The development of COX2 inhibitors.
Aspirin, arguably the world's favourite drug, has been around since the late nineteenth century, but it wasn't until the late 1970s that its ability to inhibit prostaglandin production by the cyclooxygenase enzyme was identified as the basis of its therapeutic action. Early hints of a second form of the cyclooxygenase that was differentially sensitive to other aspirin-like drugs ultimately ushered in an exciting era of drug discovery, culminating in the introduction of an entirely new generation of anti-inflammatories. This article reviews the story of this discovery and looks at the future of cyclooxygenase pharmacology.
Flower
Rod J
RJ
Department of Biochemical Pharmacology, The William Harvey Research Institute, Queen Mary University of London, Charterhouse Square, London EC1M 6BQ, UK. r.j.flower@mds.qmul.ac.uk
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000494:pharmacology*; D015195:Drug Design; D006801:Humans; D007527:Isoenzymes / Q000378:metabolism* / Q000502:physiology; D008565:Membrane Proteins; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism* / Q000502:physiology; D013329:Structure-Activity Relationship
D000894:Anti-Inflammatory Agents, Non-Steroidal; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D008565:Membrane Proteins; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; C496511:PTGS1 protein, human; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases