Reducing the Kidney Uptake of High Contrast CXCR4 PET Imaging Agents via Linker Modifications.

ABSTRACT:

Purpose

The C-X-C chemokine receptor 4 (CXCR4) is highly expressed in many subtypes of cancers, notably in several kidney-based malignancies. We synthesized, labeled, and assessed a series of radiotracers based on a previous high contrast PET imaging radiopharmaceutical [⁶⁸Ga]Ga-BL02, with modifications to its linker and metal chelator, in order to improve its tumor-to-kidney contrast ratio.

Methods

Based on the design of BL02, a piperidine-based cationic linker (BL06) and several anionic linkers (tri-Aad (BL17); tri-D-Glu (BL20); tri-Asp (BL25); and tri-cysteic acid (BL31)) were substituted for the triglutamate linker. Additionally, the DOTA chelator was swapped for a DOTAGA chelator (BL30). Each radiotracer was labeled with ⁶⁸Ga and evaluated in CXCR4

SUBMITTER: Kwon D 

PROVIDER: S-EPMC9316317 | biostudies-literature | 2022 Jul

REPOSITORIES: biostudies-literature