WATARU NOMURA

Last Updated :2022/11/02

Affiliations, Positions
Graduate School of Biomedical and Health Sciences(Pharmaceutical Sciences), Professor
E-mail
wnomurahiroshima-u.ac.jp
Self-introduction
In my research, I am interested in genome editing technology, protein engineering, and fluorescence imaging technology, with the aim of creating functional proteins that have never existed before, which will lead to developing new screening technologies and research methods using these proteins. Genome editing technology can rewrite genes that can be used in various organisms, and is expected to be applied in various industries such as medicine, agriculture and livestock industry. We expect that the development of more accurate and safer methods will lead to a wider range of applications.

Basic Information

Major Professional Backgrounds

  • 2002/04, 2005/03, Japan Society for the Promotion of Science, Research Fellow, JSPS
  • 2005/04, 2007/07, The Scripps Research Institute, Research Associate
  • 2007/08, 2011/12, Tokyo Medical and Dental University, Assistant Professor
  • 2012/01, 2013/03, Tokyo Medical and Dental University, Junior Associate Professor
  • 2013/04, 2019/03, Tokyo Medical and Dental University, Associate Professor
  • 2019/04, Hiroshima University, Graduate School of Biomedical & Health Sciences, Professor

Educational Backgrounds

  • Kyoto University, Japan, 2002/04, 2005/03
  • Kyoto University, Japan, 2000/04, 2002/03
  • Kyoto University, Japan, 1996/04, 2000/03

Academic Degrees

  • Kyoto University

Educational Activity

Course in Charge

  1. 2022, Undergraduate Education, 2Term, Biological Chemistry IV
  2. 2022, Undergraduate Education, First Semester, Practice of Biochemical Pharmacology
  3. 2022, Undergraduate Education, 2Term, Physiological Chemistry
  4. 2022, Undergraduate Education, 3Term, Japanese Pharmacopoeia
  5. 2022, Undergraduate Education, Second Semester, Experiments of Biological Chemistry
  6. 2022, Undergraduate Education, Year, Special laboratory Works in Pharmaceutical Sciences I
  7. 2022, Undergraduate Education, Year, Special laboratory Works in Pharmaceutical Sciences II
  8. 2022, Undergraduate Education, Second Semester, Special laboratory Works in Pharmaceutical Sciences III
  9. 2022, Undergraduate Education, Year, Special laboratory Works in Clinical Pharmacy I
  10. 2022, Undergraduate Education, Year, Special laboratory Works in Clinical Pharmacy II
  11. 2022, Undergraduate Education, Year, Special laboratory Works in Clinical Pharmacy III
  12. 2022, Graduate Education (Doctoral Program) , First Semester, Advanced seminar on Physiological Chemistry
  13. 2022, Graduate Education (Doctoral Program) , Second Semester, Advanced seminar on Physiological Chemistry
  14. 2022, Graduate Education (Doctoral Program) , First Semester, Advanced Seminar on Physiological Chemistry
  15. 2022, Graduate Education (Doctoral Program) , Second Semester, Advanced Seminar on Physiological Chemistry
  16. 2022, Graduate Education (Doctoral Program) , First Semester, Advanced Research on Physiological Chemistry
  17. 2022, Graduate Education (Doctoral Program) , Second Semester, Advanced Research on Physiological Chemistry
  18. 2022, Graduate Education (Master's Program) , First Semester, Lecture on Medicinal Science
  19. 2022, Graduate Education (Doctoral Program) , First Semester, Advanced Lecture on Medicinal Science
  20. 2022, Graduate Education (Master's Program) , First Semester, Seminar on Mechanisms of Signal Transduction
  21. 2022, Graduate Education (Master's Program) , Second Semester, Seminar on Mechanisms of Signal Transduction
  22. 2022, Graduate Education (Master's Program) , First Semester, Research on Mechanisms of Signal Transduction
  23. 2022, Graduate Education (Master's Program) , Second Semester, Research on Mechanisms of Signal Transduction
  24. 2022, Graduate Education (Doctoral Program) , 3Term, Trends of Genome Editing in Life Science

Research Activities

Academic Papers

  1. 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
  2. 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
  3. Effects of length and position of an extended linker on sequence-selective DNA recognition of zinc finger peptides., Biochemistry, 42(50), 2003
  4. Effects of linking 15-zinc finger domains on DNA binding specificity and multiple DNA binding modes., Bioorganic & medicinal chemistry letters, 15(9), 2005
  5. Design and synthesis of artificial zinc finger proteins., Methods in molecular biology (Clifton, N.J.), 352, 2007
  6. In vivo site-specific DNA methylation with a designed sequence-enabled DNA methylase., Journal of the American Chemical Society, 129(28), 2007
  7. Fluorophore labeling enables imaging and evaluation of specific CXCR4-ligand interaction at the cell membrane for fluorescence-based screening., Bioconjugate chemistry, 19(9), 2008
  8. Structure-activity relationship study of CXCR4 antagonists bearing the cyclic pentapeptide scaffold: identification of the new pharmacophore., Organic & biomolecular chemistry, 6(23), 2008
  9. 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
  10. 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
  11. Exploratory studies on development of the chemokine receptor CXCR4 antagonists toward downsizing., Perspectives in medicinal chemistry, 2, 2008
  12. Fluorogenically active leucine zipper peptides as tag-probe pairs for protein imaging in living cells., Angewandte Chemie (International ed. in English), 48(48), 2009
  13. CD4 mimics targeting the mechanism of HIV entry., Bioorganic & medicinal chemistry letters, 20(1), 2010
  14. Remodeling of dynamic structures of HIV-1 envelope proteins leads to synthetic antigen molecules inducing neutralizing antibodies., Bioconjugate chemistry, 21(4), 2010
  15. [Development of site-specific DNA methylase for epigenetic regulation of gene expression]., Seikagaku. The Journal of Japanese Biochemical Society, 82(5), 2010
  16. Development of crosslink-type tag-probe pairs for fluorescent imaging of proteins., Biopolymers, 94(6), 2010
  17. Peptide HIV-1 integrase inhibitors from HIV-1 gene products., Journal of medicinal chemistry, 53(14), 2010
  18. Peptidic HIV integrase inhibitors derived from HIV gene products: structure-activity relationship studies., Bioorganic & medicinal chemistry, 18(18), 2010
  19. CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist., Bioorganic & medicinal chemistry letters, 20(19), 2010
  20. Bivalent ligands of CXCR4 with rigid linkers for elucidation of the dimerization state in cells., Journal of the American Chemical Society, 132(45), 2010
  21. Fluorescent-responsive synthetic C1b domains of protein kinase Cδ as reporters of specific high-affinity ligand binding., Bioconjugate chemistry, 22(1), 2011
  22. Azamacrocyclic metal complexes as CXCR4 antagonists., ChemMedChem, 6(5), 2011
  23. Intense blue fluorescence in a leucine zipper assembly., Chembiochem : a European journal of chemical biology, 12(5), 2011
  24. Fluorescence-quenching screening of protein kinase C ligands with an environmentally sensitive fluorophore., Bioconjugate chemistry, 22(5), 2011
  25. Small molecular CD4 mimics as HIV entry inhibitors., Bioorganic & medicinal chemistry, 19(22), 2011
  26. Synthetic caged DAG-lactones for photochemically controlled activation of protein kinase C., Chembiochem : a European journal of chemical biology, 12(4), 2011
  27. A synthetic C34 trimer of HIV-1 gp41 shows significant increase in inhibition potency., ChemMedChem, 7(2), 2012
  28. Conjugation of cell-penetrating peptides leads to identification of anti-HIV peptides from matrix proteins., Bioorganic & medicinal chemistry, 20(4), 2012
  29. 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
  30. Evaluation of a synthetic C34 trimer of HIV-1 gp41 as AIDS vaccines., Bioorganic & medicinal chemistry, 20(10), 2012
  31. Pharmacophore-based small molecule CXCR4 ligands., Bioorganic & medicinal chemistry letters, 22(12), 2012
  32. The successes and failures of HIV drug discovery., Expert opinion on drug discovery, 6(10), 2011
  33. Low-molecular-weight CXCR4 ligands with variable spacers., ChemMedChem, 8(1), 2013
  34. A future perspective on the development of chemokine receptor CXCR4 antagonists., Expert opinion on drug discovery, 3(10), 2008
  35. CD4 mimics as HIV entry inhibitors: lead optimization studies of the aromatic substituents., Bioorganic & medicinal chemistry, 21(9), 2013
  36. Multimerized CHR-derived peptides as HIV-1 fusion inhibitors., Bioorganic & medicinal chemistry, 21(15), 2013
  37. Peptide-based ligand screening and functional analysis of protein kinase C., Biopolymers, 100(6), 2013
  38. Cell-permeable stapled peptides based on HIV-1 integrase inhibitors derived from HIV-1 gene products., ACS chemical biology, 8(10), 2013
  39. Anti-HIV-1 peptide derivatives based on the HIV-1 Co-receptor CXCR4., ChemMedChem, 8(10), 2013
  40. CXCR4-derived synthetic peptides inducing anti-HIV-1 antibodies., Bioorganic & medicinal chemistry, 21(22), 2013
  41. A CD4 mimic as an HIV entry inhibitor: pharmacokinetics., Bioorganic & medicinal chemistry, 21(24), 2013
  42. 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
  43. Screening for protein kinase C ligands using fluorescence resonance energy transfer., Chemical & pharmaceutical bulletin, 62(10), 2014
  44. [Chemical biology for pharmaceutical science--integrative approaches for elucidation of biological phenomena]., Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan, 135(3), 2015
  45. [Application and potential of genome engineering by artificial enzymes]., Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan, 135(3), 2015
  46. An in-cell fluorogenic Tag-probe system for protein dynamics imaging enabled by cell-penetrating peptides., Bioconjugate chemistry, 26(6), 2015
  47. 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
  48. Trivalent ligands for CXCR4 bearing polyproline linkers show specific recognition for cells with increased CXCR4 expression., Organic & biomolecular chemistry, 13(32), 2015
  49. Exploration of labeling by near infrared dyes of the polyproline linker for bivalent-type CXCR4 ligands., Bioorganic & medicinal chemistry, 23(21), 2015
  50. Utilization of the Heavy Atom Effect for the Development of a Photosensitive 8-Azacoumarin-Type Photolabile Protecting Group., Organic letters, 17(21), 2015
  51. Multimerized HIV-gp41-derived peptides as fusion inhibitors and vaccines., Biopolymers, 106(4), 2016
  52. A minimally cytotoxic CD4 mimic as an HIV entry inhibitor., Bioorganic & medicinal chemistry letters, 26(2), 2016
  53. Small-Molecule CD4 Mimics Containing Mono-cyclohexyl Moieties as HIV Entry Inhibitors., ChemMedChem, 11(8), 2016
  54. Functional evaluation of fluorescein-labeled derivatives of a peptide inhibitor of the EGF receptor dimerization., Bioorganic & medicinal chemistry, 24(16), 2016
  55. Development of anti-HIV peptides based on a viral capsid protein., Biopolymers, 108(1), 2017
  56. 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
  57. Microwave-Assisted Synthesis of Azacoumarin Fluorophores and the Fluorescence Characterization., The Journal of organic chemistry, 82(5), 2017
  58. Synthesis and Evaluation of Dimeric Derivatives of Diacylglycerol-Lactones as Protein Kinase C Ligands., Bioconjugate chemistry, 28(8), 2017
  59. Synthesis of a Chloroalkene Dipeptide Isostere-Containing Peptidomimetic and Its Biological Application., ACS medicinal chemistry letters, 9(1), 2018
  60. [ZIP tag-probe system: A fluorescence imaging tool for intercellular proteins]., Seikagaku. The Journal of Japanese Biochemical Society, 89(1), 2017
  61. 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
  62. Development of Toolboxes for Precision Genome/Epigenome Editing and Imaging of Epigenetics., Chemical record (New York, N.Y.), 18(12), 2018
  63. Efficient and Orthogonal Transcription Regulation by Chemically Inducible Artificial Transcription Factors., Biochemistry, 57(45), 2018
  64. 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
  65. Design, synthesis and biological evaluation of low molecular weight CXCR4 ligands., Bioorganic & medicinal chemistry, 27(6), 2019
  66. Dimeric C34 Derivatives Linked through Disulfide Bridges as New HIV-1 Fusion Inhibitors., Chembiochem : a European journal of chemical biology, 20(16), 2019
  67. Introducing "Future of Biochemistry 2020: The Asia-Pacific Issue", BIOCHEMISTRY, 59(1), 1-7, 2020
  68. ★, TALEN-Based Chemically Inducible, Dimerization-Dependent, Sequence-Specific Nucleases, Biochemistry, 59(2), 197-204, 20200121
  69. Synthesis of hydrophilic caged DAG-lactones for chemical biology applications, Organic and Biomolecular Chemistry, 18(22), 4217-4223, 20200614
  70. Development of a NanoBRET-Based Sensitive Screening Method for CXCR4 Ligands, BIOCONJUGATE CHEMISTRY, 30(5), 1442-1450, 2019
  71. A minimally cytotoxic CD4 mimic as an HIV entry inhibitor, Bioorganic and Medicinal Chemistry Letters, 26(2), 397-400, 20160115
  72. Small-Molecule CD4 Mimics Containing Mono-cyclohexyl Moieties as HIV Entry Inhibitors, ChemMedChem, 11(8), 940-946, 20160419
  73. Multimerized HIV-gp41-derived peptides as fusion inhibitors and vaccines, Biopolymers, 622-628, 20161104
  74. Development of anti-HIV peptides based on a viral capsid protein, Biopolymers, 108(1), 20170101
  75. Microwave-Assisted Synthesis of Azacoumarin Fluorophores and the Fluorescence Characterization, Journal of Organic Chemistry, 82(5), 2739-2744, 20170303
  76. 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
  77. Synthesis and Evaluation of Dimeric Derivatives of Diacylglycerol-Lactones as Protein Kinase C Ligands, Bioconjugate Chemistry, 28(8), 2135-2144, 20170816
  78. Creation of functional molecules based on biomolecular interactions; development toward chemical biology, Yakugaku Zasshi, 137(10), 1223-1231, 20170101
  79. ZIP tag-probe system: A fluorescence imaging tool for intercellular proteins, Seikagaku, 89(1), 115-120, 20170101
  80. Synthesis of a Chloroalkene Dipeptide Isostere-Containing Peptidomimetic and Its Biological Application, ACS Medicinal Chemistry Letters, 9(1), 7-11, 20180111
  81. 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
  82. Development of Toolboxes for Precision Genome/Epigenome Editing and Imaging of Epigenetics, Chemical Record, 18(12), 1717-1726, 20181201
  83. 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
  84. Efficient and Orthogonal Transcription Regulation by Chemically Inducible Artificial Transcription Factors, Biochemistry, 57(45), 6452-6459, 20181113
  85. 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
  86. Design, synthesis and biological evaluation of low molecular weight CXCR4 ligands, Bioorganic and Medicinal Chemistry, 27(6), 1130-1138, 20190315
  87. Development of a NanoBRET-based sensitive screening method for CXCR4 ligands, Bioconjugate Chemistry, 30(5), 1442-1450, 20190515
  88. Dimeric C34 Derivatives Linked through Disulfide Bridges as New HIV-1 Fusion Inhibitors, ChemBioChem, 20(16), 2101-2108, 20190101
  89. ★, A cell cycle-dependent CRISPR-Cas9 activation system based on an anti-CRISPR protein shows improved genome editing accuracy, Communications Biology, 3(1), 20201201
  90. Discovery of a Macropinocytosis-Inducing Peptide Potentiated by Medium-Mediated Intramolecular Disulfide Formation, ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 60(21), 11928-11936, 20210517
    Link to Paper Search Results by DOI
  91. ★, Molecular Switch Engineering for Precise Genome Editing, BIOCONJUGATE CHEMISTRY, 32(4), 639-648, 20210421
    Link to Paper Search Results by DOI

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