Development of a potent DOTA-conjugated bombesin antagonist for targeting GRPr-positive tumours

Mansi, Rosalba; Wang, Xuejuan; Forrer, Flavio; Waser, Beatrice; Cescato, Renzo; Graham, Keith; Borkowski, Sandra; Reubi, Jean Claude; Maecke, Helmut R (2011). Development of a potent DOTA-conjugated bombesin antagonist for targeting GRPr-positive tumours. European journal of nuclear medicine and molecular imaging, 38(1), pp. 97-107. Berlin: Springer 10.1007/s00259-010-1596-9

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Radiolabelled somatostatin-based antagonists show a higher uptake in tumour-bearing mouse models than agonists of similar or even distinctly higher receptor affinity. Very similar results were obtained with another family of G protein-coupled receptor ligands, the bombesin family. We describe a new conjugate, RM2, with the chelator DOTA coupled to D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH(2) via the cationic spacer 4-amino-1-carboxymethyl-piperidine for labelling with radiometals such as (111)In and (68)Ga.

Item Type:

Journal Article (Original Article)

Division/Institute:

04 Faculty of Medicine > Service Sector > Institute of Pathology

UniBE Contributor:

Waser, Beatrice; Cescato, Renzo and Reubi, Jean-Claude

ISSN:

1619-7070

Publisher:

Springer

Language:

English

Submitter:

Factscience Import

Date Deposited:

04 Oct 2013 14:08

Last Modified:

17 Mar 2015 19:09

Publisher DOI:

10.1007/s00259-010-1596-9

PubMed ID:

20717822

Web of Science ID:

000285927700015

URI:

https://boris.unibe.ch/id/eprint/708 (FactScience: 200442)

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