ORGN 398 |
| Prostaglandin H synthases (PGHS) and lipoxygenases are two classes of enzymes that play key roles in a number of biological processes. These enzymes convert arachidonic acid to compounds which are important mediators of pain and inflammation. As a result, they are important therapeutic targets for the pharmaceutical industry. However, the recent discovery that dangerous cardiovascular side effects are observed with selective PGHS-2 inhibitors demonstrates that many aspects of these enzymes are still not well understood. We are working on the synthesis of linoleic and arachidonic acid substrate analogs. The goal of these syntheses is two-fold: (a) to provide insight into the mechanism of oxygen incorporation into fatty acids by PGHS and (b) to obtain competitive inhibitors that may be used to obtain crystal structures of lipoxygenases. Such structures are eagerly anticipated as they may provide starting points to investigate the unusually large kinetic isotope effects observed for these enzymes.
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New Reactions and Methodology, Total Synthesis, Materials, Devices and Switches, Lipids, Nucleotides and Mimetics
8:00 PM-10:00 PM, Tuesday, March 27, 2007 Hyatt Regency Chicago -- Riverside Center, Poster
Sci-Mix
Division of Organic Chemistry |
