Issue 45, 2021

Synthesis, proteolytic stability, and in vitro evaluation of DOTA conjugated p160 peptide based radioconjugates: [177Lu]Lu–DOTA–p160

Abstract

In this work, we describe the synthesis, in vitro stability, and preliminary biological evaluation of [177Lu]Lu–DOTA–p160 peptide-based radiopharmaceuticals. Our findings highlight that all DOTA–p160–peptide radioconjugates exhibit favorable proteolytic and enzymatic stability with a prolonged half-life in human plasma and serum. Cell uptake studies carried out on MCF-7 cell line revealed saturable binding of the radioconjugates in the nanomolar range, thereby demonstrating their promising potential in the imaging and therapy of breast tumors.

Graphical abstract: Synthesis, proteolytic stability, and in vitro evaluation of DOTA conjugated p160 peptide based radioconjugates: [177Lu]Lu–DOTA–p160

Supplementary files

Article information

Article type
Communication
Submitted
14 9 2021
Accepted
01 11 2021
First published
02 11 2021

Org. Biomol. Chem., 2021,19, 9849-9854

Synthesis, proteolytic stability, and in vitro evaluation of DOTA conjugated p160 peptide based radioconjugates: [177Lu]Lu–DOTA–p160

J. Kaur, K. Arroub, A. Drzezga, K. Schomäcker and S. Mathur, Org. Biomol. Chem., 2021, 19, 9849 DOI: 10.1039/D1OB01812D

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