Universität zu Köln

Sitnikov, Nikolay S., Li, Yingchun, Zhang, Danfeng, Yard, Benito and Schmalz, Hans-Guenther ORCID: 0000-0003-0489-1827 (2015). Design, Synthesis, and Functional Evaluation of CO-Releasing Molecules Triggered by Penicillin G Amidase as a Model Protease. Angew. Chem.-Int. Edit., 54 (42). S. 12314 - 12319. WEINHEIM: WILEY-V C H VERLAG GMBH. ISSN 1521-3773

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Abstract

Protease-triggered CO-releasing molecules (CORMs) were developed. The viability of the approach was demonstrated through the synthesis of compounds consisting of an eta(4)-oxydiene-Fe(CO)(3) moiety connected to a penicillin G amidase (PGA)-cleavable unit through a self-immolative linker. The rate of PGA-induced hydrolysis was investigated by HPLC analysis and the subsequent CO release was quantitatively assessed through headspace gas chromatography. In an in vitro assay with human endothelial cells, typical biological effects of CO, that is, inhibition of the inflammatory response and the induction of heme oxygenase-1 expression, were observed only upon co-administration of the CORM and PGA. This work forms a promising basis for the future development of protease-specific CORMs for potential medicinal applications.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Sitnikov, Nikolay S. UNSPECIFIED UNSPECIFIED UNSPECIFIED Li, Yingchun UNSPECIFIED UNSPECIFIED UNSPECIFIED Zhang, Danfeng UNSPECIFIED UNSPECIFIED UNSPECIFIED Yard, Benito UNSPECIFIED UNSPECIFIED UNSPECIFIED Schmalz, Hans-Guenther UNSPECIFIED orcid.org/0000-0003-0489-1827 UNSPECIFIED
URN:	urn:nbn:de:hbz:38-389918
DOI:	10.1002/anie.201502445
Journal or Publication Title:	Angew. Chem.-Int. Edit.
Volume:	54
Number:	42
Page Range:	S. 12314 - 12319
Date:	2015
Publisher:	WILEY-V C H VERLAG GMBH
Place of Publication:	WEINHEIM
ISSN:	1521-3773
Language:	English
Faculty:	Faculty of Mathematics and Natural Sciences
Divisions:	Faculty of Mathematics and Natural Sciences > Department of Chemistry > Institute of Organic Chemistry
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language CARBON-MONOXIDE; ET-CORMS; TRICARBONYL COMPLEXES; BIOLOGICAL-ACTIVITIES; PRODRUGS; DELIVERY; SPACER Multiple languages Chemistry, Multidisciplinary Multiple languages
Refereed:	Yes
URI:	http://kups.ub.uni-koeln.de/id/eprint/38991