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Synthesis, in vitro evaluation, and 68 Ga‐radiolabeling of CDP 1 toward PET / CT imaging of bacterial infection
Author(s) -
Dutta Jyotibon,
Baijnath Sooraj,
Somboro Anou M.,
Nagiah Savania,
Albericio Fernando,
Torre Beatriz G.,
MarjanovicPainter Biljana,
Zeevaart Jan Rijn,
Sathekge Mike,
Kruger Hendrik G.,
Chuturgoon Anil,
Naicker Tricia,
Ebenhan Thomas,
Govender Thavendran
Publication year - 2017
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12980
Subject(s) - antimicrobial , cathelicidin , peptide , antimicrobial peptides , in vitro , bacteria , chemistry , chelation , microbiology and biotechnology , biochemistry , biology , genetics , organic chemistry
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 LL 37, 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‐ CDP 1 showed bacterial selectivity and low affinity toward hepatic cells, which are favorable characteristics for further preclinical application.