News

The Basis of an Inflammatory Inhibitor

Human cells have 518 protein kinases which act as signal pathways and are also responsible for disease. Tübingen scientists have developed skepinone-L, an agent which enables individual protein kinases to be selectively inhibited.

The protein kinase inhibitor Skepinone-L blocks p38 MAP-Kinase (left) and takes a selective effect (right). Diagram: Prof. Thilo Stehle

Protein kinases are promising drug targets for the new medicines of the 21st century. The human genome contains a total of 518 of these enzymes, which are responsible for passing on signals within cells. At least 244 of them play a role when it comes to disease. If a protein kinase goes wrong, it can lead to the growth of tumors or, in the case of auto-immune disorders, constant inflammation.

Until now, a lack of inhibitors with high potency and selectivity in vivo has hampered investigation of the p38 mitogen-activated protein kinase (MAPK) signaling pathway. University of Tübingen researchers have now described the design of skepinone-L, which appears to be the first ATP-competitive p38 MAPK inhibitor with excellent in vivo efficacy and selectivity. Therefore, skepinone-L is a valuable probe for chemical biology research, and it may foster the development of a unique class of kinase inhibitors.

Read the full article in Nature Chemical Biology: www.nature.com/nchembio/journal/vaop/ncurrent/full/nchembio.761.html

Contact: 

Prof. Dr. Stefan Laufer                                                 
Universität Tübingen
Mathematisch-Naturwissenschaftliche Fakultät
Pharmazeutische Chemie
Telefon + 49 7071 29-72459
stefan.laufer[at]uni-tuebingen.de

Prof. Dr. Thilo Stehle
Universität Tübingen 
Mathematisch-Naturwissenschaftliche Fakultät
Interfakultäres Institut für Biochemie
Telefon +49 7071 29-73043
thilo.stehle[at]uni-tuebingen.de

Eberhard Karls Universität Tübingen

Public Relations Department

Myriam Hönig

Director

Michael Seifert

Press Relations and

Research Reporting

Phone +49 7071 29-76789
Fax +49 7071 29-5566
Michael.seifert(at)uni-tuebingen.de
www.uni-tuebingen.de/aktuell

Please send us a copy of your article or report.