Y Endo

Summary

Affiliation: University of Tokyo
Country: Japan

Publications

  1. ncbi Structure-Activity study of retinoid agonists bearing substituted dicarba-closo-dodecaborane. Relation between retinoidal activity and conformation of two aromatic nuclei
    Y Endo
    Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan
    Bioorg Med Chem Lett 11:1307-11. 2001
  2. ncbi Potent estrogen agonists based on carborane as a hydrophobic skeletal structure. A new medicinal application of boron clusters
    Y Endo
    Graduate School of Phamaceutical Sciences, University of Tokyo, Japan
    Chem Biol 8:341-55. 2001
  3. ncbi Polymethylcarborane as a novel bioactive moiety: derivatives with potent retinoid antagonistic activity
    Y Endo
    Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan
    Bioorg Med Chem Lett 10:1733-6. 2000
  4. ncbi Clarification of the binding mode of teleocidin and benzolactams to the Cys2 domain of protein kinase Cdelta by synthesis of hydrophobically modified, teleocidin-mimicking benzolactams and computational docking simulation
    Y Endo
    Graduate School of Pharmaceutical Sciences, University of Tokyo, 7 3 1, Hongo, Bunkyo ku, Tokyo 113, Japan
    J Med Chem 41:1476-96. 1998
  5. ncbi Role of the hydrophobic moiety of tumor promoters. Synthesis and activity of 2-alkylated benzolactams
    Y Endo
    Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan
    Bioorg Med Chem Lett 10:63-6. 2000
  6. ncbi Enhancing effect of tumor promoters, phorbol esters and teleocidins on nuclear receptor-mediated transcription
    H Fukasawa
    Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan
    Biol Pharm Bull 23:1414-7. 2000
  7. ncbi A receptor model for tumor promoters: rational superposition of teleocidins and phorbol esters
    A Itai
    Faculty of Pharmaceutical Sciences, University of Tokyo, Japan
    Proc Natl Acad Sci U S A 85:3688-92. 1988
  8. ncbi Oxygenated cholesterols as ligands for cytosolic-nuclear tumor promoter binding protein: yakkasteroids
    Y Endo
    Faculty of Pharmaceutical Sciences, University of Tokyo, Japan
    Biochem Biophys Res Commun 194:1529-35. 1993
  9. ncbi Synthesis, computer modeling and biological evaluation of novel protein kinase C agonists based on a 7-membered lactam moiety
    Y Endo
    Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan
    Bioorg Med Chem Lett 9:173-8. 1999
  10. ncbi [The active conformation of teleocidins: design and synthesis of new active molecules]
    Y Endo
    Faculty of Pharmaceutical Sciences, University of Tokyo, Japan
    Yakugaku Zasshi 114:464-77. 1994

Collaborators

Detail Information

Publications15

  1. ncbi Structure-Activity study of retinoid agonists bearing substituted dicarba-closo-dodecaborane. Relation between retinoidal activity and conformation of two aromatic nuclei
    Y Endo
    Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan
    Bioorg Med Chem Lett 11:1307-11. 2001
    ..The relatively planar conformation at the phenyl-N-phenyl moiety seems to play a critical role in the appearance of the biological activity...
  2. ncbi Potent estrogen agonists based on carborane as a hydrophobic skeletal structure. A new medicinal application of boron clusters
    Y Endo
    Graduate School of Phamaceutical Sciences, University of Tokyo, Japan
    Chem Biol 8:341-55. 2001
    ..However, these features of carboranes may allow another application as a hydrophobic pharmacophore in biologically active molecules that interact hydrophobically with receptors...
  3. ncbi Polymethylcarborane as a novel bioactive moiety: derivatives with potent retinoid antagonistic activity
    Y Endo
    Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan
    Bioorg Med Chem Lett 10:1733-6. 2000
    ..This is the first example of derivatives of polymethylcarborane, which resembles C60 in size, with biological activity...
  4. ncbi Clarification of the binding mode of teleocidin and benzolactams to the Cys2 domain of protein kinase Cdelta by synthesis of hydrophobically modified, teleocidin-mimicking benzolactams and computational docking simulation
    Y Endo
    Graduate School of Pharmaceutical Sciences, University of Tokyo, 7 3 1, Hongo, Bunkyo ku, Tokyo 113, Japan
    J Med Chem 41:1476-96. 1998
    ..The model explains well the remarkable difference in activity between 5 and its analogue having a bulky substituent at C-8...
  5. ncbi Role of the hydrophobic moiety of tumor promoters. Synthesis and activity of 2-alkylated benzolactams
    Y Endo
    Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan
    Bioorg Med Chem Lett 10:63-6. 2000
    ..Structure-activity results indicate that a hydrophobic substituent at the C-2 position plays a critical role in the appearance of biological activities, as in the case of substitution at C-9...
  6. ncbi Enhancing effect of tumor promoters, phorbol esters and teleocidins on nuclear receptor-mediated transcription
    H Fukasawa
    Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan
    Biol Pharm Bull 23:1414-7. 2000
    ..These results suggest this reporter system is useful for the evaluation of effects on the gene expression of various tumor promoters, including non-TPA type...
  7. ncbi A receptor model for tumor promoters: rational superposition of teleocidins and phorbol esters
    A Itai
    Faculty of Pharmaceutical Sciences, University of Tokyo, Japan
    Proc Natl Acad Sci U S A 85:3688-92. 1988
    ..Their mutual spatial arrangements are most important for biological activity...
  8. ncbi Oxygenated cholesterols as ligands for cytosolic-nuclear tumor promoter binding protein: yakkasteroids
    Y Endo
    Faculty of Pharmaceutical Sciences, University of Tokyo, Japan
    Biochem Biophys Res Commun 194:1529-35. 1993
    ..Investigation of the structure-activity relationships of yakkasteroids revealed that the structure of the side chain at the 20-position is important for the binding activity to CN-TPBP...
  9. ncbi Synthesis, computer modeling and biological evaluation of novel protein kinase C agonists based on a 7-membered lactam moiety
    Y Endo
    Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan
    Bioorg Med Chem Lett 9:173-8. 1999
    ..Computational docking simulation also indicates that the relative positions of the hydrogen-bonding sites and hydrophobic regions of the compounds are well matched to the PKC delta binding site...
  10. ncbi [The active conformation of teleocidins: design and synthesis of new active molecules]
    Y Endo
    Faculty of Pharmaceutical Sciences, University of Tokyo, Japan
    Yakugaku Zasshi 114:464-77. 1994
    ..Benzolactams become the simplest molecule reproducing the conformation and activity of teleocidin, and will be a useful tool for the study of tumor-promotion and cell differentiation...
  11. ncbi Enhancement of human papillomavirus type 18 gene expression in HeLa cells by 12-O-tetradecanoylphorbol-13-acetate, 3 beta,5 alpha-dihydroxycholestan-6-one, and cholesterol
    Y Matsushima
    Faculty of Pharmaceutical Sciences, University of Tokyo, Japan
    Biol Pharm Bull 17:1292-5. 1994
    ..Treatment of the cells with cholesterol under serum-free conditions also resulted in an apparent increase of HPV18 expression...
  12. ncbi 3 beta,5 alpha-Dihydroxycholestan-6-one exists in human blood
    M Yamaguchi
    Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan
    Biol Pharm Bull 20:1044-6. 1997
    ..The oxysterol binds specifically to phorbol ester specific binding protein in vitro, and may be an endogenous ligand of the protein...
  13. ncbi Teleocidins and benzolactams inhibit cell killing by human immunodeficiency virus type 1 (HIV-1)
    Y Endo
    Faculty of Pharmaceutical Sciences, University of Tokyo, Japan
    Biol Pharm Bull 17:1147-9. 1994
    ..Teleocidin B-4 and structurally related synthetic benzolactams were found to be potent inhibitors of cell killing by HIV-1. One of the benzolactams, (-)-BL-V8-310, showed a high selectivity index...
  14. ncbi Alpha-glucosidase inhibitors with a 4,5,6,7-tetrachlorophthalimide skeleton pendanted with a cycloalkyl or dicarba-closo-dodecaborane group
    S Sou
    Institute of Molecular and Cellular Biosciences, University of Tokyo, Japan
    Chem Pharm Bull (Tokyo) 49:791-3. 2001
    ..Among them, 4,5,6,7-tetrachloro-N-cycloheptylphthalimide (9) showed the most potent activity, being approximately 30 times more active than the classical inhibitor, 1-deoxynojirimycin (1)...
  15. ncbi Utility of boron clusters for drug design. Hansch-fujita hydrophobic parameters pi of dicarba-closo-dodecaboranyl groups
    K Yamamoto
    Graduate School of Pharmaceutical Sciences, University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan
    Bioorg Med Chem Lett 11:2389-92. 2001
    ..The values (pi=2.69-4.44) vary depending on the position of substitution on the carborane cage and the isomeric form (o-, m-, p-carboranes). These values lie within the range of those of hydrocarbons...