Reducing kidney uptake of radiolabelled exendin-4 using variants of the renally cleavable linker MVK.

ABSTRACT:

Background

Peptidic radiotracers are preferentially excreted through the kidneys, which often results in high persistent renal retention of radioactivity, limiting or even preventing therapeutic clinical translation of these radiotracers. Exendin-4, which targets the glucagon-like-peptide 1 receptor (GLP-1R) overexpressed in insulinomas and in congenital hyperinsulinism, is an example thereof. The use of the tripeptide MVK, which is readily cleaved between methionine and valine by neprilysin at the renal brush border membrane, already showed promising results in reducing kidney uptake as reported in the literature. Based on our previous findings we were interested how linker variants with multiple copies of the MV-motive influence renal washout of radiolabelled exendin-4.

Result

SUBMITTER: Trachsel B 

PROVIDER: S-EPMC10477158 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature