Title : The kinetic factors that determine the affinity and selectivity for slow binding inhibition of human prostaglandin H synthase 1 and 2 by indomethacin and flurbiprofen.

Pub. Date : 1996 Feb 16

PMID : 8631960






3 Functional Relationships(s)
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1 The KI values associated with the formation of the first reversible complex (EI) for flurbiprofen with PGHS1 and PGHS2 were 0.53 +/- 0. Flurbiprofen prostaglandin-endoperoxide synthase 1 Homo sapiens
2 These results show that the overall affinity for the inhibition of PGHS1 versus PGHS2 was 30-fold greater for indomethacin (KI* = 0.032 +/- 0.005 and 1.02 +/- 0.08 microM, respectively) and 3-fold greater for flurbiprofen (KI* = 0.017 +/- 0.002 and 0.045 +/- 0.004 microM, respectively). Flurbiprofen prostaglandin-endoperoxide synthase 1 Homo sapiens
3 The results also show that for both PGHS1 and PGHS2, flurbiprofen was bound tighter to the initial EI complex than indomethacin; however, the rate of dissociation from EI* was slower for indomethacin than flurbiprofen. Flurbiprofen prostaglandin-endoperoxide synthase 1 Homo sapiens