Development and Evaluation of an ¹⁸F-Radiolabeled Monocyclam Derivative for Imaging CXCR4 Expression.

ABSTRACT: In humans, C-X-C chemokine receptor type 4 (CXCR4) is a protein that is encoded by the CXCR4 gene and binds the ligand CXCL12 (also known as SDF-1). The CXCR4-CXCL12 interaction in cancer elicits biological activities that result in tumor progression and has accordingly been the subject of significant investigation for detection and treatment of the disease. Peptidic antagonists have been labeled with a variety of radioisotopes for the detection of CXCR4, but the methodology utilizing small molecules has predominantly used radiometals. We report here the development of a ¹⁸F-radiolabeled cyclam-based small molecule radioprobe, [¹⁸F]MCFB, for imaging CXCR4 expression. The IC₅₀ value of [¹⁹F]MCFB for CXCR4 was similar to that of AMD3465 (111.3 and

SUBMITTER: Brickute D 

PROVIDER: S-EPMC6522096 | biostudies-literature | 2019 May

REPOSITORIES: biostudies-literature