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Bioorg Med Chem Lett. 2011 Oct 1;21(19):5757-61. doi: 10.1016/j.bmcl.2011.08.017. Epub 2011 Aug 8.

Improved synthesis and biological evaluation of chelator-modified α-MSH analogs prepared by copper-free click chemistry.

Author information

1
Department of Radiology, Carver College of Medicine, The University of Iowa, 500 Newton Road, ML B180, Iowa City, IA 52242, USA.

Abstract

Radionuclide chelators (DOTA, NOTA) functionalized with a monofluorocyclooctyne group were prepared. These materials reacted rapidly and in high yield with a fully deprotected azide-modified peptide via Cu-free click chemistry under mild reaction conditions (aqueous solution, room temperature). The resulting bioconjugates bind with high affinity and specificity to their cell-surface receptor targets in vitro and appear stable to degradation in mouse serum over 3h of incubation at 37°C.

PMID:
21873053
PMCID:
PMC3171621
DOI:
10.1016/j.bmcl.2011.08.017
[Indexed for MEDLINE]
Free PMC Article

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