Universität zu Köln

Feni, Lucia, Omrane, M. Aymen, Fischer, Moritz, Zlatopolskiy, Boris D., Neumaier, Bernd ORCID: 0000-0001-5425-3116 and Neundorf, Ines ORCID: 0000-0001-6450-3991 (2017). Convenient Preparation of F-18-Labeled Peptide Probes for Potential Claudin-4 PET Imaging. Pharmaceuticals, 10 (4). BASEL: MDPI. ISSN 1424-8247

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Abstract

Since pancreatic cancer is often diagnosed in a late state of cancer development, diagnostic opportunities allowing early disease detection are highly sought after. As such, cancer expression of claudin proteins is markedly dysregulated, making it an attractive target for molecular imaging like positron emission tomography (PET). Claudins are a family of transmembrane proteins that have a pivotal role as members of the tight junctions. In particular, claudin-3 and claudin-4 are frequently overexpressed in pancreatic cancer. F-18-Labeled claudin selective peptides would provide access to a novel kind of imaging tools for pancreatic cancer. In this work we describe the synthesis of the first F-18-labeled probes potentially suitable for PET imaging of claudin-4 expression. These probes were prepared using oxime ligation of 5-[F-18]fluoro-5-deoxyribose (5-[F-18]FDR) to claudin selective peptides. As a proof-of-principle, one of them, 5-[F-18]FDR-Clone 27, was isolated in >98% radiochemical purity and in 15% radiochemical yield (EOB) within 98 min, and with a molar activity of 4.0 GBq/mu mol (for 30 MBq of tracer). Moreover, we present first biological data for the prepared 5-FDR-conjugates. These tracers could pave the way for an early diagnosis of pancreatic tumor, and thus improve the outcome of anticancer therapy.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Feni, Lucia UNSPECIFIED UNSPECIFIED UNSPECIFIED Omrane, M. Aymen UNSPECIFIED UNSPECIFIED UNSPECIFIED Fischer, Moritz UNSPECIFIED UNSPECIFIED UNSPECIFIED Zlatopolskiy, Boris D. UNSPECIFIED UNSPECIFIED UNSPECIFIED Neumaier, Bernd UNSPECIFIED orcid.org/0000-0001-5425-3116 UNSPECIFIED Neundorf, Ines UNSPECIFIED orcid.org/0000-0001-6450-3991 UNSPECIFIED
URN:	urn:nbn:de:hbz:38-208750
DOI:	10.3390/ph10040099
Journal or Publication Title:	Pharmaceuticals
Volume:	10
Number:	4
Date:	2017
Publisher:	MDPI
Place of Publication:	BASEL
ISSN:	1424-8247
Language:	English
Faculty:	Faculty of Mathematics and Natural Sciences
Divisions:	Faculty of Mathematics and Natural Sciences > Department of Chemistry > Institute of Biochemistry
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language TIGHT JUNCTION STRANDS; PANCREATIC-CANCER; OXIME LIGATION; TOMOGRAPHY; EXPRESSION; PROTEIN; CARCINOMA; DIAGNOSIS; BIOCONJUGATION; RESONANCE Multiple languages Pharmacology & Pharmacy Multiple languages
Refereed:	Yes
URI:	http://kups.ub.uni-koeln.de/id/eprint/20875