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SlideshowReport

Structural basis for selective inhibition of COX-2

Description

Ovine COX-1 with the nonselective NSAID flurbiprofen bound in the COX active site.

Arg120, which is important in binding the normal substrate arachidonic acid, extends behind flurbiprofen to interact with its carboxylate.

Mouse COX-2 with the selective inhibitor SC-588 bound in the COX active site.

The phenylsulfonamide group of SC-588 extends into the side pocket made accessible by Val523.

The bulkier isoleucine at this position would prevent binding of SC-588 to COX-1.
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