Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents

  title={Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents},
  author={R. Kurumbail and A. Stevens and J. Gierse and J. McDonald and R. A. Stegeman and Jina Y. Pak and Daniel Gildehaus and Julie M. iyashiro and T. Penning and K. Seibert and P. Isakson and W. Stallings},
  • R. Kurumbail, A. Stevens, +9 authors W. Stallings
  • Published 1996
  • Chemistry, Medicine
  • Nature
  • PROSTAGLANDINSand glucocorticoids are potent mediators of inflammation. Non-steroidal anti-inflammatory drugs (NSAIDs) exert their effects by inhibition of prostaglandin production. The pharmacological target of NSAIDs is cyclooxygenase (COX, also known as PGH synthase), which catalyses the first committed step in arachidonic-acid metabolism1,2. Two isoforms of the membrane protein COX are known3: COX-1, which is constitu-tively expressed in most tissues, is responsible for the physiological… CONTINUE READING
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