ChemMedChem

Cover image for Vol. 12 Issue 3

Editorial Board Chairs: Antonello Mai, Rainer Metternich. Assoc. Editors: David Peralta, Scott Williams (Sr)

Impact Factor: 2.98

ISI Journal Citation Reports © Ranking: 2015: 18/59 (Chemistry Medicinal); 77/255 (Pharmacology & Pharmacy)

Online ISSN: 1860-7187

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal, ChemBioChem, Medicinal Research Reviews, Molecular Informatics

September 02, 2010

VIP: Synthesis and Evaluation of Bombesin Analogues Conjugated to Two Different Triazolyl-Derived Chelators for 99mTc Labeling

VIP: Synthesis and Evaluation of Bombesin Analogues Conjugated to Two Different Triazolyl-Derived Chelators for 99mTc Labeling

Luc Brans, Elisa García-Garayoa, Christian Schweinsberg, Veronique Maes, Harriet Struthers, Roger Schibli, and Dirk Tourwé*

Bombesin is a 14-residue peptide ligand that was initially isolated from the frog B. bombina. There are also mammalian versions of this signaling peptide that bind to their respective receptor subtypes. In addition to governing various processes in the central nervous system, bombesin receptors are overexpressed on a variety of tumor cell types. Bombesin and bombesin-like peptides have therefore proven useful as tumor markers, and radiolabeled bombesin peptides have been used in radiotherapy and as imaging tracers. However, high abdominal uptake of these peptides has hindered their effectiveness.

Tourwé and colleagues report the synthesis of bombesin analogues conjugated to triazole-based chelating groups for labeling with the 99mTc(CO)3 tracer core. These compounds do not suffer the high abdominal uptake that conventional compounds do, and thus show greater potential for both imaging and radiotherapeutic targeting of bombsin-receptor-positive tumors.

Received May 2, 2010; published online August 30, 2010, DOI: 10.1002/cmdc.201000191.

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