Digitale Medien
Palo Alto, Calif.
:
Annual Reviews
Annual Review of Biophysics and Biomolecular Structure
32 (2003), S. 183-206
ISSN:
1056-8700
Quelle:
Annual Reviews Electronic Back Volume Collection 1932-2001ff
Thema:
Biologie
,
Physik
Notizen:
Abstract Cyclooxygenases-1 and -2 (COX-1 and COX-2, also known as prostaglandin H2 synthases-1 and -2) catalyze the committed step in prostaglandin synthesis. COX-1 and -2 are of particular interest because they are the major targets of nonsteroidal antiinflammatory drugs (NSAIDs) including aspirin, ibuprofen, and the new COX-2-selective inhibitors. Inhibition of the COXs with NSAIDs acutely reduces inflammation, pain, and fever, and long-term use of these drugs reduces the incidence of fatal thrombotic events, as well as the development of colon cancer and Alzheimer's disease. In this review, we examine how the structures of COXs relate mechanistically to cyclooxygenase and peroxidase catalysis and how alternative fatty acid substrates bind within the COX active site. We further examine how NSAIDs interact with COXs and how differences in the structure of COX-2 result in enhanced selectivity toward COX-2 inhibitors.
Materialart:
Digitale Medien
URL:
http://dx.doi.org/10.1146/annurev.biophys.32.110601.141906
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