Effect of YM-47141, a new inhibitor produced by Flexibactor sp. Q17897, on elastase.
YM-47141, a peptidic compound recently isolated from Flexibactor sp. Q17897, strongly inhibited human leukocyte elastase (HLE) with Ki value 2.1 x 10(-7) M. Unlike other serine protease inhibitors, YM-47141 exhibited relatively weak effects on cathepsin G and alpha-chymotrypsin and its inhibitory Ki values were 9.2 x 10(-4) M and 1.3 x 10(-6) M, respectively. It had little, or no inhibitory effect on plasmin, thrombin, trypsin and kallikrein (IC50 > 10(-4) M). The inhibition of HLE by YM-47141 was reversible and of a mixed type.
Teramura
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K
Drug Serendipity Research Laboratories, Yamanouchi Pharmaceutical Co. Ltd., Tokyo, Japan.
Yasumuro
K
K
Abe
K
K
D000818:Animals; D056649:Cathepsin G; D002403:Cathepsins / Q000037:antagonists & inhibitors; D002417:Cattle; D006801:Humans; D007700:Kinetics; D019272:Leukocyte Elastase / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D010179:Pancreas / Q000201:enzymology; D010456:Peptides, Cyclic / Q000494:pharmacology*; D012697:Serine Endopeptidases; D015842:Serine Proteinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013552:Swine; D014357:Trypsin / Q000494:pharmacology
D010456:Peptides, Cyclic; D015842:Serine Proteinase Inhibitors; C097796:YM 47141; D002403:Cathepsins; D012697:Serine Endopeptidases; C534094:CTSG protein, human; D056649:Cathepsin G; D019272:Leukocyte Elastase; D014357:Trypsin