Inhibition of human leukocyte elastase, porcine pancreatic elastase, and chymotrypsin by elasnin and other 4-hydroxy-2-pyrones.
Elasnin and 15 related 4-hydroxy-2-pyrones have been assayed for in vitro inhibition of human leukocyte elastase, porcine pancreatic elastase, and bovine chymotrypsin. Inhibition constants for HL elastase range from 0.1 to 10 mM. The principal determinant of potency against the elastases is probably the substituent at position 3, which may account for the observed strong homology between the elastases in their inhibition by these compounds. Acetylation of the 4-hydroxy group has no effect on inhibition. The inhibition is noncovalent; there is no evidence of enzyme acylation by these pyrones.
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D002918:Chymotrypsin / Q000037:antagonists & inhibitors*; D006801:Humans; D007962:Leukocytes / Q000201:enzymology*; D010179:Pancreas / Q000201:enzymology*; D011480:Protease Inhibitors / Q000494:pharmacology*; D011714:Pyrans / Q000494:pharmacology*; D011753:Pyrones / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D011480:Protease Inhibitors; D011714:Pyrans; D011753:Pyrones; C017865:elasnin; D002918:Chymotrypsin