COX-2 Selectivity and Inflammatory Processes.
Abstract:Increasing amounts of experimental and clinical data support the role of selective cyclooxygenase (COX)-2 inhibition in anti-inflammatory processes and the involvement of COX-1 inhibition in the side effects associated with non steroidal anti-inflammatory drug use. This review will focus on the differences in the structure of the COX-1 and COX-2 molecules, particularly the active site and how they are bound by various NSAIDs to achieve COX-2 selectivity. This COX-2 selectivity will then be characterized in pharmacological assays in vitro and in animal models in vivo. Finally, clinical information available for this new class of selective inhibitors will be discussed.
Keywords: Acylation Site; Analgesic activity; Anti-inflamatory; Anti-pyretic activity; COX-2 selectivity; Catalytic Centre; Cox-1 and COX-2 responsible; Expression of COX-2; H-bonding Dynamics; Human Rheumatic Diseases; Ionic binding
Document Type: Review Article
Publication date: November 1, 2000
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