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Updated: May 28, 2026

MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent
Published on: September 3, 2013
A Review of Approaches to the Synthesis of DCL-Based Prostate-Specific Membrane Antigen Ligands
Nikolai Y Zyk1, Nina S Butakova1, Aleksei E Machulkin1
1Chemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russia.
Abstract:
Prostate-specific membrane antigen (PSMA) ligands are currently one of the popular platforms for creating drugs targeted at prostate cancer tumor cells. In this review, we have collected and systematized current approaches to the synthesis of PSMA ligands based on N-[N-[(S)-1,3-dicarboxypropyl]carbamoyl]-(S)-L-lysine (DCL), the most widely used scaffold in the design of such ligands. The main approaches to each stage of the synthesis of PSMA inhibitors with various structures are considered in detail, and the existing synthetic techniques are compiled and analyzed. We also review examples of using different synthetic pathways for diagnostic and therapeutic drugs based on PSMA ligands. We propose an algorithm for selecting a synthetic route based on the structure of the target ligand.

