Synthesis of an Alkyne-Modified Bleomycin Disaccharide Precursor, Conversion to a F-18-Labeled Radiotracer, and Preliminary in vivo-PET Imaging Studies
Johanna Tuomela; Alejandra Verhassel; Satish Jadhav; Pasi Virta; Olof Solin; Cheng-Bin Yim; Sajal K. Maity; Tove J. Grönroos
Synthesis of an Alkyne-Modified Bleomycin Disaccharide Precursor, Conversion to a F-18-Labeled Radiotracer, and Preliminary in vivo-PET Imaging Studies
Johanna Tuomela
Alejandra Verhassel
Satish Jadhav
Pasi Virta
Olof Solin
Cheng-Bin Yim
Sajal K. Maity
Tove J. Grönroos
WILEY-V C H VERLAG GMBH
Julkaisun pysyvä osoite on:
https://urn.fi/URN:NBN:fi-fe2021042824865
https://urn.fi/URN:NBN:fi-fe2021042824865
Tiivistelmä
The bleomycins (BLMs) are known antitumor antibiotics composed of the tumoricidal and tumor seeking domains. The peptide structure of BLMs is responsible for the cytotoxicity by selective oxidative cleavage of DNA (and RNA), while the tumor cell selectivity and internalization resides in the disaccharide moiety (i.e. BLM disaccharide). This has prompted researchers to utilize BLM disaccharide and its derivatives as constituents for the selective recognition of tumor cells, which may find further applications as new tumor imaging tools or drug delivery vehicles. In the present study a high yielding synthesis of an alkyne modified BLM disaccharide precursor that may be used as a useful agent for the click conjugation, its conversion to a F-18-labeled radiotracer, and preliminary in vivo PET imaging studies of the tracer with breast cancer (MCF-7) xenograft mouse models are described.
Kokoelmat
- Rinnakkaistallenteet [19207]