FR901451, a novel inhibitor of human leukocyte elastase from Flexibacter sp. I. Producing organism, fermentation, isolation, physico-chemical and biological properties.
A novel human leukocyte elastase (HLE) inhibitor, FR901451 was discovered in the fermentation broth of a bacteria. The bacteria was identified as Flexibacter sp. No. 758. FR901451 has a molecular weight of 1269 and a molecular formula of C60H79N13O18. The mode of inhibition against HLE is competitive, with a Ki value of 9.8 x 10(-9) M.
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
T
T
Fujita
H
H
Hatanaka
K
K
Hayashi
N
N
Shigematsu
S
S
Takase
M
M
Okamoto
M
M
Okuhara
K
K
Shimatani
A
A
Satoh
D000818:Animals; D041963:Bacteroidetes / Q000737:chemistry* / Q000648:ultrastructure; D005285:Fermentation; D006801:Humans; D019272:Leukocyte Elastase; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D008855:Microscopy, Electron, Scanning; D015394:Molecular Structure; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors*; D010456:Peptides, Cyclic / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*
C091806:FR 901451; D010456:Peptides, Cyclic; D010196:Pancreatic Elastase; D019272:Leukocyte Elastase