Aug 25, 2020 · In this study, we evaluated if the Met-Val-Lys (MVK) linker could be used to lower kidney uptake of 68 Ga-labeled DOTA-conjugated peptides and peptidomimetics.

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 …

May 1, 2020 · Methods: The DOTA conjugated linker (DOTA-AmBz-MVK(Ac)-OH; AmBz: 4-aminomethylbenzoyl), the expected cleaved metabolite DOTA-AmBz-Met-OH, and a PSMA-targeting ligand DOTA-AmBz-MVK(HTK01166)-OH were synthesized on solid-phase using standard Fmoc chemistry.

In this review, we will review established and emerging strategies that can be used to mitigate radiation-induced nephrotoxicity, with a focus on the development and incorporation of cleavable linkers for radiopharmaceutical designs.

[68 Ga]Ga-DOTA-AmBz-MVK(HTK01166)-OH retained its PSMA-targeting capability and was also cleaved by NEP. It appears that MVK can be a promising cleavable linker for use to reduce kidney uptake of radiolabeled DOTA-conjugated peptides and peptidomimetics.

Aug 25, 2020 · In this study, we evaluated if the Met-Val-Lys (MVK) linker could be used to lower kidney uptake of 68 Ga-labeled DOTA-conjugated peptides and peptidomimetics.

Sep 1, 2022 · Affinity of the radioligands to PSMA and cellular uptake and internalization was investigated using PSMA-positive PC-3 PIP and PSMA-negative PC-3 flu tumor cells.

Aug 25, 2020 · In this study, we evaluated if the Met-Val-Lys (MVK) linker could be used to lower kidney uptake of ⁶⁸Ga-labeled DOTA-conjugated peptides and peptidomimetics.

In this study, we evaluated if the Met-Val-Lys (MVK) linker could be used to lower kidney uptake of 68Ga-labeled DOTA-conjugated peptides and peptidomimetics. A model compound, [68Ga]Ga-DOTA-AmBz-MVK(Ac)-OH (AmBz: aminomethylbenzoyl), and its derivative, [68Ga]Ga-DOTA-AmBz-MVK(HTK01166)-OH, coupled with the PSMA (prostate-specific membrane

High kidney uptake is a common feature of peptide-based radiopharmaceuticals, leading to reduced detection sensitivity for lesions adjacent to kidneys and lower maximum tolerated therapeutic dose. In this study, we evaluated if the Met-Val-Lys (MVK) linker ...