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“NOTA‐PRGD 2 and NODAGA‐PRGD 2 : Bioconjugation, characterization, radiolabelling, and design space”
Author(s) -
Salvé Mallory,
Avohou Hermane T.,
Monbaliu JeanChristophe M.,
Lebrun Pierre,
Lemaire Christian,
Damblon Christian,
Tullio Pascal,
Hubert Philippe,
Hustinx Roland,
Luxen André
Publication year - 2018
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3613
Subject(s) - bioconjugation , chemistry , labelling , combinatorial chemistry , amide , chromatography , radiochemistry , organic chemistry , biochemistry
This work reports on the development of amide bond bioconjugation for the production of ‐NOTA and ‐NODAGA PRGD 2 using batch strategy and microfluidic 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 in sodium 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 pharmaceutical scale‐up.