Inhibitors of PGHS-2Transactivator activity

摘要

Prostaglandin-endoperoxide H synthase (PGHS-2) converts arachidonic acid to prostaglandin H2. PGHS-2 is an inducible gene product undetectable in most normal human tissues, but abundant in cancer cells. The present invention exploits a previously undisclosed transcriptional function of PGHS-2 distinct from its well-established enzymatic role to identify potential therapeutic agents useful in treating cancer. The method comprises a DNA binding assay in which PGHS-2 protein binding to the C/EBP, CRE and NF-&kgr;B regions of the PGHS-2 promoter in the presence and absence of test compounds is evaluated to identify inhibitors of PGHS-2 transactivation activity.