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cPLA2 inhibitors - Novel degradation-stable inhibitors of the cPLA2



Ref.-Nr. 4441

The cytosolic phospholipase A2 (cPLA2) is an enzyme that generates arachidonic acid by the cleavage of membrane phospholipids in response to stimuli like bacterial lipopolysaccharides. Arachidonic acid in turn is the precursor of the inflammatory mediator families of leukotrienes, prostaglandins and thromboxanes.

Thus, the cPLA2 is strongly involved in inflammatory reactions, and cPLA2-deficient mice accordingly show reduced inflammatory, allergic and anaphylactic reactions as well as reduced infarction and neurologic deficits after experimental stroke.
Previously developed inhibitors of the cPLA2 had the disadvantage of fast metabolic degradation, which only allowed topic application.

The herewith offered group of substances is more degradation stable and thus displays a novel class of cPLA2 inhibitors for systemic application in inflammatory and infectious diseases as well as other immunological disorders.

Commercial Opportunities

The cPLA2 has been identified as target for the inhibition of inflammatory immune responses. The invented substances are of high interest for any pharma company with an immunological pipeline and may constitute the first-in-class cPLA2 inhibitors for systemic application.

Keywords: Inflammation, Infektion, Degradation-stable, metabolic stability

Current Status

The invented substances have been characterized with regard to the inhibition of the cPLA2 (IC50 in the submicromolar range) and metabolic stability (tested in rat liver homogenates). The inventors are currently conducting such experiments with further, newly generated derivatives of the same inhibitor family.

On behalf of the Westfalian Wilhelms-University of Muenster, PROvendis offers access to rights for commercial use as well as the opportunity for further co-development.

In case of interest we will be pleased to inform you about the patent status.

Relevant Publications

Dennis EA, Cao J, Hsu YH, Magrioti V, Kokotos G. Phospholipase A2 enzymes: Physical structure, biological function, disease implication, chemical inhibition and therapeutic invention. Chem. Rev. 2011; 111: 6130-85.
Ghomashchi F, et al. Interfacial kinetic and binding properties of mammalian group IVB phospholipase A2 (cPLA2) and comparison with other cPLA2 isoforms. J. Biol. Chem. 2010; 285: 36100-11.

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Prof. Dr. Frank Entschladen

Prof. Dr. Frank Entschladen

Dieses Angebot


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