Selective PET imaging of CXCR4 using the Al¹⁸F-labeled antagonist LY2510924.

ABSTRACT:

Background

[⁶⁸Ga]PentixaFor detects C-X-C chemokine receptor type 4 (CXCR4) overexpression in various malignancies, such as multiple myeloma and non-Hodgkin lymphomas, as well as in endocrine and inflammatory disorders. This study aimed to develop an Al¹⁸F-labeled radiotracer derived from LY2510924 for CXCR4-targeted imaging, leveraging the physical and logistical advantages of fluorine-18.

Methods

We designed a CXCR4-specific radioprobe, [¹⁸F]AlF-NOTA-SC, based on LY2510924 by incorporating a triglutamate linker and NOTA chelator to enable Al¹⁸F-labeling. The in vitro CXCR4 affinity was assessed using cell-based binding assays. Subsequently, in vivo pharmacokinetics and tumor uptake of [¹⁸F]AlF-NOTA-SC were assessed in

SUBMITTER: Spahn MA 

PROVIDER: S-EPMC11928405 | biostudies-literature | 2025 Apr

REPOSITORIES: biostudies-literature