PLA–Inhibitor (stoPLA) – New class of NSAIDs for oral and transdermal inflammation treatment
PLA2 enzymes cleave phospholipids at the sn-2-position.
They exist as secreted and cytosolic forms. The cytosolic PLA2 (cPLA2) appears to play a key role in the pathway leading to the formation of inflammatory lipid mediators such as prostaglandins, leukotrienes and platelet activating factor, thus this enzyme is instrumental in pathogenic processes causing pain and inflammation. Presently topical application of glucocorticoids constitutes the most common way in the treatment of inflammatory dermatological disorders. Unfortunately, exposure of glucocorticoids has serious side effects, like skin atrophia, which limit their use as medication for inflammatory dermatitis. stoPLA is a new class of heteroaryl-substituted acetone derivatives for the effective inhibition of cytosolic PLA2 (cPLA2). These compounds effectively interact with the synthesis of prostaglandins and leukotrienes and reduce inflammatory processes. The new heteroaryl-substituted acetone derivatives have also an excellent solubility profile and are stable against metabolic inactivation through ketogroup reduction.
Further Information: PDF
PROvendis GmbH
Phone: +49 (0)208/94105 10
Contact
Dipl.-Ing. Alfred Schillert
Media Contact
All latest news from the category: Technology Offerings
Newest articles
Lighting up the future
New multidisciplinary research from the University of St Andrews could lead to more efficient televisions, computer screens and lighting. Researchers at the Organic Semiconductor Centre in the School of Physics and…
Researchers crack sugarcane’s complex genetic code
Sweet success: Scientists created a highly accurate reference genome for one of the most important modern crops and found a rare example of how genes confer disease resistance in plants….
Evolution of the most powerful ocean current on Earth
The Antarctic Circumpolar Current plays an important part in global overturning circulation, the exchange of heat and CO2 between the ocean and atmosphere, and the stability of Antarctica’s ice sheets….