edoc

Molecular assembly of multifunctional ⁹⁹(m)Tc radiopharmaceuticals using "clickable" amino acid derivatives

Mindt, Thomas L. and Struthers, Harriet and Spingler, Bernhard and Brans, Luc and Tourwé, Dirk and García-Garayoa, Elisa and Schibli, Roger. (2010) Molecular assembly of multifunctional ⁹⁹(m)Tc radiopharmaceuticals using "clickable" amino acid derivatives. ChemMedChem, Vol. 5, H. 12. pp. 2026-2038.

Full text not available from this repository.

Official URL: http://edoc.unibas.ch/dok/A6006300

Downloads: Statistics Overview

Abstract

Synthetic strategies that enable the efficient and selective combination of different biologically active entities hold great promise for the development of multifunctional hybrid conjugates useful for biochemical and medical applications. Starting from side-chain-functionalized N( )-propargyl lysine derivatives, conjugates containing a ⁹⁹(m)Tc-based imaging probe for SPECT and two different moieties (e.g., tumor-targeting vectors, pharmacological modifiers, affinity tags, or second imaging probes) can be assembled using the Cu(I)-catalyzed alkyne-azide cycloaddition in efficient one-pot protocols. This strategy was successfully applied to the preparation of a ⁹⁹(m)Tc-labeled conjugate comprising a tumor-targeting peptide sequence (bombesin(7-14)) and a low-molecular-weight albumin binder, a pharmacological modifier that prolongs the blood circulation time of the conjugate. Evaluation of the conjugate in vitro and in vivo provided promising results for its use as an imaging agent for the visualization of tumors positive for the gastrin-releasing peptide receptor. The methodology presented herein provides an attractive synthetic tool for the preparation of multifunctional ⁹⁹(m)Tc-based radiopharmaceuticals with significant potential for a multitude of applications.
Faculties and Departments:03 Faculty of Medicine > Bereich Querschnittsfächer (Klinik) > Ehemalige Einheiten Querschnittsfächer (Klinik) > Radiologische Chemie (Mindt)
03 Faculty of Medicine > Departement Klinische Forschung > Bereich Querschnittsfächer (Klinik) > Ehemalige Einheiten Querschnittsfächer (Klinik) > Radiologische Chemie (Mindt)
UniBasel Contributors:Mindt, Thomas L.
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:Wiley-VCH
ISSN:1860-7179
Note:Publication type according to Uni Basel Research Database: Journal article
Related URLs:
Identification Number:
Last Modified:24 May 2013 09:13
Deposited On:26 Apr 2013 07:01

Repository Staff Only: item control page