Bacithrocins A, B and C, novel thrombin inhibitors.
Novel thrombin inhibitors, bacithrocins A, B and C, have been isolated from the culture broth of Bacillus laterosporus Laubach NR 2988. The structures of these inhibitors have been determined to be N-acyl-L-phenylalanyl-DL-arginal by the 2D-NMR experiments on their oxidation products and by amino acid analysis. Bacithrocin A inhibits thrombin, factor Xa and trypsin with IC50s of 48, 13 and 0.65 microM, respectively, which are similar to those of bacithrocins B and C. Bacithrocins prolong the clotting time induced by thrombin and factor Xa.
Kamiyama
T
T
Nippon Roche Research Center, Kanagawa, Japan.
Umino
T
T
Nakamura
Y
Y
Itezono
Y
Y
Sawairi
S
S
Satoh
T
T
Yokose
K
K
D000595:Amino Acid Sequence; D001407:Bacillus / Q000378:metabolism*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004151:Dipeptides / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D065427:Factor Xa Inhibitors; D005285:Fermentation; D009682:Magnetic Resonance Spectroscopy; D008969:Molecular Sequence Data; D015394:Molecular Structure; D010206:Papain / Q000037:antagonists & inhibitors; D016339:Spectrometry, Mass, Fast Atom Bombardment; D013917:Thrombin / Q000037:antagonists & inhibitors*; D014361:Trypsin Inhibitors
D004151:Dipeptides; D065427:Factor Xa Inhibitors; D014361:Trypsin Inhibitors; C089887:bacithrocin A; C089888:bacithrocin B; C089889:bacithrocin C; D013917:Thrombin; D010206:Papain