Universität zu Köln

Wodtke, Robert, Wodtke, Johanna, Hauser, Sandra ORCID: 0000-0001-8206-6000, Laube, Markus, Bauer, David, Rothe, Rebecca ORCID: 0000-0002-0615-1112, Neuber, Christin, Pietsch, Markus, Kopka, Klaus, Pietzsch, Jens ORCID: 0000-0002-1610-1493 and Loeser, Reik (2021). Development of an F-18-Labeled Irreversible Inhibitor of Transglutaminase 2 as Radiometric Tool for Quantitative Expression Profiling in Cells and Tissues. J. Med. Chem., 64 (6). S. 3462 - 3479. WASHINGTON: AMER CHEMICAL SOC. ISSN 1520-4804

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Abstract

The transamidase activity of transglutaminase 2 (TGase 2) is considered to be important for several pathophysiological processes including fibrotic and neoplastic tissue growth, whereas in healthy cells this enzymatic function is predominantly latent. Methods that enable the highly sensitive detection of TGase 2, such as application of radiolabeled activity-based probes, will support the exploration of the enzyme's function in various diseases. In this context, the radiosynthesis and detailed in vitro radiopharmacological evaluation of an F-18-labeled N-epsilon-acryloyllysine piperazide are reported. Robust and facile detection of the radiotracer-TGase 2 complex by autoradiography of thin layer plates and polyacrylamide gels after chromatographic and electrophoretic separation owing to irreversible covalent bond formation was demonstrated for the isolated protein, cell lysates, and living cells. By use of this radiotracer, quantitative data on the expression profile of activatable TGase 2 in mouse organs and selected tumors were obtained for the first time by autoradiography of tissue sections.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Wodtke, Robert UNSPECIFIED UNSPECIFIED UNSPECIFIED Wodtke, Johanna UNSPECIFIED UNSPECIFIED UNSPECIFIED Hauser, Sandra UNSPECIFIED orcid.org/0000-0001-8206-6000 UNSPECIFIED Laube, Markus UNSPECIFIED UNSPECIFIED UNSPECIFIED Bauer, David UNSPECIFIED UNSPECIFIED UNSPECIFIED Rothe, Rebecca UNSPECIFIED orcid.org/0000-0002-0615-1112 UNSPECIFIED Neuber, Christin UNSPECIFIED UNSPECIFIED UNSPECIFIED Pietsch, Markus UNSPECIFIED UNSPECIFIED UNSPECIFIED Kopka, Klaus UNSPECIFIED UNSPECIFIED UNSPECIFIED Pietzsch, Jens UNSPECIFIED orcid.org/0000-0002-1610-1493 UNSPECIFIED Loeser, Reik UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-582490
DOI:	10.1021/acs.jmedchem.1c00096
Journal or Publication Title:	J. Med. Chem.
Volume:	64
Number:	6
Page Range:	S. 3462 - 3479
Date:	2021
Publisher:	AMER CHEMICAL SOC
Place of Publication:	WASHINGTON
ISSN:	1520-4804
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language ACTIVITY-BASED PROBES; CHEMICAL PROBES; PET TRACERS; ENZYME; BINDING; IDENTIFICATION; MECHANISM; CALCIUM; SITES; GTP Multiple languages Chemistry, Medicinal Multiple languages
URI:	http://kups.ub.uni-koeln.de/id/eprint/58249