Comparison of DOTA and NODAGA as chelates for 68Ga-labelled CDP1 as novel infection PET imaging agents

被引:0
作者
A. H. Mdlophane
T. Ebenhan
B. Marjanovic-Painter
T. Govender
M. M. Sathekge
J. R. Zeevaart
机构
[1] Nuclear Medicine,Radiochemistry
[2] University of Pretoria and Steve Biko Academic Hospital,Preclinical Imaging Facility
[3] The South African Nuclear Energy Corporation (Necsa),Catalysis and Peptide Research Unit, School of Health Sciences
[4] Nuclear Medicine Research Infrastructure (NuMeRI),School of Chemistry and Physics
[5] University of KwaZulu-Natal,Department of Science and Technology, Preclinical Drug Development Platform
[6] University of KwaZulu-Natal,undefined
[7] North West University,undefined
来源
Journal of Radioanalytical and Nuclear Chemistry | 2019年 / 322卷
关键词
CDP1; NODAGA; DOTA; Ga; Antimicrobial peptides; Infection imaging; PET;
D O I
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中图分类号
学科分类号
摘要
The cathelicidin-derived peptide (CDP1) is a human antimicrobial peptide that preferentially targets bacterial membranes in response to infection. CDP1 was functionalised with NODAGA and DOTA for complexation with gallium-68 to evaluate its potential as an infection imaging tracer. The synthesis of [68Ga]Ga–NODAGA–CDP1 and [68Ga]Ga–DOTA–CDP1 were optimised for pH, molarity, incubation time and temperature, and product purification. The integrity and protein binding were investigated employing [68Ga]GaCl3 and [68Ga]Ga–DOTA–TATE as internal references. [68Ga]Ga–NODAGA–CDP1 displayed good labelling properties with higher product yield compared to [68Ga]Ga–DOTA–CDP1. In contrast, [68Ga]Ga–DOTA–CDP1 showed better stability and is the preferred candidate for an in vivo investigation.
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页码:629 / 638
页数:9
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