Reactome | PTGS2 dimer binds PTGS inhibitors

PTGS2 dimer binds PTGS inhibitors

Stable Identifier

R-HSA-9716836

Type

Reaction [binding]

Species

Homo sapiens

Compartment

cytosol, endoplasmic reticulum membrane

ReviewStatus

5/5

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Inhibition of PTGS2 in cells involved in inflammation, fever, and pain explains the therapeutic activity of non-specific PTGS inhibitors (flurbiprofen, diclofenac, meclofenamic acid, nimesulide, ketoprofen, ibuprofen, naproxen, ketorolac, mefenamic acid, oxaprozin, phenylbutazone, piroxicam, suprofen) which show good anti-inflammatory and analgesic efficiency. Due to their simultaneous inhibition of PTGS1, they have side effects like ulcers and upper gastrointestinal complications, as well as increased heart attack and stroke risk (Grosser et al, 2017).

Literature References

PubMed ID	Title	Journal	Year
28710775	Cyclooxygenase Inhibition: Pain, Inflammation, and the Cardiovascular System Grosser, T, Theken, KN, FitzGerald, GA	Clin Pharmacol Ther	2017
21467029	Human cyclooxygenase-2 is a sequence homodimer that functions as a conformational heterodimer Dong, L, Vecchio, AJ, Sharma, NP, Jurban, BJ, Malkowski, MG, Smith, WL	J. Biol. Chem.	2011
10966456	Cyclooxygenases: structural, cellular, and molecular biology Smith, WL, DeWitt, DL, Garavito, RM	Annu Rev Biochem	2000
8901870	Flexibility of the NSAID binding site in the structure of human cyclooxygenase-2 Luong, C, Miller, A, Barnett, J, Chow, J, Ramesha, C, Browner, MF	Nat. Struct. Biol.	1996