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Cyclooxygenase 1 (COX-1), also known as prostaglandin-endoperoxide synthase 1 (HUGO PTGS1), is an enzyme that in humans is encoded by the PTGS1 gene. [ 5 ] [ 6 ] In humans it is one of three cyclooxygenases .
COX is a common target for anti-inflammatory drugs. The most significant difference between the isoenzymes, which allows for selective inhibition, is the substitution of isoleucine at position 523 in COX-1 with valine in COX-2. The smaller Val 523 residue in COX-2 allows access to a hydrophobic side-pocket in the enzyme (which Ile 523 ...
17708 Ensembl ENSG00000198804 ENSMUSG00000064351 UniProt P00395 P00397 RefSeq (mRNA) n/a n/a RefSeq (protein) n/a NP_904330 Location (UCSC) Chr M: 0.01 – 0.01 Mb Chr M: 0.01 – 0.01 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Protein family Cytochrome c oxidase subunit I Structure of the 13-subunit oxidized cytochrome c oxidase. Identifiers Symbol COX1 or COI Pfam PF00115 ...
Structure of COX-2 inactivated by Aspirin. In the active site of each of the two enzymes, Serine 516 has been acetylated. Also visible is the salicylic acid which has transferred the acetyl group, and the heme cofactor. There are at least two different cyclooxygenase isozymes: COX-1 (PTGS1) and COX-2 (PTGS2).
COX-2 is an enzyme facultatively expressed in inflammation, and it is inhibition of COX-2 that produces the desirable effects of NSAIDs. [125] When nonselective COX-1/COX-2 inhibitors (such as aspirin, ibuprofen, and naproxen) lower stomach prostaglandin levels, ulcers of the stomach or duodenum and internal bleeding can result. [126]
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The two enzymes were renamed COX-1, referring to the original enzyme and COX-2. [5] Building on those results, scientists started focusing on selective COX-2 inhibitors. Enormous effort was spent on the development of NSAIDs between the 1960s and 1980 so there were numerous pharmacophores to test when COX-2 was discovered.
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