Progress in covalent site-specific labeling strategy and its application in radiopharmaceuticals
WU Qiu-yan
CHU Jin-yu
LIANG Xu-rui
SU Peng-yuan
ZHANG Ya
DENG Wan-su
HUANG He
ZHANG Tao
Abstract：Radiopharmaceuticals are the"soul"of nuclear medicine,capable of correlating the molecular mechanism at the micro level with the macro disease phenotype.They are extensively utilized in the diagnosis and treatment of clinical diseases and constitute the cornerstone of precision medicine.Currently,there are two primary approaches for radionuclide labeling of radiopharmaceuticals.Non-metallic radionuclides are directly linked to the carriers through covalent bonds,and the binding effect is robust.Conversely,radiometallic nuclides require chelating agents to form coordination bonds and then bind to ligands,and the binding effect is relatively weak.Thus,covalently labeled binding methods are more appealing in the development of radiopharmaceuticals.This paper primarily presents the covalent site-specific labeling strategy and its application progress in radiopharmaceuticals,aiming to offer reference for relevant radiopharmaceutical development.
Keywords：radionuclidesconvalent site-specific labelingcoodination chelation labelingorganic radio-chemistryradiohalogen chemistryradiopharmaceuticals
Publication Date：2025-05-30
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：7( 1070-1076 )