Targeting integrin αvβ6 with gallium-68 tris (hydroxypyridinone) based PET probes

Giuseppe Floresta, Siham Memdouh, Truc Pham, Michelle T Ma, Philip J Blower, Robert C Hider, Vincenzo Abbate, Agostino Cilibrizzi

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Expression of the cellular transmembrane receptor αvβ6 integrin is mostly restricted to malignant epithelial cells in a wide variety of carcinomas, including pancreatic and others derived from epithelial tissues. Thus, this protein is considered an attractive target for tumour imaging and therapy. Two different 68Ga hexadentate tris (3,4-hydroxypyridinone) (THP) chelators were produced in this study and coupled to the αvβ6 integrin-selective peptide cyclo(FRGDLAFp(NMe)K) via NHS chemistry. Radiolabelling experiments confirmed a high radiochemical yield of the two PET probes. In addition, cellular binding studies showed high binding affinities in the nanomolar range. The two integrin αvβ6-peptide-THP synthesized and radiolabeled in this study will facilitate in vivo monitoring of transmembrane receptor αvβ6 integrin by using the advantage of THP chemistry for rapid, efficient and stable gallium chelation.

Original languageEnglish
Pages (from-to)12796-12803
Number of pages8
JournalDalton transactions (Cambridge, England : 2003)
Issue number34
Early online date11 Aug 2022
Publication statusPublished - 30 Aug 2022

ASJC Scopus subject areas

  • Inorganic Chemistry


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