Inhibition of (Ca2+ + Mg2+)-ATPase by carbodiimides. A structure-activity study.
Nine hydrophobic carbodiimides were synthesized and their chemical reactivities (towards acetic acid) and inhibitory capacities (towards the (Ca2+ + Mg2+)-ATPase were measured. No correlation between chemical reactivity and inhibitory efficacy emerges, but a significant effect of molecular bulk on reactivity towards the calcium-protectable carboxyl groups of the ATPase is noted: methyl-substituted compounds inhibit the enzyme in the presence of Ca2+, while aryl- or cyclohexyl-substituted compounds do not inactivate in the presence of Ca2+.
Chadwick
C C
CC
Thomas
E W
EW
D000085:Acetates; D019342:Acetic Acid; D000818:Animals; D017301:Ca(2+) Mg(2+)-ATPase; D000252:Calcium-Transporting ATPases / Q000037:antagonists & inhibitors*; D002234:Carbodiimides; D004024:Dicyclohexylcarbodiimide / Q000031:analogs & derivatives* / Q000494:pharmacology; D012519:Sarcoplasmic Reticulum / Q000201:enzymology; D013329:Structure-Activity Relationship
D000085:Acetates; D002234:Carbodiimides; D004024:Dicyclohexylcarbodiimide; D017301:Ca(2+) Mg(2+)-ATPase; D000252:Calcium-Transporting ATPases; D019342:Acetic Acid