Takayoshi Suzuki

Summary

Affiliation: Nagoya City University
Country: Japan

Publications

  1. ncbi request reprint Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 15:331-5. 2005
  2. ncbi request reprint Design and synthesis of non-hydroxamate histone deacetylase inhibitors: identification of a selective histone acetylating agent
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem 13:4332-42. 2005
  3. ncbi request reprint Non-hydroxamate histone deacetylase inhibitors
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Curr Med Chem 12:2867-80. 2005
  4. ncbi request reprint Epigenetic control using natural products and synthetic molecules
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Curr Med Chem 13:935-58. 2006
  5. ncbi request reprint Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    J Med Chem 48:1019-32. 2005
  6. ncbi request reprint Thiol-based SAHA analogues as potent histone deacetylase inhibitors
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Aichi, Nagoya 467 8603, Japan
    Bioorg Med Chem Lett 14:3313-7. 2004
  7. ncbi request reprint Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Nagoya, Aichi 467 8603, Japan
    J Med Chem 49:4809-12. 2006
  8. ncbi request reprint 2-Anilinobenzamides as SIRT inhibitors
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences Nagoya City University 3 1 Tanabe Dori, Nagoya, Aichi, Japan
    ChemMedChem 1:1059-62. 2006
  9. doi request reprint Design, synthesis, enzyme inhibition, and tumor cell growth inhibition of 2-anilinobenzamide derivatives as SIRT1 inhibitors
    Takayoshi Suzuki
    Nagoya City University, Tanabe dori, Mizuho ku, Aichi, Japan
    Bioorg Med Chem 17:5900-5. 2009
  10. doi request reprint Design, synthesis, inhibitory activity, and binding mode study of novel DNA methyltransferase 1 inhibitors
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 20:1124-7. 2010

Detail Information

Publications76

  1. ncbi request reprint Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 15:331-5. 2005
    ..Kinetic enzyme assays and molecular modeling suggested that the mercaptoacetamide moiety of 5b interacts with the zinc in the active site of HDACs and removes a water molecule from the reactive site of the deacetylation...
  2. ncbi request reprint Design and synthesis of non-hydroxamate histone deacetylase inhibitors: identification of a selective histone acetylating agent
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem 13:4332-42. 2005
    ..Among these, methyl sulfoxide 15 inhibited HDACs in enzyme assays and caused hyperacetylation of histone H4 while not inducing the accumulation of acetylated alpha-tubulin in HCT116 cells...
  3. ncbi request reprint Non-hydroxamate histone deacetylase inhibitors
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Curr Med Chem 12:2867-80. 2005
    ..In this review, we introduce non-hydroxamate HDAC inhibitors describing their design, enzyme inhibition, cancer cell growth inhibition and isozyme selectivity...
  4. ncbi request reprint Epigenetic control using natural products and synthetic molecules
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Curr Med Chem 13:935-58. 2006
    ..In this review, we present natural products and synthetic molecules that inhibit or activate enzymes catalyzing DNA methylation or histone modifications, and discuss the potential of epigenetic therapy...
  5. ncbi request reprint Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    J Med Chem 48:1019-32. 2005
    ..Kinetical enzyme assay and molecular modeling suggest the thiol formed by enzymatic hydrolysis within the cell interacts with the zinc ion in the active site of HDACs...
  6. ncbi request reprint Thiol-based SAHA analogues as potent histone deacetylase inhibitors
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Aichi, Nagoya 467 8603, Japan
    Bioorg Med Chem Lett 14:3313-7. 2004
    ..Compound 6, in which the hydroxamic acid of SAHA was replaced by a thiol, was found to be as potent as SAHA, and optimization of this series led to the identification of HDAC inhibitors more potent than SAHA...
  7. ncbi request reprint Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Nagoya, Aichi 467 8603, Japan
    J Med Chem 49:4809-12. 2006
    ..Aliphatic compounds 17b-20b selectively caused alpha-tubulin acetylation over histone H4 acetylation. In enzyme assays using HDAC1, HDAC4, and HDAC6, compounds 17a-19a exhibited HDAC6-selective inhibition over HDAC1 and HDAC4...
  8. ncbi request reprint 2-Anilinobenzamides as SIRT inhibitors
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences Nagoya City University 3 1 Tanabe Dori, Nagoya, Aichi, Japan
    ChemMedChem 1:1059-62. 2006
  9. doi request reprint Design, synthesis, enzyme inhibition, and tumor cell growth inhibition of 2-anilinobenzamide derivatives as SIRT1 inhibitors
    Takayoshi Suzuki
    Nagoya City University, Tanabe dori, Mizuho ku, Aichi, Japan
    Bioorg Med Chem 17:5900-5. 2009
    ..Among these, compounds 3 and 5 inhibited SIRT1 activity in enzyme assays and suppressed the growth of Daudi and HCT116 cells...
  10. doi request reprint Design, synthesis, inhibitory activity, and binding mode study of novel DNA methyltransferase 1 inhibitors
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 20:1124-7. 2010
    ..Among this series, compounds 5-8 were found to be more potent DNMT1 inhibitors than RG108, a DNMT1 inhibitor reported previously by Siedlecki et al. The binding mode analysis of compound 5 is also reported...
  11. ncbi request reprint Explorative study on isoform-selective histone deacetylase inhibitors
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Chem Pharm Bull (Tokyo) 57:897-906. 2009
    ..Furthermore, we elucidated the functions of HDAC6 by chemical genetic approaches using these inhibitors. The results of this research also suggested the feasibility of using isoform-selective HDAC inhibitors as therapeutic agents...
  12. ncbi request reprint Design, synthesis, and biological activity of folate receptor-targeted prodrugs of thiolate histone deacetylase inhibitors
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 17:4208-12. 2007
    ..The activity of 1 was significantly reduced by free folic acid, suggesting that cellular uptake of 1 is mediated by FR...
  13. doi request reprint Identification of a cell-active non-peptide sirtuin inhibitor containing N-thioacetyl lysine
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 19:5670-2. 2009
    ..Compound 1 selectively inhibited SIRT1 in enzyme assays. Compound 1 also caused a dose-dependent increase in p53 acetylation in human colon cancer HCT116 cells, indicating the inhibition of SIRT1 in these cells...
  14. ncbi request reprint Identification of a potent and stable antiproliferative agent by the prodrug formation of a thiolate histone deacetylase inhibitor
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 17:1558-61. 2007
    ..Among these compounds, S-2-methyl-3-phenylpropanoyl compound 2 showed more potent antiproliferative activity and higher stability in human plasma than S-isobutyryl compound NCH-51...
  15. ncbi request reprint Rational design of non-hydroxamate histone deacetylase inhibitors
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Mini Rev Med Chem 6:515-26. 2006
    ..In this review, we present the rational design, inhibitory effect and antiproliferative activity of non-hydroxamate HDAC inhibitors...
  16. doi request reprint Synthesis and biological activity of optically active NCL-1, a lysine-specific demethylase 1 selective inhibitor
    Daisuke Ogasawara
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem 19:3702-8. 2011
    ..In cell growth inhibition assays, the two isomers showed similar activity in HEK293 cells and SH-SY5Y cells, whereas the (1S,2R)-isomer showed approximately four times more potent activity than the (1R,2S)-isomer in HeLa cells...
  17. ncbi request reprint Nitrogen-substitution effect on in vivo mutagenicity of chrysene
    Katsuya Yamada
    Graduate School of Pharmaceutical Sciences, Nagoya City University, Tanabedori, Mizuho ku, Nagoya 467 8603, Japan
    Mutat Res 586:1-17. 2005
    ..These results suggest that the two types of nitrogen substitutions in the chrysene structure may enhance mutagenicity in the mouse lung, although they showed no difference in the target-organ specificity and the mutation spectrum...
  18. ncbi request reprint Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors
    Yukihiro Itoh
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    J Med Chem 50:5425-38. 2007
    ..They also blocked the growth of estrogen receptor alpha-positive breast cancer MCF-7 cells that had been treated with estrogen. These findings suggested that HDAC6-selective inhibitors have potential as anticancer agents...
  19. doi request reprint Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors
    Shohei Hamada
    Graduate School of Pharmaceutical Sciences, Nagoya City University, Mizuho ku, Nagoya, Aichi, Japan
    J Med Chem 53:5629-38. 2010
    ..These findings suggest that combination treatment with JMJD2 inhibitors and LSD1 inhibitors may represent a novel strategy for anticancer chemotherapy...
  20. ncbi request reprint Novel histone deacetylase inhibitors: design, synthesis, enzyme inhibition, and binding mode study of SAHA-based non-hydroxamates
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 13:4321-6. 2003
    ..analogues bearing nucleophilic functional groups which could bind covalently to HDACs (compounds 16-18). In this series, semicarbazide 8b and bromoacetamides 18b,c were found to be potent HDAC inhibitors for non-hydroxamates...
  21. pmc FFA1-selective agonistic activity based on docking simulation using FFA1 and GPR120 homology models
    Masato Takeuchi
    Department of Genomic Drug Discovery Science, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan
    Br J Pharmacol 168:1570-83. 2013
    ..CONCLUSION AND IMPLICATIONS A docking simulation approach using FFA1 receptor and GPR120 homology models could be useful in predicting FFA1 receptor-selective agonists...
  22. doi request reprint Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    J Med Chem 51:7640-4. 2008
    ..These results provide a basis for constructing new tools for probing the biology of GPR120 and for developing new candidate therapeutic agents...
  23. ncbi request reprint Synthesis and evaluation of 2-Nonylaminopyridine derivatives as PPAR ligands
    Shinya Usui
    Graduate School of Pharmaceutical Sciences, Nagoya City University, Nagoya, Aichi, Japan
    Chem Pharm Bull (Tokyo) 55:1053-9. 2007
    ..In the human hypodermic preadipocyte differentiation test, it was demonstrated that the maximal activity of compounds 3 and 4 was higher than that of rosiglitazone...
  24. ncbi request reprint Identification of cell-active lysine specific demethylase 1-selective inhibitors
    Rie Ueda
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    J Am Chem Soc 131:17536-7. 2009
    ..These inhibitors show in vivo H3K4-methylating activity and antiproliferative activity and should be useful as lead structures for anticancer drugs and as tools for studying the biological roles of LSD1...
  25. doi request reprint Structure-activity relationships of GPR120 agonists based on a docking simulation
    Qi Sun
    Department of Genomic Drug Discovery Science, Graduate School of Pharmaceutical Sciences, Kyoto University, 46 29 Yoshida Shimoadachi cho, Sakyo ku, Kyoto 606 8501, Japan
    Mol Pharmacol 78:804-10. 2010
    ..Taken together, our present study showed that a docking simulation using a GPR120 homology model might be useful to predict the agonistic activity of compounds...
  26. doi request reprint Piloty's acid derivative with improved nitroxyl-releasing characteristics
    Kazuyuki Aizawa
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 23:2340-3. 2013
    ..The high HNO-releasing activity is suggested to be due to electronic and steric effects. Compound 17 may be a useful tool for biological experiments...
  27. doi request reprint Novel bisbenzimide-nitroxides for nuclear redox imaging in living cells
    Mamiko Ikeda
    Graduate School of Pharmaceutical Sciences, Nagoya City University, Tanabe dori 3 1, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 22:1949-52. 2012
    ..This fluorescence increase was inhibited by pretreatment of 1mM ascorbic acid. These results show that compound 3 was suitable for nuclear-specific redox imaging in murine macrophages...
  28. doi request reprint Photocontrollable peroxynitrite generator based on N-methyl-N-nitrosoaminophenol for cellular application
    Naoya Ieda
    Graduate School of Pharmaceutical Science, Nagoya City University, 3 1, Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    J Am Chem Soc 134:2563-8. 2012
    ..Generation of ONOO(-) from P-NAP in HCT-116 cells upon photoirradiation was successfully imaged with HKGreen-3A. This is the first example of a photocontrollable ONOO(-) donor applicable to cultured cells...
  29. ncbi request reprint New series of antiprion compounds: pyrazolone derivatives have the potent activity of inhibiting protease-resistant prion protein accumulation
    Ayako Kimata
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1, Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    J Med Chem 50:5053-6. 2007
    ....
  30. doi request reprint Design, synthesis, and biological activity of boronic acid-based histone deacetylase inhibitors
    Nobuaki Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    J Med Chem 52:2909-22. 2009
    ..Our findings indicate that these boronic acid derivatives represent an entry into a new class of HDAC inhibitors...
  31. doi request reprint Photoinduced nitric oxide release from a nitrobenzene derivative in mitochondria
    Taeko Horinouchi
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Nagoya, Aichi 467 8603, Japan
    Chemistry 17:4809-13. 2011
    ..Our results indicate that RpNO is an effective NO donor for time-controlled, mitochondria-specific NO treatment...
  32. doi request reprint Peroxynitrite generation from a NO-releasing nitrobenzene derivative in response to photoirradiation
    Naoya Ieda
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Nagoya, Aichi 467 8603, Japan
    Chem Commun (Camb) 47:6449-51. 2011
    ....
  33. doi request reprint Multiple bond-conjugated photoinduced nitric oxide releaser working with two-photon excitation
    Kazuhiro Hishikawa
    Graduate School of Pharmaceutical Science, Nagoya City University, 3 1 Tanabe dori Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 20:302-5. 2010
    ..Their decomposition and NO release in response to one-photon excitation, and their decomposition in response to two-photon excitation were examined. Their photoinduced decomposition characteristics are discussed...
  34. doi request reprint Inhibition of human sirtuins by in situ generation of an acetylated lysine-ADP-ribose conjugate
    Tomomi Asaba
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    J Am Chem Soc 131:6989-96. 2009
    ..These results have implications for the development of selective sirtuin inhibitors by means of mechanism-based drug design...
  35. doi request reprint Lysine-specific demethylase 1-selective inactivators: protein-targeted drug delivery mechanism
    Daisuke Ogasawara
    Graduate School of Medical Science, Kyoto Prefectural University of Medicine, 13 Nishitakatsukasa cho, Taishogun Kita ku, Kyoto 603 8334 Japan Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603 Japan
    Angew Chem Int Ed Engl 52:8620-4. 2013
    ..Biological and mechanistic studies indicate that 1 inhibits LSD1 potently and selectively. ..
  36. ncbi request reprint Photoinduced upregulation of calcitonin gene-related peptide in A549 cells through HNO release from a hydrophilic photocontrollable HNO donor
    Kazuya Matsuo
    Department of Organic and Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Nagoya, Aichi 467 8603, Japan
    Chem Pharm Bull (Tokyo) 60:1055-62. 2012
    ..This result demonstrates the suitability of this photocontrollable HNO donor for biological investigations...
  37. ncbi request reprint Novel mitochondria-localizing TEMPO derivative for measurement of cellular oxidative stress in mitochondria
    Shizuka Ban
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 17:2055-8. 2007
    ..Synthesized 1 localized in mitochondria and detected oxidative stress in an endotoxic model of a mouse macrophage-like cell line. Compound 1 is therefore a potentially useful probe for evaluating oxidative stress in mitochondria...
  38. ncbi request reprint Identification of novel PPARalpha ligands by the structural modification of a PPARgamma ligand
    Shinya Usui
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 16:3249-54. 2006
    ..Compound 10, the meta isomer of a PPARgamma agonist 1, has been identified as a PPARalpha ligand. The introduction of methyl and ethyl groups at the C-2 position of the propanoic acid of 10 further improved the PPARalpha-binding potency...
  39. doi request reprint Development of a DNA-binding TEMPO derivative for evaluation of nuclear oxidative stress and its application in living cells
    Mamiko Ikeda
    Graduate School of Pharmaceutical Sciences, Nagoya City University, Nagoya, Aichi, Japan
    Free Radic Biol Med 49:1792-7. 2010
    ..Thus, subcellular redox microenvironments show marked variability in endotoxin-stimulated living cells...
  40. doi request reprint Photoinduced nitric oxide release from a hindered nitrobenzene derivative by two-photon excitation
    Kazuhiro Hishikawa
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori Mizuho ku, Nagoya, Aichi 467 8603, Japan
    J Am Chem Soc 131:7488-9. 2009
    ..After pulse laser irradiation to a solution of Flu-DNB, oxidation products of NO were observed. This is the first account of a non-nitrosyl-chelated metal ion containing NO donor which can be controlled by the TPE technique...
  41. doi request reprint Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors
    Shohei Hamada
    Nagoya City University, Tanabe dori, Mizuho ku, Aichi, Japan
    Bioorg Med Chem Lett 19:2852-5. 2009
    ..NOG and compound 1 inhibited histone lysine demethylases JMJD2A, 2C and 2D in enzyme assays, and their dimethyl ester prodrugs DMOG and 21 exerted histone lysine methylating activity in cellular assays...
  42. ncbi request reprint In vivo mutagenicity of benzo[f]quinoline, benzo[h]quinoline, and 1,7-phenanthroline using the lacZ transgenic mice
    Katsuya Yamada
    Graduate School of Pharmaceutical Sciences, Nagoya City University, Tanabedori, Mizuho ku, Nagoya 467 8603, Japan
    Mutat Res 559:83-95. 2004
    ..These results suggest that the in vivo mutagenicity of 1,7-Phe might be caused by the same mechanism as that of quinoline, which induced the same mutational spectrum change (G:C to C:G transversion)...
  43. ncbi request reprint Synthesis of a photocontrollable hydrogen sulfide donor using ketoprofenate photocages
    Naoki Fukushima
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Chem Commun (Camb) 50:587-9. 2014
    ..Photocontrolled H2S release from this donor was also demonstrated in bovine serum. This H2S donor should be suitable for use in various biological systems. ..
  44. ncbi request reprint Preparation of C60-based active esters and coupling of C60 moiety to amines or alcohols
    Hiroki Tsumoto
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabedori, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 18:657-60. 2008
    ..Reactions of the active esters with amines or alcohols proceeded easily to give a variety of compounds having the C(60) moiety...
  45. doi request reprint A novel mitochondria-localizing nitrobenzene derivative as a donor for photo-uncaging of nitric oxide
    Taeko Horinouchi
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 21:2000-2. 2011
    ..NBDNO was colocalized with MitoRed, a mitochondrial stain, in HCT116 colon cancer cells. Our results indicate that NBDNO is an effective NO donor for time-controlled, mitochondria-specific NO treatment...
  46. ncbi request reprint Metabolic activation of 10-aza-substituted benzo[a]pyrene by cytochrome P450 1A2 in human liver microsomes
    Katsuya Yamada
    Graduate School of Pharmaceutical Sciences, Nagoya City University, Tanabedori, Mizuho ku, Nagoya 467 8603, Japan
    Mutat Res 557:159-65. 2004
    ..With regard to the proposal that BaP may be activated by human CYP1A1, our results suggest that the nitrogen-substitution at position-10 of BaP may cause the CYP enzyme-specificity in metabolic activation to change from CYP1A1 to CYP1A2...
  47. ncbi request reprint Design, synthesis, and biological activity of novel PPARgamma ligands based on rosiglitazone and 15d-PGJ2
    Shinya Usui
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 15:1547-51. 2005
    ..Molecular modeling suggested that the nonyl group of 9 interacted with hydrophobic amino acid residues constructing the hydrophobic region of PPARgamma protein where the alkyl chain of 15d-PGJ2 is expected to be located...
  48. ncbi request reprint Isoform-selective histone deacetylase inhibitors
    Yukihiro Itoh
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Curr Pharm Des 14:529-44. 2008
    ..In this review, we cover isoform-selective HDAC inhibitors, including their biochemical and pharmacological functions...
  49. ncbi request reprint Identification of novel SIRT2-selective inhibitors using a click chemistry approach
    Prima R Tatum
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 24:1871-4. 2014
    ..Screening identified two SIRT2-selective inhibitors, which were more SIRT2-selective than AGK2, a known SIRT2 inhibitor. These findings will be useful for further development of SIRT2-selective inhibitors. ..
  50. doi request reprint An overview of phenylcyclopropylamine derivatives: biochemical and biological significance and recent developments
    Mohammed Naseer Ahmed Khan
    Graduate School of Pharmaceutical Sciences, Nagoya City University, Nagoya, Aichi, Japan
    Med Res Rev 33:873-910. 2013
    ..Furthermore, we also highlight recent advance in this area and discuss their future applications for beneficial therapeutic effects...
  51. doi request reprint A reductant-resistant and metal-free fluorescent probe for nitroxyl applicable to living cells
    Kodai Kawai
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Nagoya, Aichi 467 8603, Japan
    J Am Chem Soc 135:12690-6. 2013
    ..These results suggest that P-Rhod is suitable for detection of HNO in living cells. ..
  52. doi request reprint Novel histone deacetylase inhibitor NCH-51 activates latent HIV-1 gene expression
    Ann Florence B Victoriano
    Department of Molecular and Cellular Biology, Nagoya City University Graduate School for Medical Sciences, Nagoya, Aichi, Japan
    FEBS Lett 585:1103-11. 2011
    ..When Sp1 expression was knocked-down by small interfering RNA, the NCH-51-mediated activation of a stably integrated HIV-1 LTR was attenuated. Moreover, the Sp1 inhibitor mithramycin A abolished the effects of NCH-51...
  53. ncbi request reprint Photoinduced nitric oxide release from nitrobenzene derivatives
    Takayoshi Suzuki
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    J Am Chem Soc 127:11720-6. 2005
    ....
  54. ncbi request reprint Alternative photoinduced release of HNO or NO from an acyl nitroso compound, depending on environmental polarity
    Kazuya Matsuo
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Chem Commun (Camb) 46:3788-90. 2010
    ..Production of either nitric oxide (NO) or nitroxyl (HNO) was photoinduced from this compound, depending on the environmental polarity...
  55. doi request reprint Syntheses of water-soluble [60]fullerene derivatives and their enhancing effect on neurite outgrowth in NGF-treated PC12 cells
    Hiroki Tsumoto
    Graduate School of Pharmaceutical Sciences, Nagoya City University, Mizuho ku, Nagoya, Aichi, Japan
    Bioorg Med Chem Lett 20:1948-52. 2010
    ....
  56. doi request reprint Fine spatiotemporal control of nitric oxide release by infrared pulse-laser irradiation of a photolabile donor
    Hidehiko Nakagawa
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1, Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    ACS Chem Biol 8:2493-500. 2013
    ..To our knowledge, this is the first demonstration of induction of biological responses in vitro and in vivo by means of precisely controlled, two-photon-mediated release of NO. ..
  57. pmc Loss of deacetylation activity of Hdac6 affects emotional behavior in mice
    Masahide Fukada
    Department of Embryology, Institute for Developmental Research, Aichi Human Service Center, Kasugai, Aichi, Japan
    PLoS ONE 7:e30924. 2012
    ..These findings suggest that HDAC6-mediated reversible acetylation might contribute to maintain proper neuronal activity in serotonergic neurons, and also provide a new therapeutic target for depression...
  58. ncbi request reprint Novel membrane-localizing TEMPO derivatives for measurement of cellular oxidative stress at the cell membrane
    Shizuka Ban
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 17:1451-4. 2007
    ..Compound 1 is therefore a potentially useful probe for evaluating oxidative stress at the cell membrane...
  59. ncbi request reprint Phenylpropanoic acid derivatives bearing a benzothiazole ring as PPARdelta-selective agonists
    Hiroki Fujieda
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 17:4351-7. 2007
    ..Optimization of this series led to the identification of a potent and selective PPARdelta agonist 17. Molecular modeling suggested that compound 17 occupies the Y-shaped pocket of PPARdelta appropriately...
  60. ncbi request reprint In vivo genotoxicity evaluation of dimethylarsinic acid in MutaMouse
    Yasuhiro Noda
    Department of Biochemical Toxicology, Nihon University College of Pharmacy, 7 7 1 Narashinodai, Funabashi shi 274 8555, Japan
    Mutat Res 513:205-12. 2002
    ..The assay for micronuclei gave marginally positive results with arsenite, but not with DMA. These results suggest that the mutagenicity of DMA and arsenite might be too low to be detected in the MutaMouse...
  61. ncbi request reprint Hydroxyl radical scavenging by edaravone derivatives: Efficient scavenging by 3-methyl-1-(pyridin-2-yl)-5-pyrazolone with an intramolecular base
    Hidehiko Nakagawa
    Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1, Tanabe dori, Mizuho ku, Nagoya, Aichi 467 8603, Japan
    Bioorg Med Chem Lett 16:5939-42. 2006
    ..Its efficient radical scavenging activity was assumed to be due to the increase of its anion form, an active form, by a hydrogen-bonded intramolecular base...
  62. doi request reprint Degradation of filamin induces contraction of vascular smooth muscle cells in type-I collagen matrix honeycombs
    Masashi Uchida
    Graduate School of Pharmaceutical Sciences, Chiba University, 1 8 1 Inohana, Chuo Ku, Chiba, Japan
    Cell Physiol Biochem 27:669-80. 2011
    ..The role of filamin, an actin-binding protein that links actin filaments in SMCs, was investigated...
  63. ncbi request reprint Effect of 10-aza-substitution on benzo[a]pyrene mutagenicity in vivo and in vitro
    Katsuya Yamada
    Faculty of Graduate School of Pharmaceutical Sciences, Nagoya City University, Tanabedori, Mizuho ku, Nagoya 467 8603, Japan
    Mutat Res 521:187-200. 2002
    ..These results indicate that 10-aza-substitution markedly modifies the nature of mutagenicity of benzo[a]pyrene in both in vivo and in vitro mutagenesis assays...
  64. ncbi request reprint DNA adducts and mutagenic specificity of the ubiquitous environmental pollutant 3-nitrobenzanthrone in Muta Mouse
    Volker M Arlt
    Section of Molecular Carcinogenesis, Institute of Cancer Research, Surrey, United Kingdom
    Environ Mol Mutagen 43:186-95. 2004
    ..These results suggest that G:C-->T:A transversions induced by 3-NBA are caused by misreplication of adducted guanine residues through incorporation of adenine opposite the adduct (A-rule)...
  65. ncbi request reprint Mutagenicity of aristolochic acid in the lambda/lacZ transgenic mouse (MutaMouse)
    Arihiro Kohara
    Division of Genetics and Mutagenesis, National Institute of Health Sciences, 1 18 1, Kamiyoga, Setagaya Ku, 158 8501, Tokyo, Japan
    Mutat Res 515:63-72. 2002
    ..These results suggested that AA, which is activated by cytochrome P450 and peroxidase to form cyclic nitrenium ions that bind to deoxyadenine, caused the A to T transversions in the target organs of mice...
  66. ncbi request reprint Potassium bromate treatment predominantly causes large deletions, but not GC>TA transversion in human cells
    Yang Luan
    Division of Cellular and Gene Therapy Products, National Institute of Health Sciences, 1 18 1 Kamiyoga, Setagaya Ku, Tokyo 158 8501, Japan
    Mutat Res 619:113-23. 2007
    ..However, we could not observe the similarity of gene expression profile in the treatment of KBrO(3) to ionizing-irradiation as well as oxidative damage inducers...
  67. ncbi request reprint Granulocyte colony-stimulating factor promotes the translocation of protein kinase Ciota in neutrophilic differentiation cells
    Toshie Kanayasu-Toyoda
    Division of Cellular and Gene Therapy Products, National Institute of Health Sciences, Tokyo, Japan
    J Cell Physiol 211:189-96. 2007
    ..These data indicate that the G-CSF-induced dynamic translocation and activation processes of PKCiota are important to neutrophilic proliferation...
  68. ncbi request reprint Dinitropyrenes induce gene mutations in multiple organs of the lambda/lacZ transgenic mouse (Muta Mouse)
    Arihiro Kohara
    Division of Genetics and Mutagenesis, National Institute of Health Sciences, 1 18 1, Kamiyoga, Setagaya Ku, 158 8501, Tokyo, Japan
    Mutat Res 515:73-83. 2002
    ..The present study showed a relevant use of the cII gene as an additional target for mutagenesis in the Muta Mouse and revealed a mutagenic specificity of DNPs in vivo...
  69. ncbi request reprint Flow cytometric analysis of micronuclei in peripheral blood reticulocytes: I. Intra- and interlaboratory comparison with microscopic scoring
    Stephen D Dertinger
    Litron Laboratories, Rochester, New York 14623, USA
    Toxicol Sci 94:83-91. 2006
    ..Furthermore, data presented herein demonstrate a clear advantage of flow cytometry-based scoring over microscopy-significantly lower inter- and intralaboratory variation and higher statistical sensitivity...
  70. ncbi request reprint Regional mutagenicity of heterocyclic amines in the intestine: mutation analysis of the cII gene in lambda/lacZ transgenic mice
    Toshiaki Itoh
    Department of Molecular Bacteriology, Graduate School of Medicine, The University of Tokushima, 3 18 15 Kuramoto cho, Tokushima 770 8503, Japan
    Mutat Res 539:99-108. 2003
    ..1 times the control value. Mutagenic potency was in the order PhIP>MeIQ>IQ; Trp-P-2 did not significantly increase the MF in any tissue. The cecum was the most susceptible organ to HCA mutagenicity...
  71. ncbi request reprint In vivo transgenic mutation assays
    Veronique Thybaud
    Aventis Pharma, Drug Safety Evaluation, Vitry sur Seine, France
    Mutat Res 540:141-51. 2003
    ....
  72. ncbi request reprint Benzimidazole derivatives bearing substituted biphenyls as hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitors: structure-activity relationship studies and identification of a potent and highly selective inhibitor JTK-109
    Shintaro Hirashima
    Central Pharmaceutical Research Institute, Japan Tobacco Inc, Takatsuki, Osaka 569 1125, Japan
    J Med Chem 49:4721-36. 2006
    ..Among the new compounds, compound 10n (JTK-109) exhibited favorable pharmacokinetic profiles, high selectivity for NS5B, and good safety profiles, suggesting the potential for a clinical candidate in the treatment of hepatitis C...
  73. ncbi request reprint Genotoxicity of microcystin-LR in human lymphoblastoid TK6 cells
    Li Zhan
    Division of Genetics and Mutagenesis, National Institute of Health Sciences, 1 18 1 Kamiyoga, Setagaya Ku, Tokyo 158 8501, Japan
    Mutat Res 557:1-6. 2004
    ..These results indicate that MCLR had a clastogenic effect. We discuss the mechanisms of MCLR genotoxicity and the possibility of its being a hepatocarcinogen...
  74. ncbi request reprint HX531, a retinoid X receptor antagonist, inhibited the 9-cis retinoic acid-induced binding with steroid receptor coactivator-1 as detected by surface plasmon resonance
    Toshie Kanayasu-Toyoda
    National Institute of Health Sciences, 1 18 1, Kamiyoga, Setagaya Ku, 158 8501 Tokyo, Japan
    J Steroid Biochem Mol Biol 94:303-9. 2005
    ..This SPR assay system was applied to obtain quantitative kinetic data of RXR ligand binding to the SRC-1 peptide and the alteration of these data by antagonists...
  75. ncbi request reprint Benzimidazole inhibitors of hepatitis C virus NS5B polymerase: identification of 2-[(4-diarylmethoxy)phenyl]-benzimidazole
    Tomio Ishida
    Chemical Research Laboratories, Central Pharmaceutical Research Institute, Japan Tobacco Inc, 1 1 Murasaki cho, Takatsuki, Osaka 569 1125, Japan
    Bioorg Med Chem Lett 16:1859-63. 2006
    ..They inhibit subgenomic HCV RNA replication in the replicon cells at low micromolar concentrations (EC(50) as low as 1.1microM). They are selective against DNA polymerases (IC(50)>10microM) and exhibit low cytotoxicity...
  76. ncbi request reprint Evaluation of liver and peripheral blood micronucleus assays with 9 chemicals using young rats. A study by the Collaborative Study Group for the Micronucleus Test (CSGMT)/Japanese Environmental Mutagen Society (JEMS)-Mammalian Mutagenicity Study Group (MM
    Hiroshi Suzuki
    Ina Research Inc, 2148 188 Nishiminowa, Ina shi, Nagano 399 4501, Japan
    Mutat Res 583:133-45. 2005
    ....