Belactins A and B, new serine carboxypeptidase inhibitors produced by Actinomycete. I. Taxonomy, production, isolation and biological activities.
Belactins A and B, new inhibitors of serine carboxypeptidase were discovered in the fermentation broth of Saccharopolyspora sp. MK19-42F6. They were purified by ethyl acetate extraction, silica gel chromatography, Sephadex LH20 chromatography, Capcellpak C18 SG120 reversed phase HPLC and centrifugal partition chromatography (CPC) following their inhibitory activity against carboxypeptidase Y (CP-Y). The inhibition constants (Ki) of belactins A and B against CP-Y are 0.14 and 0.27 microM respectively. Belactins A and B have highly specific inhibitory activities for CP-Y among various peptidases, have no antimicrobial activities at 100 micrograms/ml and have low toxicities.
Murakami
S
S
Institute of Microbial Chemistry, Tokyo, Japan.
Harada
S
S
Kojima
F
F
Kinoshita
N
N
Takahashi
Y
Y
Hamada
M
M
Takeuchi
T
T
Aoyagi
T
T
D001549:Benzamides / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D002268:Carboxypeptidases / Q000037:antagonists & inhibitors*; D043402:Cathepsin A; D004305:Dose-Response Relationship, Drug; D005960:Glucosides / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D007783:Lactones / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000494:pharmacology*; D016930:Saccharopolyspora / Q000737:chemistry* / Q000145:classification
D001549:Benzamides; D005960:Glucosides; D007783:Lactones; D011480:Protease Inhibitors; C098701:belactin A; C098702:belactin B; D002268:Carboxypeptidases; D043402:Cathepsin A; C022633:serine carboxypeptidase