ArticleRoyal Society open science2023
Synthesis and radiolabelling of PSMA-targeted derivatives containing GYK/MVK cleavable linkers.
Article in Royal Society open science, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed.
- Article
- The [18F] F-PSMA Probe: Chemical Perspectives.Current medicinal chemistry · 2025Review
- Improvement of End-of-Synthesis Radiochemical Purity ofPharmaceutics · 2024Article
- New tactics in the design of theranostic radiotracers.Npj imaging · 2024Review
- Reducing kidney uptake of radiolabelled exendin-4 using variants of the renally cleavable linker MVK.EJNMMI radiopharmacy and chemistry · 2023Article
- Synthesis and radiolabelling of PSMA-targeted derivatives containing GYK/MVK cleavable linkers.Royal Society open science · 2023Article
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Authors and funding
5 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Targeted radionuclide therapy (TRT) is a promising strategy to treat different types of cancer. TRT relies on a targeting vector used to deliver a therapeutic radionuclide specifically to the tumour site. Several low molecular weight ligands targeting the prostate-specific membrane antigen (PSMA) have been synthesized, but their pharmacokinetic properties still need to be optimized. Hereby, we describe the synthesis of new conjugates, featuring the cleavable linkers Gly-Tyr-Lys (GYK) and Met-Val-Lys (MVK), to reduce the dose delivered to the kidneys. Compounds were synthesized by solid-phase peptide synthesis (SPPS) and obtained in greater than 95% chemical purity. Radiolabelling was performed with both In-111 and Lu-177 to validate potential use of the compounds as both imaging and therapeutic agents. Radiochemical purity greater than 80% was obtained for both nuclides, but significant radiolysis was observed for the methionine-containing analogue. The results obtained thus far with the GYK-PSMA conjugate could warrant further biological investigations.
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