Synthesis, in vitro evaluation, and68Ga-radiolabeling of CDP1 toward PET/CT imaging of bacterial infection.
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 synthesizednatGa-CDP1 showed bacterial selectivity and low affinity toward hepatic cells, which are favorable characteristics for further preclinical application.
Catalysis and Peptide Research Unit, School of Health Sciences and School of Chemistry and Physics, University of KwaZulu-Natal, Durban, South Africa.
Jyotibon
J
Dutta
Catalysis and Peptide Research Unit, School of Health Sciences and School of Chemistry and Physics, University of KwaZulu-Natal, Durban, South Africa.
Sooraj
S
Baijnath
Catalysis and Peptide Research Unit, School of Health Sciences and School of Chemistry and Physics, University of KwaZulu-Natal, Durban, South Africa.
Anou M
AM
Somboro
Discipline of Medical Biochemistry, School of Laboratory Medicine and Medical Sciences, College of Health Sciences, University of KwaZulu Natal, Durban, South Africa.
Savania
S
Nagiah
Catalysis and Peptide Research Unit, School of Health Sciences and School of Chemistry and Physics, University of KwaZulu-Natal, Durban, South Africa.|School of Chemistry and Physics, University of KwaZulu-Natal, Durban, South Africa.
Fernando
http://orcid.org/0000-0002-8946-0462
F
Albericio
Catalysis and Peptide Research Unit, School of Health Sciences and School of Chemistry and Physics, University of KwaZulu-Natal, Durban, South Africa.
Beatriz G
BG
de la Torre
The South African Nuclear Energy Corporation (Necsa), Radiochemistry, Pelindaba, Brits, South Africa.|Department of Science and Technology, Preclinical Drug Development Platform, North West University, Potchefstroom, South Africa.
Biljana
B
Marjanovic-Painter
The South African Nuclear Energy Corporation (Necsa), Radiochemistry, Pelindaba, Brits, South Africa.|Department of Nuclear Medicine, University of Pretoria, Pretoria, South Africa.
Jan Rijn
JR
Zeevaart
University of Pretoria and Steve Biko Academic Hospital, Pretoria, South Africa.
Mike
M
Sathekge
Catalysis and Peptide Research Unit, School of Health Sciences and School of Chemistry and Physics, University of KwaZulu-Natal, Durban, South Africa.
Hendrik G
HG
Kruger
Discipline of Medical Biochemistry, School of Laboratory Medicine and Medical Sciences, College of Health Sciences, University of KwaZulu Natal, Durban, South Africa.
Anil
A
Chuturgoon
Catalysis and Peptide Research Unit, School of Health Sciences and School of Chemistry and Physics, University of KwaZulu-Natal, Durban, South Africa.
Tricia
T
Naicker
University of Pretoria and Steve Biko Academic Hospital, Pretoria, South Africa.
Thomas
T
Ebenhan
Catalysis and Peptide Research Unit, School of Health Sciences and School of Chemistry and Physics, University of KwaZulu-Natal, Durban, South Africa.
Thavendran
http://orcid.org/0000-0003-2511-2503
T
Govender
D000085:Acetates / Q000138:chemical synthesis / Q000737:chemistry*; D023181:Antimicrobial Cationic Peptides / Q000138:chemical synthesis / Q000737:chemistry*; D001419:Bacteria / Q000302:isolation & purification*; D001424:Bacterial Infections / Q000000981:diagnostic imaging*; D002614:Chelating Agents / Q000138:chemical synthesis / Q000737:chemistry*; D005710:Gallium Radioisotopes / Q000737:chemistry*; D056945:Hep G2 Cells; D006573:Heterocyclic Compounds, 1-Ring / Q000138:chemical synthesis / Q000737:chemistry*; D006801:Humans; D000072078:Positron Emission Tomography Computed Tomography / Q000379:methods*; D060327:Solid-Phase Synthesis Techniques; D054804:Cathelicidins
C572723:1-(1,3-carboxypropyl)-4,7-carboxymethyl-1,4,7-triazacyclononane; D000085:Acetates; D023181:Antimicrobial Cationic Peptides; D002614:Chelating Agents; D005710:Gallium Radioisotopes; D006573:Heterocyclic Compounds, 1-Ring; D054804:Cathelicidins

NODAGA
; 
PET
; CDP1; LL37; bacteria; infection; solid-phase peptide synthesis