Aspirin-like Molecules that Covalently Inactivate Cyclooxygenase-2

Many of aspirin's therapeutic effects arise from its acetylation of cyclooxygenase-2 (COX-2), whereas its antithrombotic and ulcerogenic effects result from its acetylation of COX-1. Here, aspirin-like molecules were designed that preferentially acetylate and irreversibly inactivate COX-2. The...

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Veröffentlicht in:	Science (American Association for the Advancement of Science) 1998-05, Vol.280 (5367), p.1268-1270
Hauptverfasser:	Kalgutkar, Amit S., Crews, Brenda C., Rowlinson, Scott W., Garner, Carlos, Seibert, Karen, Marnett, Lawrence J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylation Acetylene - analogs & derivatives Acetylene - chemical synthesis Acetylene - chemistry Acetylene - pharmacology Alkynes Animals Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis Anti-Inflammatory Agents, Non-Steroidal - chemistry Anti-Inflammatory Agents, Non-Steroidal - pharmacology Aspirin Aspirin - chemistry Aspirin - pharmacology Binding Sites Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cell Division - drug effects Cell growth Cell Line Colonic Neoplasms - enzymology Colonic Neoplasms - pathology Colorectal cancer Cyclooxygenase 2 Cyclooxygenase 2 Inhibitors Cyclooxygenase inhibitors Cyclooxygenase Inhibitors - chemical synthesis Cyclooxygenase Inhibitors - chemistry Cyclooxygenase Inhibitors - pharmacology Dinoprostone - biosynthesis Drug Design Enzyme inhibitors Enzymes Health aspects Humans Indomethacin - pharmacology Inhibition Inhibitory concentration 50 Innovations Ions Isoenzymes - chemistry Isoenzymes - genetics Isoenzymes - metabolism Macrophages Macrophages - enzymology Medical research Medical sciences Membrane Proteins Mice Molecules Mutagenesis, Site-Directed Nonsteroidal anti-inflammatory agents Nonsteroidal anti-inflammatory drugs Pharmacology. Drug treatments Prostaglandin D2 - biosynthesis Prostaglandin-Endoperoxide Synthases - chemistry Prostaglandin-Endoperoxide Synthases - genetics Prostaglandin-Endoperoxide Synthases - metabolism Prostaglandins Rats Rats, Inbred Lew Sulfides Sulfides - chemical synthesis Sulfides - chemistry Sulfides - pharmacology Thromboxane B2 - biosynthesis Tumor Cells, Cultured
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