Article (Scientific journals)
NOTA‐PRGD2 and NODAGA‐PRGD2: Bioconjugation, characterization, radiolabelling, and design space
Salvé, Mallory; Avohou, Tonakpon Hermane; Monbaliu, Jean-Christophe et al.
2018In Journal of Labelled Compounds and Radiopharmaceuticals, 61, p. 487-500
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J Label Compd Radiopharm. 2018;61:487–500. Copyright © 2018 John Wiley & Sons, Ltd.


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Keywords :
[68Ga]Ga‐NODAGA‐PRGD2; [68Ga]Ga‐NOTA‐PRGD2; Design Space; dimeric RGD peptide; Gallium‐68; mass spectrometry; nuclear magnetic resonance; radiolabelling
Abstract :
[en] This work reports on the development of amide bond bioconjugation for the production of ‐NOTA and ‐NODAGA PRGD2 using batch strategy andmicrofluidic reactor technology. The final radiolabelling step was fully optimized using Design of Experiments and Design Space approaches, hence targeting robust labelling yields in routine. Optimal labelling conditions were defined insodium acetate buffer as 168 μg/mL peptide concentration, 4.9 pH, 47.5°C temperature, and 12.5‐minute reaction time. Upon optimization, the Gallium‐68 radiolabelling was fully automated. All the work was designed to be compliant to the GMP environment and to support the pharmaceuticalscale‐up.
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Salvé, Mallory ;  Université de Liège - ULiège > Département des sciences cliniques > Médecine nucléaire
Avohou, Tonakpon Hermane ;  Université de Liège - ULiège > Département de pharmacie > Chimie analytique
Monbaliu, Jean-Christophe  ;  Université de Liège - ULiège > Département de chimie (sciences) > CITOS
Lebrun, Pierre ;  Université de Liège - ULiège > Département de pharmacie > Chimie analytique
Lemaire, Christian ;  Université de Liège - ULiège > Centre de recherches du cyclotron
Damblon, Christian ;  Université de Liège - ULiège > Département de chimie (sciences) > Chimie biologique structurale
De Tullio, Pascal ;  Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique
Hubert, Philippe  ;  Université de Liège - ULiège > Département de pharmacie > Chimie analytique
Hustinx, Roland  ;  Université de Liège - ULiège > Département des sciences cliniques > Médecine nucléaire
Luxen, André ;  Université de Liège - ULiège > Département de chimie (sciences) > Laboratoire de chimie organique de synthèse
Language :
English
Title :
NOTA‐PRGD2 and NODAGA‐PRGD2: Bioconjugation, characterization, radiolabelling, and design space
Publication date :
12 February 2018
Journal title :
Journal of Labelled Compounds and Radiopharmaceuticals
ISSN :
0362-4803
eISSN :
1099-1344
Publisher :
John Wiley & Sons, Hoboken, United States
Volume :
61
Pages :
487-500
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 01 June 2018

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