Effect of the antiallergic drug disodium cromoglycate and various derivatives on alkaline phosphatase.
Disodium cromoglycate (DSCG) inhibits alkaline phosphatase in a non-competitive manner, the enzyme undergoing a conformational change which is attenuated by the presence of calcium ions. The structurally related pyranone and benzoic acid are weak inhibitors of the enzyme and produce a similar conformational change. Coumarin does not induce any conformational change in the enzyme suggesting that the 4-oxo group in DSCG may be essential for its effect.
Ochoa de Aspuru
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Department of Biochemistry and Molecular Biology, Faculty of Pharmacy, University of Basque Country, Vitoria-Gasteiz, Spain.
Lourdes Zatón
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AM
D000469:Alkaline Phosphatase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D001565:Benzoates / Q000494:pharmacology; D019817:Benzoic Acid; D002118:Calcium / Q000378:metabolism; D002417:Cattle; D002645:Chickens; D003374:Coumarins / Q000494:pharmacology; D004205:Cromolyn Sodium / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D001728:Dicumarol / Q000494:pharmacology; D007700:Kinetics; D011487:Protein Conformation / Q000187:drug effects; D013329:Structure-Activity Relationship; D014783:Viscosity
D001565:Benzoates; D003374:Coumarins; D001728:Dicumarol; D019817:Benzoic Acid; C030123:coumarin; D000469:Alkaline Phosphatase; D004205:Cromolyn Sodium; D002118:Calcium