Ellen Sandor & (art)n

The COX2 protein structure using cylinders to represent the alpha-helices which are connected by loops having less regular structure. The protein has three major domains, here colored green (the egf or epidermal growth factor domain), orange (the membrane domain) and red (the catalytic domain). Embedded in the catalytic domain are a heme molecule (grey spheres) and a drug molecule acting to inhibit this enzyme. The drug is colored purple, with several atoms colored red (oxygen), blue (nitrogen) and yellow (sulphur). The drug is surrounded by a dot surface indicating how it might enter into the enzyme through the membrane domain of the protein. Finally, one of the tyrosine amino acids in the catalytic domain is shown between the heme and the inhibitor. This tyrosine is crucial to the catalytic enzymatic activity of this protein. The protein is known as COX2 or cyclo-oxygenase 2. Monsanto is developing drugs which inhbit this enzyme. These drugs act as anti-inflammatory drugs, like aspirin but without the gastro-intenstinal side-effects. Some steroids, such as cortisone have been used as anti-inflammatory drugs, but have undesirable side effects. But new, selective COX2 inhibitors are not steroids and they do not have the gastro-intenstinal side-effects of older drugs such as aspirin, ibuprofen or naproxen. These drugs are new members of an important class of drugs called non-steroidal anti-inflammatory drugs, or NSAIDs. All NSAIDs have analgesic, anti-inflammatory and antipyretic activity. They share a joint mechanism of action–blockage of the enzyme cyclo-oxygenase which is involved in the metabolism of arachidonic acid to prostaglandins. Arachidonic acid is released from membrane phospholipids in response to inflammatory stimuli.