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

被引：7

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

页码：629 / 638

页数：10

共 47 条

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