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PMID: 8114674 Published · ppublish English Journal Article

Overexpression of human prostaglandin G/H synthase-1 and -2 by recombinant vaccinia virus: inhibition by nonsteroidal anti-inflammatory drugs and biosynthesis of 15-hydroxyeicosatetraenoic acid.

Molecular pharmacology ·Vol. 45 ·No. 2 ·1994-02-00 ·Pages 245-54

O'Neill GP, Mancini JA, Kargman S, Yergey J, Kwan MY, Falgueyret JP, Abramovitz M, Kennedy BP, Ouellet M, Cromlish W

Abstract

Human prostaglandin G/H synthase (hPGHS)-1 and hPGHS-2, key enzymes in the formation of prostanoids from arachidonic acid, were expressed at high levels in COS-7 cells using a T7 RNA polymerase/vaccinia virus expression system. The open reading frame of hPGHS-2 cloned into vaccinia virus without its natural 5' and 3' untranslated regions directed only low levels of hPGHS-2 enzyme activity in COS-7 cells. High-level hPGHS-2 expression was achieved by appending the 3' untranslated region of hPGHS-1 to the hPGHS-2 open reading frame, with subsequent expression of the hybrid mRNA using vaccinia virus. Enzymatically active recombinant hPGHS-1 and hPGHS-2 were present as glycosylated proteins in the microsomal fraction prepared from infected cells, whereas recombinant hPGHS-1 and hPGHS-2 prepared from the microsomal fraction of cells treated with tunicamycin, an inhibitor of N-linked glycosylation, were enzymatically inactive. The major prostanoid products formed by microsomes from COS-7 cells containing either recombinant hPGHS-1 or hPGHS-2 after incubation with arachidonic acid were prostaglandin D2 and E2, with lower levels of prostaglandin F2 alpha and 6-keto-prostaglandin F1 alpha. A range of potencies were observed for various nonsteroidal anti-inflammatory drugs as inhibitors of prostaglandin E2 synthesis by hPGHS-1 and hPGHS-2. Recombinant hPGHS-1 and hPGHS-2 both produced 15- and 11-hydroxyeicosatetraenoic acid (HETE) from arachidonic acid, with 15-HETE production by hPGHS-2 being stimulated 5-fold by preincubation with aspirin. Chiral phase high performance liquid chromatography analysis showed that aspirin-treated hPGHS-2 produced 15(R)-HETE, with no detectable 15(S)-HETE.

MeSH Terms
Animals Anti-Inflammatory Agents, Non-Steroidal/pharmacology Arachidonic Acid/pharmacology Aspirin/pharmacology Base Sequence Cell Line Chromatography, High Pressure Liquid Cloning, Molecular Electrophoresis, Polyacrylamide Gel Humans Hydroxyeicosatetraenoic Acids/biosynthesis Immunoblotting Microsomes/drug effects Molecular Sequence Data Prostaglandin-Endoperoxide Synthases/biosynthesis,metabolism Recombinant Proteins/biosynthesis Vaccinia virus/immunology,metabolism
Chemicals
Anti-Inflammatory Agents, Non-Steroidal Hydroxyeicosatetraenoic Acids Recombinant Proteins Arachidonic Acid 15-hydroxy-5,8,11,13-eicosatetraenoic acid Prostaglandin-Endoperoxide Synthases Aspirin
Authors & Affiliations
10 authors, click to expand affiliations / ORCID
O'Neill G P
Department of Pharmacology, Merck Frosst Centre for Therapeutic Research, Pointe Claire-Dorval, Quebec, Canada.
Mancini J A
Kargman S
Yergey J
Kwan M Y
Falgueyret J P
Abramovitz M
Kennedy B P
Ouellet M
Cromlish W
Article Info
Journal
Molecular pharmacology
Abbr.
Mol Pharmacol
ISSN
0026-895X
Published
1994-02-00
Pages
245-54
Language
English
Region
United States
NLM ID
0035623
Subset
IM
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