.1089/cbr.2012.1244
PMID: 23461410 [Indexed for MEDLINE]

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