Highly Efficient and Stable Strain-Release Radioiodination for Thiol Chemoselective Bioconjugation.

We report a novel thiol selective radioiodination method based on strain-release reaction. A new heterobifunctional radioiodination agent which has very good thiol selectivity and excellent stability with high radiolabeling yield was synthesized, characterized, and applied successfully for thiol-contained peptide labeling.