Abstract
Chemokines and chemokine receptors have been recognized as critical signal components that maintain the physiological functions of various cells, particularly the immune cells. The signals of chemokines/chemokine receptors guide various leukocytes to respond to inflammatory reactions and infectious agents. Many chemokine receptors play supportive roles in the differentiation, proliferation, angiogenesis, and metastasis of diverse tumor cells. In addition, the signaling functions of a few chemokine receptors are associated with cardiac, pulmonary, and brain disorders. Over the years, numerous promising molecules ranging from small molecules to short peptides and antibodies have been developed to study the role of chemokine receptors in healthy states and diseased states. These drug-like candidates are in turn exploited as radiolabeled probes for the imaging of chemokine receptors using noninvasive in vivo imaging, such as positron emission tomography (PET). Recent advances in the development of radiotracers for various chemokine receptors, particularly of CXCR4, CCR2, and CCR5, shed new light on chemokine-related cancer and cardiovascular research and the subsequent drug development. Here, we present the recent progress in PET radiotracer development for imaging of various chemokine receptors.
Highlights
Chemokines are biologically active peptides whose primary function is to induce cell migration
This review is intended to provide an overview of the development of various positron emission tomography (PET) radiotracers for imaging of chemokine receptors involved in cancer and cardiovascular and pulmonary disorders
Of the radiotracers developed for chemokine receptors far, the majority of them are based on peptides and cyclam chelator moieties, and only a few of them are based on small molecules
Summary
Chemokines are biologically active peptides whose primary function is to induce cell migration. Several PET radiotracers have been developed to image different chemokine receptors in animal and human subjects. This review is intended to provide an overview of the development of various PET radiotracers for imaging of chemokine receptors involved in cancer and cardiovascular and pulmonary disorders. Of the radiotracers developed for chemokine receptors far, the majority of them are based on peptides and cyclam chelator moieties, and only a few of them are based on small molecules. Small-molecule radiotracers have gathered the least consideration compared to peptidic or chelator-functionalized radiotracers for the imaging of chemokine receptors. Radiometal labeling of a peptide or small protein that structurally mimics a chemokine should be considered where the small-molecule radiotracer fails to engage its receptor. The development of various PET radiotracers for and PET imaging of chemokine receptors at the preclinical and clinical levels are reviewed
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
