PEGylation of a PN2S Chelating Agent: an Efficient Micelle-Based Labeling Method for the Development of 99mTechnetium and 188Rhenium Radiopharmaceuticals Useful for Tumor Diagnosis and Treatment

摘要

N-(N-(3-diphenylphosfinopropionyl)glycyl)- cysteine [PN2S-OH] is a small molecule that can chelate 99mtechnetium and 188rhenium. PEGylation of such molecule, firstly performed to exploit the EPR effect for tumor targeting, lead to the discovery of a new easy labeling method of such conjugates with Tc and Re. In fact the conjugates are able to reduce directly these radiometals in the reduced form suitable for coordination, generating a new class of radiopharmaceuticals useful for tumor diagnosis and treatment [1]