In vitro and in vivo characterization of novel 18F-labeled bombesin analogues for targeting GRPR-positive tumors

Mu, Linjing; Honer, Michael; Becaud, Jessica; Martic, Miljen; Schubiger, Pius A; Ametamey, Simon M; Stellfeld, Timo; Graham, Keith; Borkowski, Sandra; Lehmann, Lutz; Dinkelborg, Ludger; Srinivasan, Ananth (2010). In vitro and in vivo characterization of novel 18F-labeled bombesin analogues for targeting GRPR-positive tumors. Bioconjugate chemistry, 21(10), pp. 1864-71. Washington, D.C.: American Chemical Society 10.1021/bc100222u

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The gastrin-releasing peptide receptor (GRPR) is overexpressed on a number of human tumors and has been targeted with radiolabeled bombesin analogues for the diagnosis and therapy of these cancers. Seven bombesin analogues containing various linkers and peptide sequences were designed, synthesized, radiolabeled with (18)F, and characterized in vitro and in vivo as potential PET imaging agents. Binding studies displayed nanomolar binding affinities toward human GRPR for all synthesized bombesin analogues. Two high-affinity peptide candidates 6b (K(i) = 0.7 nM) and 7b (K(i) = 0.1 nM) were chosen for further in vivo evaluation. Both tracers revealed specific uptake in GRPR-expressing PC-3 tumors and the pancreas. Compared to [(18)F]6b, compound [(18)F]7b was characterized by superior tumor uptake, higher specificity of tracer uptake, and more favorable tumor-to-nontarget ratios. In vivo PET imaging allowed for the visualization of PC-3 tumor in nude mice suggesting that [(18)F]7b is a promising PET tracer candidate for the diagnosis of GRPR-positive tumors in humans.

Item Type:	Journal Article (Original Article)
Division/Institute:	04 Faculty of Medicine > Department of Intensive Care, Emergency Medicine and Anaesthesiology (DINA) > Clinic and Policlinic for Anaesthesiology and Pain Therapy
UniBE Contributor:	Lehmann, Lutz Eric
ISSN:	1043-1802
Publisher:	American Chemical Society
Language:	English
Submitter:	Jeannie Wurz
Date Deposited:	04 Oct 2013 14:08
Last Modified:	05 Dec 2022 14:00
Publisher DOI:	10.1021/bc100222u
PubMed ID:	20857927
Web of Science ID:	000283101000020
URI:	https://boris.unibe.ch/id/eprint/557 (FactScience: 199730)