Belactins A and B, new serine carboxypeptidase inhibitors produced by Actinomycete. II. Physico-chemical properties, structure determinations and enzymatic inhibitory activities compared with other beta-lactone containing inhibitors.
Belactins A and B, new inhibitors of serine carboxypeptidase were discovered in the fermentation broth of Saccharopolyspora sp. MK19-42F6. The structures of belactins A and B were determined to be 4-[3-[(2-amino-5-chlorobenzoyl)amino]-1,1-dimethyl-2-oxobutyl]-3- methyl-2-oxetanone and 4-[3-[[2-(beta-glucopyranosylamino)-5-chlorobenzoyl]amino]-1,1- dimethyl-2-oxobutyl]-3-methyl-2-oxetanone respectively by various spectral analyses. Belactins A and B do not inhibit esterase or lipase at 100 micrograms/ml but have more specific inhibitory activities towards carboxypeptidase Y (CP-Y) compared with other beta-lactone-containing inhibitors, such as ebelactones A, B and esterastin.
Murakami
S
S
Institute of Microbial Chemistry, Tokyo, Japan.
Takahashi
Y
Y
Naganawa
H
H
Takeuchi
T
T
Aoyagi
T
T
D001549:Benzamides / Q000737:chemistry* / Q000302:isolation & purification; D002268:Carboxypeptidases / Q000037:antagonists & inhibitors*; D043402:Cathepsin A; D004950:Esterases / Q000187:drug effects; D005960:Glucosides / Q000737:chemistry* / Q000494:pharmacology; D007783:Lactones / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D008049:Lipase / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D011480:Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D016930:Saccharopolyspora / Q000737:chemistry
D001549:Benzamides; D005960:Glucosides; D007783:Lactones; D011480:Protease Inhibitors; C098701:belactin A; C098702:belactin B; D004950:Esterases; D008049:Lipase; D002268:Carboxypeptidases; D043402:Cathepsin A; C022633:serine carboxypeptidase