Selective prostaglandin G/H synthase (PGHS)-2 inhibitors show greater inhibitory activities on human PGHS-2 than on murine PGHS-2 in intact cells.

Abstract:

:Excess eicosanoid formation during inflammation has been attributed to the expression of the gene coding for the inducible isoform of prostaglandin G/H synthase (PGHS-2). Human and murine PGHS-2 proteins differ in 73 out of the 604 amino acids. When comparing the inhibitory effects of a panel of PGHS-inhibitors in a whole cell human and murine PGHS-2 assay carried out under identical conditions, classical NSAIDs with the exception of aspirin and tenoxicam showed similar inhibitory effects on both human and murine PGHS-2 enzymes. However, the PGHS-2 selective inhibitors nimesulide, flosulide and NS398 showed a much greater inhibition of human PGHS-2. We suggest that these differences could be due to the genetic differences of human and murine PGHS-2.

journal_name

Inflammopharmacology

journal_title

Inflammopharmacology

authors

Berg J,Fellier H,Bodenteich A,Christoph T,Towart R

doi

10.1007/s10787-997-0020-y

subject

Has Abstract

pub_date

1997-01-01 00:00:00

pages

119-26

issue

2

eissn

0925-4692

issn

1568-5608

journal_volume

5

pub_type

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