Forum for Science, Industry and Business

Sponsored by:     3M 
Search our Site:

 

Potent and Highly Selective Allosteric Inhibitors of PKC-zeta for the Treatment of Inflammatory Diseases and Cancer

22.05.2014

<b>Background</b> Protein kinase C zeta (PKCζ) is implicated in the development of several inflammatory diseases and a promising therapeutic target. PKCζ controls TH2 response and is important for the regulation of NF-κB transcriptional activity. Moreover, there is increasing evidence for an involvement of PKCζ in tumor development, where it controls chemoresistance and cancer–related inflammation. <b>Invention</b> Scientists of Saarland University and German University in Cairo have discovered 1,3,5-trisubstituted and 1,3,4,5-tetrasubstituted pyrazolines as a potent and selective class of allosteric PKCζ inhibitors. Several of the compounds show inhibitory activity in the nanomolar range. The compounds have an allosteric mode of action by binding the less conserved PIF pocked domain and are highly selective for the specific PKC isoform. <b>Applications</b> The present technology opens up an innovative therapeutic approach for the treatment of inflammatory diseases in which the identified compounds can serve as starting points for drug development. First experiments indicate relevance particularly for chronic obstructive pulmonary disease (COPD). <b>Advantages</b> • Innovative potent small molecules for selective PKCζ inhibition • Allosteric mode of action increases selectivity • Highly versatile scaffold for the independent optimization of four substituents • Specific targeting may contribute to fewer side effects • Potential treatment of diseases with high unmet medical need

Further information: PDF

Universität des Saarlandes Wissens- und Technologietransfer GmbH PatentVerwertungsAgentur der saarländischen Hochschulen
Phone: +49 (0)681/302-71302

Contact
Dipl.-Kfm. Axel Koch (MBA), Dr. Conny Clausen, Dr. Nicole Comtesse, Dr. Frank Döbrich

As Germany's association of technology- and patenttransfer agencies TechnologieAllianz e.V. is offering businesses access to the entire range of innovative research results of almost all German universities and numerous non-university research institutions. More than 2000 technology offers of 14 branches are beeing made accessable to businesses in order to assure your advance on the market. At www.technologieallianz.de a free, fast and non-bureaucratic access to all further offers of the German research landscape is offered to our members aiming to sucessfully transfer technologies.

info@technologieallianz.de | TechnologieAllianz e.V.
Further information:
http://www.technologieallianz.de/angebote.php?sort=sag&id=03575&lang=en
http://www.technologieallianz.de/

More articles from Technology Offerings:

nachricht New Lithium Salts of Pentafluorophenylamide Anions as Electrolytes in Lithium Ionic Batteries
18.04.2017 | TechnologieAllianz e.V.

nachricht Gratings on glass surfaces
28.03.2017 | TechnologieAllianz e.V.

All articles from Technology Offerings >>>

The most recent press releases about innovation >>>

Die letzten 5 Focus-News des innovations-reports im Überblick:

Im Focus: Can we see monkeys from space? Emerging technologies to map biodiversity

An international team of scientists has proposed a new multi-disciplinary approach in which an array of new technologies will allow us to map biodiversity and the risks that wildlife is facing at the scale of whole landscapes. The findings are published in Nature Ecology and Evolution. This international research is led by the Kunming Institute of Zoology from China, University of East Anglia, University of Leicester and the Leibniz Institute for Zoo and Wildlife Research.

Using a combination of satellite and ground data, the team proposes that it is now possible to map biodiversity with an accuracy that has not been previously...

Im Focus: Climate satellite: Tracking methane with robust laser technology

Heatwaves in the Arctic, longer periods of vegetation in Europe, severe floods in West Africa – starting in 2021, scientists want to explore the emissions of the greenhouse gas methane with the German-French satellite MERLIN. This is made possible by a new robust laser system of the Fraunhofer Institute for Laser Technology ILT in Aachen, which achieves unprecedented measurement accuracy.

Methane is primarily the result of the decomposition of organic matter. The gas has a 25 times greater warming potential than carbon dioxide, but is not as...

Im Focus: How protons move through a fuel cell

Hydrogen is regarded as the energy source of the future: It is produced with solar power and can be used to generate heat and electricity in fuel cells. Empa researchers have now succeeded in decoding the movement of hydrogen ions in crystals – a key step towards more efficient energy conversion in the hydrogen industry of tomorrow.

As charge carriers, electrons and ions play the leading role in electrochemical energy storage devices and converters such as batteries and fuel cells. Proton...

Im Focus: A unique data centre for cosmological simulations

Scientists from the Excellence Cluster Universe at the Ludwig-Maximilians-Universität Munich have establised "Cosmowebportal", a unique data centre for cosmological simulations located at the Leibniz Supercomputing Centre (LRZ) of the Bavarian Academy of Sciences. The complete results of a series of large hydrodynamical cosmological simulations are available, with data volumes typically exceeding several hundred terabytes. Scientists worldwide can interactively explore these complex simulations via a web interface and directly access the results.

With current telescopes, scientists can observe our Universe’s galaxies and galaxy clusters and their distribution along an invisible cosmic web. From the...

Im Focus: Scientists develop molecular thermometer for contactless measurement using infrared light

Temperature measurements possible even on the smallest scale / Molecular ruby for use in material sciences, biology, and medicine

Chemists at Johannes Gutenberg University Mainz (JGU) in cooperation with researchers of the German Federal Institute for Materials Research and Testing (BAM)...

All Focus news of the innovation-report >>>

Anzeige

Anzeige

Event News

Plants are networkers

19.06.2017 | Event News

Digital Survival Training for Executives

13.06.2017 | Event News

Global Learning Council Summit 2017

13.06.2017 | Event News

 
Latest News

Individualized fiber components for the world market

23.06.2017 | Physics and Astronomy

How brains surrender to sleep

23.06.2017 | Life Sciences

Can we see monkeys from space? Emerging technologies to map biodiversity

23.06.2017 | Information Technology

VideoLinks
B2B-VideoLinks
More VideoLinks >>>