Article
Functional analysis of the molecular determinants of cyclooxygenase-2 acetylation by 2-acetoxyphenylhept-2-ynyl sulfide.
Archives of biochemistry and biophysics - 1 Jan 2003
Phillip Hochgesang G, Nemeth-Cawley Jennifer F, Rowlinson Scott W, Caprioli Richard M, Marnett Lawrence J
Abstract excerpt
Selective inhibition of cyclooxygenase-2 (COX-2) leads to relief of pain and inflammation with reduced gastrointestinal side effects relative to nonsteroidal anti-inflammatory drugs. 2-Acetoxyphenylhept-2-ynyl sulfide (APHS) is a selective COX-2 inhibitor that covalently modifies the protein by acetylating Ser-530. We utilized site-directed mutants in the COX-2 active site to probe the molecular determinants of...
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