Synthesis, in vitro evaluation, and 68 Ga-radiolabeling of CDP1 toward PET/CT imaging of bacterial infection.
Jyotibon DuttaSooraj BaijnathAnou M SomboroSavania NagiahFernando AlbericioBeatriz G de la TorreBiljana Marjanovic-PainterJan Rijn ZeevaartMike SathekgeHendrik G KrugerAnil ChuturgoonTricia NaickerThomas EbenhanThavendran GovenderPublished in: Chemical biology & drug design (2017)
Bacterial infections are a major concern in the human health sector due to poor diagnosis and development of multidrug-resistant strains. PET/CT provides a means for the non-invasive detection and localization of the infectious foci; however, the radiotracers available are either cumbersome to prepare or their exact contribution toward the imaging is not yet established. Human antimicrobial peptides are of interest for development as PET radiotracers as they are an integral component of the immune system, non-immunogenic toward the recipient, and show selectivity toward pathogens such as bacteria. Herein we report on the potential of LL37, a human cathelicidin antimicrobial peptide, as a radiotracer for bacterial imaging. Bifunctional chelator 1,4,7-triazacyclononane,1-glutaric acid-4,7-acetic acid was utilized to functionalize the antimicrobial peptide, which in turn was capable of chelating gallium. The synthesized nat Ga-CDP1 showed bacterial selectivity and low affinity toward hepatic cells, which are favorable characteristics for further preclinical application.
Keyphrases
- pet ct
- human health
- high resolution
- positron emission tomography
- endothelial cells
- multidrug resistant
- risk assessment
- gram negative
- induced apoptosis
- induced pluripotent stem cells
- computed tomography
- oxidative stress
- drug resistant
- pseudomonas aeruginosa
- bone marrow
- cell cycle arrest
- mass spectrometry
- mesenchymal stem cells
- fluorescence imaging
- highly efficient
- cell therapy
- structural basis
- molecular dynamics
- density functional theory
- single molecule