Biochemical pharmacology of nonsteroidal anti-inflammatory drugs

Aspirin and conventional nonsteroidal anti-inflammatory drugs are nonselective inhibitors of cyclooxygenase-1 (COX-1) and COX-2 enzymes. Two classes of selective COX-2 inhibitors: (1) sulfonamides, such as L-745,337, and (2) tricyclic methyl sulfone derivatives, such as SC58125, have been developed....

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Bibliographic Details
Published in:Biochemical pharmacology 1998-03, Vol.55 (5), p.543-547
Main Author: WU, K. K.-Y
Format: Article
Language:English
Subjects:
Animals
Anti-Inflammatory Agents, Non-Steroidal - pharmacology
aspirin
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
colon cancer
cyclooxygenase
Cyclooxygenase Inhibitors - pharmacology
Humans
inflammation
Isoenzymes - antagonists & inhibitors
Medical sciences
nonsteroidal anti-inflammatory drugs
Pharmacology. Drug treatments
salicylate effect on NF-KB
Salicylates - pharmacology
Salicylic Acid
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Summary:Aspirin and conventional nonsteroidal anti-inflammatory drugs are nonselective inhibitors of cyclooxygenase-1 (COX-1) and COX-2 enzymes. Two classes of selective COX-2 inhibitors: (1) sulfonamides, such as L-745,337, and (2) tricyclic methyl sulfone derivatives, such as SC58125, have been developed. X-ray crystal structures of COX-1 and COX-2 have provided valuable information regarding the structural basis for their COX-2 selectivity. These compounds have less gastrointestinal complications in animal experiments. Their clinical efficacy and side-effects are being evaluated. Salicylate has very weak activity against either COX isoform and yet possesses anti-inflammatory actions. Recent studies indicate that it suppresses the expression of genes involved in inflammation. These activities may provide a plausible explanation for the pharmacological dilemma and, furthermore, may represent novel mechanisms for controlling inflammation.
ISSN:0006-2952
1873-2968
DOI:10.1016/S0006-2952(97)00342-0