A single amino acid difference between cyclooxygenase-1 (COX-1) and -2 (COX-2) reverses the selectivity of COX-2 specific inhibitors.

@article{Gierse1996ASA,
  title={A single amino acid difference between cyclooxygenase-1 (COX-1) and -2 (COX-2) reverses the selectivity of COX-2 specific inhibitors.},
  author={James K. Gierse and Joseph J. McDonald and Scott D. Hauser and Shaukat H. Rangwala and Carol M. Koboldt and Karen Seibert},
  journal={The Journal of biological chemistry},
  year={1996},
  volume={271 26},
  pages={
          15810-4
        }
}
Nonsteroidal anti-inflammatory drugs (NSAIDs) currently available for clinical use inhibit both COX-1 and COX-2. This suggests that clinically useful NSAIDs inhibit pro-inflammatory prostaglandins (PGs) derived from the activity of COX-2, as well as PGs in tissues like the stomach and kidney (via COX-1). A new class of compounds has recently been developed (SC-58125) that have a high degree of selectivity for the inducible form of cyxlooxygenase (COX-2) over the constitutive form (COX-1). This… CONTINUE READING

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