WATARU NOMURA

Last Updated :2021/03/01

Affiliations, Positions
Graduate School of Biomedical and Health Sciences(Pharmaceutical Sciences), Professor
E-mail
wnomurahiroshima-u.ac.jp

Basic Information

Academic Degrees

  • Kyoto University

Educational Activity

Course in Charge

  1. 2020, Undergraduate Education, Year, Special laboratory Works in Clinical Pharmacy III
  2. 2020, Undergraduate Education, 3Term, Biological Chemistry IV
  3. 2020, Undergraduate Education, First Semester, Practice of Biochemical Pharmacology
  4. 2020, Undergraduate Education, 2Term, Physiological Chemistry
  5. 2020, Undergraduate Education, 3Term, Japanese Pharmacopoeia
  6. 2020, Undergraduate Education, Second Semester, Experiments of Biological Chemistry
  7. 2020, Undergraduate Education, Year, Special laboratory Works in Pharmaceutical Sciences I
  8. 2020, Undergraduate Education, Year, Special laboratory Works in Pharmaceutical Sciences II
  9. 2020, Undergraduate Education, Second Semester, Special laboratory Works in Pharmaceutical Sciences III
  10. 2020, Undergraduate Education, Year, Special laboratory Works in Clinical Pharmacy I
  11. 2020, Undergraduate Education, Year, Special laboratory Works in Clinical Pharmacy II
  12. 2020, Graduate Education (Doctoral Program) , First Semester, Advanced seminar on Physiological Chemistry
  13. 2020, Graduate Education (Doctoral Program) , Second Semester, Advanced seminar on Physiological Chemistry
  14. 2020, Graduate Education (Doctoral Program) , First Semester, Advanced research on Physiological Chemistry
  15. 2020, Graduate Education (Doctoral Program) , Second Semester, Advanced research on Physiological Chemistry
  16. 2020, Graduate Education (Doctoral Program) , First Semester, Advanced Seminar on Physiological Chemistry
  17. 2020, Graduate Education (Doctoral Program) , Second Semester, Advanced Seminar on Physiological Chemistry
  18. 2020, Graduate Education (Doctoral Program) , First Semester, Advanced Research on Physiological Chemistry
  19. 2020, Graduate Education (Doctoral Program) , Second Semester, Advanced Research on Physiological Chemistry
  20. 2020, Graduate Education (Master's Program) , First Semester, Seminar on Mechanisms of Signal Transduction
  21. 2020, Graduate Education (Master's Program) , Second Semester, Seminar on Mechanisms of Signal Transduction
  22. 2020, Graduate Education (Master's Program) , First Semester, Research on Mechanisms of Signal Transduction
  23. 2020, Graduate Education (Master's Program) , Second Semester, Research on Mechanisms of Signal Transduction
  24. 2020, Graduate Education (Doctoral Program) , 3Term, Trends of Genome Editing in Life Science

Research Activities

Academic Papers

  1. Benzolactam-related compounds promote apoptosis of HIV-infected human cells via protein kinase C-induced HIV latency reversal., The Journal of biological chemistry, 294(1), 2019
  2. Design, synthesis and biological evaluation of low molecular weight CXCR4 ligands., Bioorganic & medicinal chemistry, 27(6), 2019
  3. Development of a NanoBRET-Based Sensitive Screening Method for CXCR4 Ligands., Bioconjugate chemistry, 30(5), 2019
  4. Dimeric C34 Derivatives Linked through Disulfide Bridges as New HIV-1 Fusion Inhibitors., Chembiochem : a European journal of chemical biology, 20(16), 2019
  5. Synthesis of a Chloroalkene Dipeptide Isostere-Containing Peptidomimetic and Its Biological Application., ACS medicinal chemistry letters, 9(1), 2018
  6. Delivery of a Proapoptotic Peptide to EGFR-Positive Cancer Cells by a Cyclic Peptide Mimicking the Dimerization Arm Structure of EGFR., Bioconjugate chemistry, 29(6), 2018
  7. Development of Toolboxes for Precision Genome/Epigenome Editing and Imaging of Epigenetics., Chemical record (New York, N.Y.), 18(12), 2018
  8. Efficient and Orthogonal Transcription Regulation by Chemically Inducible Artificial Transcription Factors., Biochemistry, 57(45), 2018
  9. Inhibition of EGFR Activation by Bivalent Ligands Based on a Cyclic Peptide Mimicking the Dimerization Arm Structure of EGFR., Chemical & pharmaceutical bulletin, 66(11), 2018
  10. Development of anti-HIV peptides based on a viral capsid protein., Biopolymers, 108(1), 2017
  11. Bivalent 14-mer peptide ligands of CXCR4 with polyproline linkers with anti-chemotactic activity against Jurkat cells., Journal of peptide science : an official publication of the European Peptide Society, 23(7-8), 2017
  12. Microwave-Assisted Synthesis of Azacoumarin Fluorophores and the Fluorescence Characterization., The Journal of organic chemistry, 82(5), 2017
  13. Synthesis and Evaluation of Dimeric Derivatives of Diacylglycerol-Lactones as Protein Kinase C Ligands., Bioconjugate chemistry, 28(8), 2017
  14. Creation of Functional Molecules Based on Biomolecular Interactions; Development toward Chemical Biology., Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan, 137(10), 2017
  15. [ZIP tag-probe system: A fluorescence imaging tool for intercellular proteins]., Seikagaku. The Journal of Japanese Biochemical Society, 89(1), 2017
  16. Multimerized HIV-gp41-derived peptides as fusion inhibitors and vaccines., Biopolymers, 106(4), 2016
  17. A minimally cytotoxic CD4 mimic as an HIV entry inhibitor., Bioorganic & medicinal chemistry letters, 26(2), 2016
  18. Small-Molecule CD4 Mimics Containing Mono-cyclohexyl Moieties as HIV Entry Inhibitors., ChemMedChem, 11(8), 2016
  19. Functional evaluation of fluorescein-labeled derivatives of a peptide inhibitor of the EGF receptor dimerization., Bioorganic & medicinal chemistry, 24(16), 2016
  20. [Chemical biology for pharmaceutical science--integrative approaches for elucidation of biological phenomena]., Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan, 135(3), 2015
  21. [Application and potential of genome engineering by artificial enzymes]., Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan, 135(3), 2015
  22. An in-cell fluorogenic Tag-probe system for protein dynamics imaging enabled by cell-penetrating peptides., Bioconjugate chemistry, 26(6), 2015
  23. Anti-HIV screening for cell-penetrating peptides using chloroquine and identification of anti-HIV peptides derived from matrix proteins., Bioorganic & medicinal chemistry, 23(15), 2015
  24. Trivalent ligands for CXCR4 bearing polyproline linkers show specific recognition for cells with increased CXCR4 expression., Organic & biomolecular chemistry, 13(32), 2015
  25. Exploration of labeling by near infrared dyes of the polyproline linker for bivalent-type CXCR4 ligands., Bioorganic & medicinal chemistry, 23(21), 2015
  26. Utilization of the Heavy Atom Effect for the Development of a Photosensitive 8-Azacoumarin-Type Photolabile Protecting Group., Organic letters, 17(21), 2015
  27. Development of a traceable linker containing a thiol-responsive amino acid for the enrichment and selective labelling of target proteins., Organic & biomolecular chemistry, 12(23), 2014
  28. Screening for protein kinase C ligands using fluorescence resonance energy transfer., Chemical & pharmaceutical bulletin, 62(10), 2014
  29. Low-molecular-weight CXCR4 ligands with variable spacers., ChemMedChem, 8(1), 2013
  30. CD4 mimics as HIV entry inhibitors: lead optimization studies of the aromatic substituents., Bioorganic & medicinal chemistry, 21(9), 2013
  31. Multimerized CHR-derived peptides as HIV-1 fusion inhibitors., Bioorganic & medicinal chemistry, 21(15), 2013
  32. Peptide-based ligand screening and functional analysis of protein kinase C., Biopolymers, 100(6), 2013
  33. Cell-permeable stapled peptides based on HIV-1 integrase inhibitors derived from HIV-1 gene products., ACS chemical biology, 8(10), 2013
  34. Anti-HIV-1 peptide derivatives based on the HIV-1 Co-receptor CXCR4., ChemMedChem, 8(10), 2013
  35. CXCR4-derived synthetic peptides inducing anti-HIV-1 antibodies., Bioorganic & medicinal chemistry, 21(22), 2013
  36. A CD4 mimic as an HIV entry inhibitor: pharmacokinetics., Bioorganic & medicinal chemistry, 21(24), 2013
  37. A synthetic C34 trimer of HIV-1 gp41 shows significant increase in inhibition potency., ChemMedChem, 7(2), 2012
  38. Conjugation of cell-penetrating peptides leads to identification of anti-HIV peptides from matrix proteins., Bioorganic & medicinal chemistry, 20(4), 2012
  39. Effects of DNA binding of the zinc finger and linkers for domain fusion on the catalytic activity of sequence-specific chimeric recombinases determined by a facile fluorescent system., Biochemistry, 51(7), 2012
  40. Evaluation of a synthetic C34 trimer of HIV-1 gp41 as AIDS vaccines., Bioorganic & medicinal chemistry, 20(10), 2012
  41. Pharmacophore-based small molecule CXCR4 ligands., Bioorganic & medicinal chemistry letters, 22(12), 2012
  42. Fluorescent-responsive synthetic C1b domains of protein kinase Cδ as reporters of specific high-affinity ligand binding., Bioconjugate chemistry, 22(1), 2011
  43. Azamacrocyclic metal complexes as CXCR4 antagonists., ChemMedChem, 6(5), 2011
  44. Intense blue fluorescence in a leucine zipper assembly., Chembiochem : a European journal of chemical biology, 12(5), 2011
  45. Fluorescence-quenching screening of protein kinase C ligands with an environmentally sensitive fluorophore., Bioconjugate chemistry, 22(5), 2011
  46. Small molecular CD4 mimics as HIV entry inhibitors., Bioorganic & medicinal chemistry, 19(22), 2011
  47. Synthetic caged DAG-lactones for photochemically controlled activation of protein kinase C., Chembiochem : a European journal of chemical biology, 12(4), 2011
  48. The successes and failures of HIV drug discovery., Expert opinion on drug discovery, 6(10), 2011
  49. CD4 mimics targeting the mechanism of HIV entry., Bioorganic & medicinal chemistry letters, 20(1), 2010
  50. Remodeling of dynamic structures of HIV-1 envelope proteins leads to synthetic antigen molecules inducing neutralizing antibodies., Bioconjugate chemistry, 21(4), 2010
  51. [Development of site-specific DNA methylase for epigenetic regulation of gene expression]., Seikagaku. The Journal of Japanese Biochemical Society, 82(5), 2010
  52. Development of crosslink-type tag-probe pairs for fluorescent imaging of proteins., Biopolymers, 94(6), 2010
  53. Peptide HIV-1 integrase inhibitors from HIV-1 gene products., Journal of medicinal chemistry, 53(14), 2010
  54. Peptidic HIV integrase inhibitors derived from HIV gene products: structure-activity relationship studies., Bioorganic & medicinal chemistry, 18(18), 2010
  55. CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist., Bioorganic & medicinal chemistry letters, 20(19), 2010
  56. Bivalent ligands of CXCR4 with rigid linkers for elucidation of the dimerization state in cells., Journal of the American Chemical Society, 132(45), 2010
  57. Synthesis of protein kinase Cdelta C1b domain by native chemical ligation methodology and characterization of its folding and ligand binding., Journal of peptide science : an official publication of the European Peptide Society, 15(10), 2009
  58. Structure-activity relationship study on artificial CXCR4 ligands possessing the cyclic pentapeptide scaffold: the exploration of amino acid residues of pentapeptides by substitutions of several aromatic amino acids., Organic & biomolecular chemistry, 7(18), 2009
  59. Fluorogenically active leucine zipper peptides as tag-probe pairs for protein imaging in living cells., Angewandte Chemie (International ed. in English), 48(48), 2009
  60. Fluorophore labeling enables imaging and evaluation of specific CXCR4-ligand interaction at the cell membrane for fluorescence-based screening., Bioconjugate chemistry, 19(9), 2008
  61. Structure-activity relationship study of CXCR4 antagonists bearing the cyclic pentapeptide scaffold: identification of the new pharmacophore., Organic & biomolecular chemistry, 6(23), 2008
  62. Exploratory studies on development of the chemokine receptor CXCR4 antagonists toward downsizing., Perspectives in medicinal chemistry, 2, 2008
  63. A future perspective on the development of chemokine receptor CXCR4 antagonists., Expert opinion on drug discovery, 3(10), 2008
  64. Design and synthesis of artificial zinc finger proteins., Methods in molecular biology (Clifton, N.J.), 352, 2007
  65. In vivo site-specific DNA methylation with a designed sequence-enabled DNA methylase., Journal of the American Chemical Society, 129(28), 2007
  66. Effects of linking 15-zinc finger domains on DNA binding specificity and multiple DNA binding modes., Bioorganic & medicinal chemistry letters, 15(9), 2005
  67. Influence of TFIIIA-type linker at the N- or C-terminal of nine-zinc finger protein on DNA-binding site., Biochemical and biophysical research communications, 300(1), 2003
  68. Effects of length and position of an extended linker on sequence-selective DNA recognition of zinc finger peptides., Biochemistry, 42(50), 2003
  69. Interconversion between serine and aspartic acid in the alpha helix of the N-terminal zinc finger of Sp1: implication for general recognition code and for design of novel zinc finger peptide recognizing complementary strand., Biochemistry, 41(28), 2002
  70. Synthesis of hydrophilic caged DAG-lactones for chemical biology applications, ORGANIC & BIOMOLECULAR CHEMISTRY, 18(22), 4217-4223, 2020
  71. Introducing "Future of Biochemistry 2020: The Asia-Pacific Issue", BIOCHEMISTRY, 59(1), 1-7, 2020
  72. TALEN-Based Chemically Inducible, Dimerization-Dependent, Sequence-Specific Nucleases, Biochemistry, 59(2), 197-204, 20200121
  73. Synthesis of hydrophilic caged DAG-lactones for chemical biology applications, Organic and Biomolecular Chemistry, 18(22), 4217-4223, 20200614
  74. Development of a NanoBRET-Based Sensitive Screening Method for CXCR4 Ligands, BIOCONJUGATE CHEMISTRY, 30(5), 1442-1450, 2019
  75. A minimally cytotoxic CD4 mimic as an HIV entry inhibitor, Bioorganic and Medicinal Chemistry Letters, 26(2), 397-400, 20160115
  76. Small-Molecule CD4 Mimics Containing Mono-cyclohexyl Moieties as HIV Entry Inhibitors, ChemMedChem, 11(8), 940-946, 20160419
  77. Multimerized HIV-gp41-derived peptides as fusion inhibitors and vaccines, Biopolymers, 622-628, 20161104
  78. Development of anti-HIV peptides based on a viral capsid protein, Biopolymers, 108(1), 20170101
  79. Microwave-Assisted Synthesis of Azacoumarin Fluorophores and the Fluorescence Characterization, Journal of Organic Chemistry, 82(5), 2739-2744, 20170303
  80. Bivalent 14-mer peptide ligands of CXCR4 with polyproline linkers with anti-chemotactic activity against Jurkat cells, Journal of Peptide Science, 23(7-8), 574-580, 20170701
  81. Synthesis and Evaluation of Dimeric Derivatives of Diacylglycerol-Lactones as Protein Kinase C Ligands, Bioconjugate Chemistry, 28(8), 2135-2144, 20170816
  82. Creation of functional molecules based on biomolecular interactions; development toward chemical biology, Yakugaku Zasshi, 137(10), 1223-1231, 20170101
  83. ZIP tag-probe system: A fluorescence imaging tool for intercellular proteins, Seikagaku, 89(1), 115-120, 20170101
  84. Synthesis of a Chloroalkene Dipeptide Isostere-Containing Peptidomimetic and Its Biological Application, ACS Medicinal Chemistry Letters, 9(1), 7-11, 20180111
  85. Delivery of a Proapoptotic Peptide to EGFR-Positive Cancer Cells by a Cyclic Peptide Mimicking the Dimerization Arm Structure of EGFR, Bioconjugate Chemistry, 29(6), 2050-2057, 20180620
  86. Development of Toolboxes for Precision Genome/Epigenome Editing and Imaging of Epigenetics, Chemical Record, 18(12), 1717-1726, 20181201
  87. Inhibition of EGFR activation by bivalent ligands based on a cyclic peptide mimicking the dimerization arm structure of EGFR, Chemical and Pharmaceutical Bulletin, 66(11), 1083-1089, 20180101
  88. Efficient and Orthogonal Transcription Regulation by Chemically Inducible Artificial Transcription Factors, Biochemistry, 57(45), 6452-6459, 20181113
  89. Benzolactam-related compounds promote apoptosis of HIV-infected human cells via protein kinase C–induced HIV latency reversal, Journal of Biological Chemistry, 294(1), 116-129, 20190104
  90. Design, synthesis and biological evaluation of low molecular weight CXCR4 ligands, Bioorganic and Medicinal Chemistry, 27(6), 1130-1138, 20190315
  91. Development of a NanoBRET-based sensitive screening method for CXCR4 ligands, Bioconjugate Chemistry, 30(5), 1442-1450, 20190515
  92. Dimeric C34 Derivatives Linked through Disulfide Bridges as New HIV-1 Fusion Inhibitors, ChemBioChem, 20(16), 2101-2108, 20190101
  93. A cell cycle-dependent CRISPR-Cas9 activation system based on an anti-CRISPR protein shows improved genome editing accuracy, Communications Biology, 3(1), 20201201

Awards

  1. 2016/09/17, Young Investigator Award, Japanese Pharmaceutical Society, Kanto-branch, 生体分子間相互作用を基盤とする機能分子の創製とケミカルバイオロジーへの展開
  2. 2013/11/08, Young Investigator Award, Japanese Peptide Society, Development of Peptide-derived Molecular Probes and Inhibitors Based on the Interactions with Biomacromolecules