Simple and convenient radiolabeling of proteins using a prelabeling-approach with thiol-DOTA

Bioorg Med Chem Lett. 2009 Apr 1;19(7):1926-9. doi: 10.1016/j.bmcl.2009.02.052. Epub 2009 Feb 20.

Abstract

Commonly applied methods for radiometal-labeling of proteins require complex and protracted derivatization reactions of the protein and the subsequent radiolabeling is time-consuming due to the low reaction temperatures applicable. Therefore, a convenient and efficient prelabeling technique for proteins using the DOTA derivative 2,2',2''-(10-(2-(2-mercaptoethylamino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid (thiol-DOTA) containing a thiol moiety for rapid and selective introduction into maleimide-derivatized proteins was developed. Thiol-DOTA was labeled with (68)Ga, (90)Y and (177)Lu and subsequently introduced into bovine serum albumin and a human IgG with maximum radiochemical yields of 66%. The entire radiolabeling procedure was completed after only 30 min making this a favorable new labeling technique for proteins.

MeSH terms

  • Animals
  • Cattle
  • Heterocyclic Compounds, 1-Ring / chemistry*
  • Humans
  • Immunoglobulin G / chemistry
  • Isotope Labeling / methods*
  • Maleimides / chemistry
  • Metals / chemical synthesis
  • Metals / chemistry
  • Proteins / chemistry*
  • Serum Albumin, Bovine / chemistry

Substances

  • 2,2',2''-(10-(2-(2-mercaptoethylamino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid
  • Heterocyclic Compounds, 1-Ring
  • Immunoglobulin G
  • Maleimides
  • Metals
  • Proteins
  • maleimide
  • Serum Albumin, Bovine