4.5 Article

A DOTA-peptide conjugate by copper-free click chemistry

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 16, Pages 4805-4807

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.06.111

Keywords

DOTA; Copper-free; Click chemistry; Peptides; Chelators; Bioconjugates

Funding

  1. University of Iowa Holden Comprehensive Cancer Center
  2. American Cancer Society
  3. Iowa Cardiovascular Interdisciplinary Research Fellowship [HL07121]

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Attachment of DOTA to a novel monofluoro-cyclooctyne facilitates bioconjugation to an azide-modified peptide via Cu-free click chemistry. The resulting conjugate was radiolabeled with (111)In to afford a potential targeted molecular imaging agent with high specific activity and an excellent radiochemical purity. (C) 2010 Elsevier Ltd. All rights reserved.

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