Startseite Effect of a spacer moiety on radiometal labelled Neurotensin derivatives
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Effect of a spacer moiety on radiometal labelled Neurotensin derivatives

  • A. Mascarin , I. E. Valverde und T. L. Mindt EMAIL logo
Veröffentlicht/Copyright: 14. Oktober 2013

Abstract

The binding sequence of the regulatory peptide Neurotensin, NT(8-13), represents a promising tumour-specific vector for the development of radiopeptides useful in nuclear oncology for the diagnosis (imaging) and therapy of cancer. A number of radiometal-labelled NT(8-13) derivatives have been reported, however, the effect of the spacer which connects the vector with the radiometal complex has yet not been investigated systematically. Because a spacer moiety can influence potentially important biological characteristics of radiopeptides, we synthesized three [DOTA(177Lu)]-X-NT(8-13) derivatives and evaluated the effect of a spacer (X) on the physico-chemical properties of the conjugate including lipophilicity, stability, and in vitro receptor affinity and cell internalization.

Received: 2012-12-13
Accepted: 2013-5-6
Published Online: 2013-10-14
Published in Print: 2013-11-1

© 2013 by Walter de Gruyter Berlin Boston

Heruntergeladen am 28.11.2025 von https://www.degruyterbrill.com/document/doi/10.1524/ract.2013.2090/html?lang=de
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