title: FR901277, a novel inhibitor of human leukocyte elastase from Streptomyces resistomycificus. Producing organism, fermentation, isolation, physico-chemical and biological properties.
abstract: A novel human leukocyte elastase inhibitor, FR901277 was discovered in the fermentation broth of Streptomyces resistomycificus No. 7622. FR901277 has a molecular weight of 961 and a molecular formula of C47H63N9O13. The mode of inhibition is competitive, with a Ki of 1.2 x 10(-8) M. Oral administration of FR901277 at doses from 32 to 320 mg/kg significantly prevented human leukocyte elastase-induced foot edema in mice.
authors.affiliation: Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Fujie
authors.forename: Y
authors.initials: Y
authors.lastname: Shinguh
authors.forename: H
authors.initials: H
authors.lastname: Hatanaka
authors.forename: N
authors.initials: N
authors.lastname: Shigematsu
authors.forename: H
authors.initials: H
authors.lastname: Murai
authors.forename: T
authors.initials: T
authors.lastname: Fujita
authors.forename: M
authors.initials: M
authors.lastname: Yamashita
authors.forename: M
authors.initials: M
authors.lastname: Okamoto
authors.forename: M
authors.initials: M
authors.lastname: Okuhara
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D005285:Fermentation; D019272:Leukocyte Elastase; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors*; D013302:Streptomyces / Q000737:chemistry*
chemical_list: D004791:Enzyme Inhibitors; D010196:Pancreatic Elastase; D019272:Leukocyte Elastase