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

被引：5
|
作者：
Mdlophane, A. H. [1 ,2 ,3 ]
Ebenhan, T. [1 ,2 ,4 ]
Marjanovic-Painter, B. [3 ]
Govender, T. [5 ,6 ]
Sathekge, M. M. [1 ,2 ,4 ]
Zeevaart, J. R. [3 ,4 ,7 ]
机构：
[1] Univ Pretoria, Nucl Med, Crn Malherbe & Steve Biko Rd, ZA-0001 Pretoria, South Africa
[2] Steve Biko Acad Hosp, Crn Malherbe & Steve Biko Rd, ZA-0001 Pretoria, South Africa
[3] South African Nucl Energy Corp Necsa, Radiochem, Pelindaba, Bldg P1600, ZA-0240 Brits, South Africa
[4] Pelindaba, Preclin Imaging Facil, Nucl Med Res Infrastruct NuMeRI, ZA-0240 Brits, South Africa
[5] Univ KwaZulu Natal, Sch Hlth Sci, Catalysis & Peptide Res Unit, ZA-4001 Durban, South Africa
[6] Univ KwaZulu Natal, Sch Chem & Phys, ZA-4001 Durban, South Africa
[7] North West Univ, Dept Sci & Technol Preclin Drug Dev Platform, 11 Hoffman St, ZA-2520 Potchefstroom, South Africa
来源：
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY | 2019年 / 322卷 / 02期
关键词：
CDP1; NODAGA; DOTA; Ga-68; Antimicrobial peptides; Infection imaging; PET; ANTIMICROBIAL PEPTIDES; UBIQUICIDIN; ANTIBACTERIAL; COMPLEXES; TRACER; GA-68; LL-37;
D O I：
10.1007/s10967-019-06693-5
中图分类号：
O65 [分析化学];
学科分类号：
070302 ; 081704 ;
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 [Ga-68]Ga-NODAGA-CDP1 and [Ga-68]Ga-DOTA-CDP1 were optimised for pH, molarity, incubation time and temperature, and product purification. The integrity and protein binding were investigated employing [Ga-68]GaCl3 and [Ga-68]Ga-DOTA-TATE as internal references. [Ga-68]Ga-NODAGA-CDP1 displayed good labelling properties with higher product yield compared to [Ga-68]Ga-DOTA-CDP1. In contrast, [Ga-68]Ga-DOTA-CDP1 showed better stability and is the preferred candidate for an in vivo investigation.
引用
收藏
页码：629 / 638
页数：10
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