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

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          Abstract

          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.

          Abstract

          Two 68Ga-radiolabeled integrin αvβ6-peptide-THPs to enable in vivo monitoring of the transmembrane receptor αvβ6 integrin, by taking advantage of THP chemistry for rapid, efficient and stable gallium chelation.

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          Author and article information

          Journal
          Dalton Trans
          Dalton Trans
          DT
          ICHBD9
          Dalton Transactions (Cambridge, England : 2003)
          The Royal Society of Chemistry
          1477-9226
          1477-9234
          11 August 2022
          30 August 2022
          11 August 2022
          : 51
          : 34
          : 12796-12803
          Affiliations
          [a] King's College London, Institute of Pharmaceutical Science, Franklin Wilkins Building London SE1 9NH UK agostino.cilibrizzi@ 123456kcl.ac.uk
          [b] Department of Drug and Health Sciences, University of Catania Catania Italy
          [c] King's College London, Division of Imaging Sciences and Biomedical Engineering, Fourth Floor Lambeth Wing, St Thomas’ Hospital London SE1 7EH UK
          [d] Centre for Therapeutic Innovation, University of Bath Bath UK
          Author information
          https://orcid.org/0000-0002-0668-1260
          https://orcid.org/0000-0002-3349-7346
          https://orcid.org/0000-0001-6290-1590
          https://orcid.org/0000-0003-4510-3639
          https://orcid.org/0000-0002-3300-0520
          https://orcid.org/0000-0002-9711-5183
          Article
          d2dt00980c
          10.1039/d2dt00980c
          9425781
          35972045
          8def4e0f-1a0b-4fb4-85ff-ca24b04e4992
          This journal is © The Royal Society of Chemistry
          History
          : 30 March 2022
          : 11 August 2022
          Page count
          Pages: 8
          Funding
          Funded by: Horizon 2020 Framework Programme, doi 10.13039/100010661;
          Award ID: 893784
          Funded by: Royal Society, doi 10.13039/501100000288;
          Award ID: IEC\R2\212003
          Funded by: Cancer Research UK, doi 10.13039/501100000289;
          Award ID: C63178/A24959
          Funded by: EPSRC Centre for Doctoral Training in Medical Imaging, doi 10.13039/501100013915;
          Award ID: EP/L015226/1
          Funded by: Rosetrees Trust, doi 10.13039/501100000833;
          Award ID: M685
          Award ID: M606
          Funded by: Wellcome Trust, doi 10.13039/100010269;
          Award ID: 212885/Z/ 18/Z
          Funded by: Engineering and Physical Sciences Research Council, doi 10.13039/501100000266;
          Award ID: WT088641/Z/09/Z
          Categories
          Chemistry
          Custom metadata
          Paginated Article

          Inorganic & Bioinorganic chemistry
          Inorganic & Bioinorganic chemistry

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