Expression of the cellular transmembrane receptor alpha v beta 6 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 Ga-68 hexadentate tris (3,4-hydroxypyridinone) (THP) chelators were produced in this study and coupled to the alpha v beta 6 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 alpha v beta 6-peptide-THP synthesized and radiolabeled in this study will facilitate in vivo monitoring of transmembrane receptor alpha v beta 6 integrin by using the advantage of THP chemistry for rapid, efficient and stable gallium chelation.

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

Floresta G.;Pham T.;
2022

Abstract

Expression of the cellular transmembrane receptor alpha v beta 6 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 Ga-68 hexadentate tris (3,4-hydroxypyridinone) (THP) chelators were produced in this study and coupled to the alpha v beta 6 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 alpha v beta 6-peptide-THP synthesized and radiolabeled in this study will facilitate in vivo monitoring of transmembrane receptor alpha v beta 6 integrin by using the advantage of THP chemistry for rapid, efficient and stable gallium chelation.
Antigens, Neoplasm
Chelating Agents
Integrin alphaVbeta3
Integrins
Peptides
Tissue Distribution
Gallium Radioisotopes
Positron-Emission Tomography
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.11769/537931
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