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COX-2 Selectivity and Inflammatory Processes.

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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.
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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: 2000-11-01

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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