Imaging CXCR4 Expression with Iodinated and Brominated Cyclam Derivatives.

ABSTRACT:

Purpose

CXCR4 is one of several "chemokine" receptors expressed on malignant tumors (including GBM and PCNSL) and hematopoietic stem cells. Although ⁶⁸Ga-pentixafor and ⁶⁸Ga-NOTA-NFB have been shown to effectively image CXCR4 expression in myeloma and other systemic malignancies, imaging CXCR4 expression in brain tumors has been more limited due to the blood-brain barrier (BBB) and a considerable fraction of CXCR4 staining is intracellular.

Methods

We synthesized 6 iodinated and brominated cyclam derivatives with high affinity (low nM range) for CXCR4, since structure-based estimates of lipophilicity suggested rapid transfer across the BBB and tumor cell membranes.

Results

We tested 3 iodinated and 3 brominated cyclam derivatives in several CXCR4

SUBMITTER: Zhang H 

PROVIDER: S-EPMC7497443 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature