Search Results - "Kozono, Toshiro"
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Factor VIIa inhibitors: Target hopping in the serine protease family using X-ray structure determination
Published in Bioorganic & medicinal chemistry (15-08-2008)“…We succeeded in target hopping in the serine protease family using crystal structures of human FVIIa/TF in complex with peptide mimetic inhibitors. Selective…”
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Design and Synthesis of Peptidomimetic Factor VIIa Inhibitors
Published in Chemical & Pharmaceutical Bulletin (01-01-2010)“…Selective factor VIIa-tissue factor complex (FVIIa/TF) inhibition is regarded as a promising target for developing new anticoagulant drugs. In previous…”
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Structure-based design of P3 moieties in the peptide mimetic factor VIIa inhibitor
Published in Biochemical and biophysical research communications (11-02-2005)“…Selective factor VIIa-tissue factor complex (FVIIa/TF) inhibition is seen as a promising target for developing new anticoagulant drugs. Structure-based designs…”
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Novel interactions of large P3 moiety and small P4 moiety in the binding of the peptide mimetic factor VIIa inhibitor
Published in Biochemical and biophysical research communications (28-01-2005)“…Selective factor VIIa-tissue factor complex (FVIIa/TF) inhibition is seen as a promising target for developing new anticoagulant drugs. A novel peptide mimetic…”
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Design and Synthesis of N-terminal Cyclic Motilin Partial Peptides: A Novel Pure Motilin Antagonist
Published in Chemical & pharmaceutical bulletin (2001)“…Motilin antagonist was designed and synthesized on the basis of the structure-activity relationship analysis of porcine motilin that we reported recently. The…”
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Structure-Activity Study of Intact Porcine Motilin
Published in Chemical & pharmaceutical bulletin (01-11-1999)“…Biologically important sites on intact porcine motilin (pMTL) were explored using its partial peptides. The partial peptides were synthesized using Fmoc…”
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Discovery and structure–activity relationship of coumarin derivatives as TNF-α inhibitors
Published in Bioorganic & medicinal chemistry letters (17-05-2004)“…A series of coumarin-based TNF-α inhibitors 1 has been synthesized to establish structure–activity relationship. The discovery and structure–activity…”
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Industrial Synthesis of Maxacalcitol, the Antihyperparathyroidism and Antipsoriatic Vitamin D3 Analogue Exhibiting Low Calcemic Activity
Published in Organic process research & development (20-05-2005)“…Maxacalcitol, the 22-oxa-derivative of 1α,25-dihydroxyvitamin D3 and used currently as an antihyperparathyroidism and antipsoriatic drug, has been synthesized…”
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Crystal structure of human factor VIIa/tissue factor in complex with peptide mimetic inhibitor
Published in Biochemical and biophysical research communications (26-11-2004)“…The 3D structure of human factor VIIa/soluble tissue factor in complex with a peptide mimetic inhibitor, propylsulfonamide- d-Thr-Met- p-aminobenzamidine, is…”
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Design and efficient synthesis of 2 alpha-(omega-hydroxyalkoxy)-1 alpha,25-dihydroxyvitamin D3 Analogues, including 2-epi-ED-71 and their 20-epimers with HL-60 cell differentiation activity
Published in Journal of organic chemistry (29-10-2004)“…A concise and efficient synthetic approach to 2 alpha-(omega-hydroxyalkoxy)-1 alpha,25-dihydroxyvitamin D(3) (4a-c), including 2-epi-ED-71, was developed…”
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Discovery and structure-activity relationship of coumarin derivatives as TNF-α inhibitors
Published in Bioorganic & medicinal chemistry letters (17-05-2004)“…The discovery and structure-activity relationship of a novel series of coumarin-based TNF-alpha inhibitors is described. Starting from the initial lead 1a,…”
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Design and Synthesis of Novel Tetra-Peptide Motilin Agonists
Published in Bioorganic & medicinal chemistry (01-06-2002)“…A series of novel tetra-peptide motilin agonists, having the general structure H-Phe-Val-X-Ile-NH 2, were designed, on the basis of structure–activity…”
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Design and Synthesis of Motilin Antagonists Derived from the [1−4] Fragment of Porcine Motilin
Published in Journal of medicinal chemistry (31-01-2002)“…A series of cyclic peptides having the general structure H-Phe-c[-Nε-Lys-X-NH-(CH2) n -CO-] were designed on the basis of structure−activity relationship…”
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Design and Synthesis of N-terminal Cyclic Motilin Partial Peptides
Published in Chemical & pharmaceutical bulletin (01-01-2001)“…Motilin antagonist was designed and synthesized on the basis of the structure-activity relationship analysis of porcine motilin that we reported recently. The…”
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Structure of human factor VIIa/tissue factor in complex with a peptide-mimetic inhibitor: high selectivity against thrombin by introducing two charged groups in P2 and P4
Published in Acta crystallographica. Section F, Structural biology and crystallization communications (01-02-2005)“…The crystal structure of human factor VIIa/soluble tissue factor (FVIIa/sTF) in complex with a highly selective peptide‐mimetic FVIIa inhibitor which shows…”
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Synthesis and biological activity of KCB-328 and its analogues: Novel class III antiarrhythmic agents with little reverse frequency dependence
Published in Bioorganic & medicinal chemistry letters (04-01-1999)“…A series of 3,4-dimethoxyphenethylamine derivatives was prepared, and their prolongation effects on effective refractory period of contractile response (ERPc)…”
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Flat revertant inducers, styryl diphenylamine derivatives, inhibit growth and metastasis of murine tumor cells in vivo
Published in Anticancer research (01-01-1997)“…Previously, we reported that a novel styryl diphenylamine derivative, RX-465, reverts the transformed phenotype of human fibrosarcoma HT1080 cells in vitro. To…”
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