Dataset Information

Evaluation of Met-Val-Lys as a Renal Brush Border Enzyme-Cleavable Linker to Reduce Kidney Uptake of ⁶⁸Ga-Labeled DOTA-Conjugated Peptides and Peptidomimetics.

ABSTRACT: 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 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 antigen)-targeting motif of the previously reported HTK01166 were synthesized and evaluated to determine if they could be recognized and cleaved by the renal brush border enzymes. Additionally, positron emission tomography (PET)

SUBMITTER: Bendre S

PROVIDER: S-EPMC7503470 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature

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Dataset Information

Evaluation of Met-Val-Lys as a Renal Brush Border Enzyme-Cleavable Linker to Reduce Kidney Uptake of ⁶⁸Ga-Labeled DOTA-Conjugated Peptides and Peptidomimetics.

OmicsDI is part of the ELIXIR infrastructure

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Dataset Information

Evaluation of Met-Val-Lys as a Renal Brush Border Enzyme-Cleavable Linker to Reduce Kidney Uptake of 68Ga-Labeled DOTA-Conjugated Peptides and Peptidomimetics.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Evaluation of Met-Val-Lys as a Renal Brush Border Enzyme-Cleavable Linker to Reduce Kidney Uptake of ⁶⁸Ga-Labeled DOTA-Conjugated Peptides and Peptidomimetics.