Yoshiyuki Okumura

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The prostaglandin (PG) EP(4) receptor subtype is expressed by peripheral sensory neurons. Although a potential role of EP(4) receptor in pain has been suggested, a limited number of selective ligands have made it difficult to explore the physiological functions of EP(4) or its potential as a new analgesic target. Here, we describe the in vitro and in vivo(More)
We studied the clinical features of 59 chronic pulmonary aspergillosis cases (aspergilloma, chronic necrotizing pulmonary aspergillosis) which we experienced in our hospital. To diagnose this disease, X-rays, sputum culture and serologic tests were mainly examined, X-ray findings were a fungus ball type in 47% of cases and thickened wall of a cavity type in(More)
The biological properties of elastase inhibitor from Aspergillus flavus (AFLEI) were investigated. AFLEI was produced at the highest rate when casamino acid was used as the nitrogen source. When a mixture of AFLEI (approx. molecular weight, 7,500) and elastase from A. flavus (approx. molecular weight, 40,000) was detected using anti-AFLEI antibody,(More)
Elastolytic and elastase inhibitory activities were investigated for 13 strains of Aspergillus fumigatus, three strains of Aspergillus flavus and three strains of Aspergillus niger. Nine of the 13 strains of A. fumigatus and all strains of A. flavus demonstrated elastase activity (more than 1 unit ml(-1)). Six of the 13 strains of A. fumigatus and all(More)
The amino acid sequence of elastase inhibitor, AFLEI, isolated from Aspergillus flavus was determined by the Edman sequencing procedure of peptides derived from digests utilizing clostripain. A molecular weight of 7,525.8 was observed by TOF-MS. AFLEI contained 68 amino acid residues and has a calculated molecular weight of 7,526.2. The search for amino(More)
A novel elastase inhibitor from Aspergillus flavus (AFLEI) was isolated, and biochemical properties of AFLEI were examined. Column chromatography using diethylaminoethyl (DE) 52-Cellulose and Sephadex G-75 was used to purify the inhibitor. The final preparation was found to be homogeneous as indicated by a single band after disc polyacrylamide gel (PAGE)(More)
An elastase inhibitor from Aspergillus fumigatus (AFUEI) was isolated, and its biochemical properties and primary structure examined. The inhibitor was purified by column chromatography using DE52 cellulose and Sephadex G-75, and was found to be homogeneous as indicated by a single band following discontinuous PAGE and SDS-PAGE. A molecular mass of 7525.1(More)
Described herein are structure-activity relationships (SARs) of 4-[5-fluoro-3-[4-(2-methyl-1H-imidazol-1-yl)benzyloxy]-phenyl]-4-methoxy-3,4,5,6-tetrahydro-2H-pyran (1, CJ-12,918), an imidazole 5-lipoxygenase (5-LO) inhibitor. When 1 was tested in preclinical studies, cataract formation was observed in rats; however, this compound was metabolized(More)
Structural modification of imidazole 5-lipoxygenase (5-LO) inhibitors for optimizing inhibitory potency, pharmacokinetic behavior and toxicity (ocular) profile led to 4-{3-[4-(2-methyl-1H-imidazol-1-yl)phenylthio]}phenyl-3,4,5,6-tetrahydro-2H-pyran-4-carboxamide (6) with no observable ocular toxicity. The orally active and safe imidazole 5-LO inhibitor 6(More)
A novel acid proteinase (Tropiase) was isolated from Candida tropicalis IFO 0589 by DE52-cellulose, and DEAE-Cosmogel column chromatographies. The purified tropiase gave a single band on disc polyacrylamide gel electrophoresis, isoelectric focusing and sodium dodecyl sulfate (SDS) polyacrylamide gel electrophoresis. The enzyme preparation had a molecular(More)