Amide Inhibitors of Human Secreted Phospholipase A2

Background

Recent studies have revealed an important role for the enzyme phospholipase A2 (PLA2) in various aspects of inflammation in the peripheral and central nervous system. PLA2 consists of a superfamily of enzymes involved in the turnover of phospholipids; their metabolic products can induce both inflammation and demyelination. Therefore, PLA2 enzymes are good candidates as drug targets for the treatment.

Technology Description

UC San Diego researchers have developed novel amide compounds for the treatment of inflammation. The new molecules are potent inhibitors of secreted PLA2 (sPLA2).

Advantages

• Potential drugs for the treatment of MS and spinal cord injuries.
  
• High degree of specificity respectively for the sPLA2.

State Of Development

This technology is offered exclusively or nonexclusively in the U.S. and/or worldwide territories. A commercial sponsor for potential future research is sought.

Related Materials

• Antonopoulou, G., Barbayianni, E., Magrioti, V., Cotton, N., Stephens, D., Constantinou-Kokotou,V., Dennis, E.A. and Kokotos, G., Structure-Activity Relationships of Natural and Non-Natural Amino Acid-Based Amide and 2-Oxoamide Inhibitors of Human Phospholipase A2 Enzymes, Bioorg.Med.Chem., 16, 10257-10269 (2008).

Patent Status