Expanding the Applicability of the Metal Labeling of Biomolecules by the RIKEN Click Reaction: A Case Study with Gallium-68 Positron Emission Tomography

Chembiochem. 2018 Oct 4;19(19):2055-2060. doi: 10.1002/cbic.201800335. Epub 2018 Sep 14.


Radiolabeled biomolecules with short half-life times are of increasing importance for positron emission tomography (PET) imaging studies. Herein, we demonstrate an improved and generalized method for synthesizing a [radiometal]-unsaturated aldehyde as a lysine-labeling probe that can be easily conjugated into various biomolecules through the RIKEN click reaction. As a case study, 68 Ga-PET imaging of U87MG xenografted mice is demonstrated by using the 68 Ga-DOTA-RGDyK peptide, which is selective to αV β3 integrins.

Keywords: biomolecules; click chemistry; gallium; positron emission tomography; radiopharmaceuticals.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Gallium Radioisotopes / chemistry
  • Gallium Radioisotopes / pharmacokinetics*
  • Heterografts
  • Humans
  • Integrin alphaVbeta3 / metabolism
  • Mice
  • Mice, Inbred BALB C
  • Peptides / chemistry
  • Peptides / pharmacokinetics*
  • Positron-Emission Tomography / methods*
  • Radiopharmaceuticals / pharmacokinetics*
  • Tissue Distribution


  • Gallium Radioisotopes
  • Integrin alphaVbeta3
  • Peptides
  • Radiopharmaceuticals
  • Gallium-68