Related Experiment Videos
Structural basis for selective inhibition of COX-2 by nimesulide
G F Fabiola1, V Pattabhi, K Nagarajan
1Department of Crystallography & Biophysics, University of Madras, India.
Bioorganic & Medicinal Chemistry
|January 30, 1999
Abstract:
Nimesulide 1 is a novel nonsteroidal antiinflammatory drug which inhibits the enzyme cyclooxygenase 2 (COX-2) more selectively than cyclooxygenase 1 (COX-1). Molecular modelling studies have been carried out on complexes of 1 with COX-1 and with mutants of COX-1 simulating COX-2. These indicate that the mutations I523V and S516A largely contribute to the selectivity. A comparative study with SC-558 2 has also been performed.