Semin Vasc Med 2003; 03(2): 107-112
DOI: 10.1055/s-2003-40668
Copyright © 2003 by Thieme Medical Publishers, Inc., 333 Seventh Avenue, New York, NY 10001, USA. Tel.: +1(212) 584-4662

Aspirin and Other Cyclooxygenase Inhibitors: New Therapeutic Insights

Kenneth K. Wu
  • Vascular Biology Research Center and Division of Hematology, The University of Texas-Houston Health Science Center, Houston, TX
Further Information

Publication History

Publication Date:
18 July 2003 (online)


Aspirin acetylates serine-530 of cyclooxygenase-1 (COX-1), thereby blocking thromboxane A2 synthesis in platelets and reducing platelet aggregation. This mechanism of action accounts for the effect of aspirin on prevention of coronary artery and cerebrovascular thrombosis. Aspirin is less effective in inhibiting COX-2 activity, whereas celecoxib and rofecoxib selectively inhibit COX-2 activity as they contain a side chain to anchor to the side pocket of COX-2 substrate channel. Aspirin and salicylate at therapeutic concentrations inhibit COX-2 protein expression through interference with binding of CCAAT/enhancer binding protein β (C/EBPβ) to its cognate site on COX-2 promoter/enhancer. Expression of other genes, such as inducible nitric oxide synthase and interleukin-4, may be inhibited by aspirin and salicylate by a C/EBP-dependent mechanism. Aspirin at suprapharmacological concentrations inhibits NF-κB-mediated gene transcription and protects tissue from injury. These recent studies provide new insight into the pharmacological actions of aspirin and salicylate preparations and implicate C/EBPβ as a potential target for therapy of inflammation and tissue injury.


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