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COX-2 Selectivity and Inflammatory Processes.

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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

DOI: http://dx.doi.org/10.2174/0929867003374255

Publication date: November 1, 2000

More about this publication?
  • 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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