WATARU NOMURA

Last Updated :2024/04/03

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. 2024, Undergraduate Education, 2Term, Functional Morphology
  2. 2024, Undergraduate Education, 2Term, Biological Chemistry IV
  3. 2024, Undergraduate Education, 3Term, Introduction to Pharmaceutical Sciences
  4. 2024, Undergraduate Education, First Semester, Research Practice A
  5. 2024, Undergraduate Education, Second Semester, Research Practice B
  6. 2024, Undergraduate Education, First Semester, Practice of Biochemical Pharmacology
  7. 2024, Undergraduate Education, 2Term, Physiological Chemistry
  8. 2024, Undergraduate Education, 3Term, Japanese Pharmacopoeia
  9. 2024, Undergraduate Education, Second Semester, Experiments of Biological Chemistry
  10. 2024, Undergraduate Education, Year, Special laboratory Works in Pharmaceutical Sciences I
  11. 2024, Undergraduate Education, Year, Special laboratory Works in Pharmaceutical Sciences II
  12. 2024, Undergraduate Education, Second Semester, Special laboratory Works in Pharmaceutical Sciences III
  13. 2024, Undergraduate Education, Year, Special laboratory Works in Clinical Pharmacy I
  14. 2024, Undergraduate Education, Year, Special laboratory Works in Clinical Pharmacy II
  15. 2024, Undergraduate Education, Year, Special laboratory Works in Clinical Pharmacy III
  16. 2024, Graduate Education (Doctoral Program) , First Semester, Advanced Seminar on Physiological Chemistry
  17. 2024, Graduate Education (Doctoral Program) , Second Semester, Advanced Seminar on Physiological Chemistry
  18. 2024, Graduate Education (Doctoral Program) , First Semester, Advanced Research on Physiological Chemistry
  19. 2024, Graduate Education (Doctoral Program) , Second Semester, Advanced Research on Physiological Chemistry
  20. 2024, Graduate Education (Master's Program) , First Semester, Lecture on Medicinal Science
  21. 2024, Graduate Education (Doctoral Program) , First Semester, Advanced Lecture on Medicinal Science
  22. 2024, Graduate Education (Master's Program) , First Semester, Seminar on Mechanisms of Signal Transduction
  23. 2024, Graduate Education (Master's Program) , Second Semester, Seminar on Mechanisms of Signal Transduction
  24. 2024, Graduate Education (Master's Program) , First Semester, Research on Mechanisms of Signal Transduction
  25. 2024, Graduate Education (Master's Program) , Second Semester, Research on Mechanisms of Signal Transduction
  26. 2024, Graduate Education (Doctoral Program) , First Semester, Advanced Seminar on Physiological Chemistry for Medicinal Sciences
  27. 2024, Graduate Education (Doctoral Program) , Second Semester, Advanced Seminar on Physiological Chemistry for Medicinal Sciences
  28. 2024, Graduate Education (Doctoral Program) , First Semester, Advanced Research on Physiological Chemistry for Medicinal Sciences
  29. 2024, Graduate Education (Doctoral Program) , Second Semester, Advanced Research on Physiological Chemistry for Medicinal Sciences
  30. 2024, Graduate Education (Doctoral Program) , 3Term, Trends of Genome Editing in Life Science

Research Activities

Academic Papers

  1. Development of the 8-aza-3-bromo-7-hydroxycoumarin-4-ylmethyl group as a new entry of photolabile protecting groups, Tetrahedron, 70(29), 4400-4404, 20140722
  2. Development of a fluoride-responsive amide bond cleavage device that is potentially applicable to a traceable linker, Tetrahedron, 70(34), 5122-5127, 20140826
  3. Development of site-specific DNA methylase for epigenetic regulation of gene expression, Seikagaku, 82(5), 393-397, 20101201
  4. Significant effect of linker sequence on DNA recognition by multi-zinc finger protein, Biochemical and Biophysical Research Communications, 282(4), 1001-1007, 20010101
  5. Multiconnection of identical zinc finger: Implication for DNA binding affinity and unit modulation of the three zinc finger domain, Biochemistry, 40(9), 2932-2941, 20010306
  6. 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
  7. 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
  8. Effects of length and position of an extended linker on sequence-selective DNA recognition of zinc finger peptides., Biochemistry, 42(50), 2003
  9. Effects of linking 15-zinc finger domains on DNA binding specificity and multiple DNA binding modes., Bioorganic & medicinal chemistry letters, 15(9), 2005
  10. Design and synthesis of artificial zinc finger proteins., Methods in molecular biology (Clifton, N.J.), 352, 2007
  11. In vivo site-specific DNA methylation with a designed sequence-enabled DNA methylase., Journal of the American Chemical Society, 129(28), 2007
  12. Fluorophore labeling enables imaging and evaluation of specific CXCR4-ligand interaction at the cell membrane for fluorescence-based screening., Bioconjugate chemistry, 19(9), 2008
  13. Structure-activity relationship study of CXCR4 antagonists bearing the cyclic pentapeptide scaffold: identification of the new pharmacophore., Organic & biomolecular chemistry, 6(23), 2008
  14. 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
  15. 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
  16. Exploratory studies on development of the chemokine receptor CXCR4 antagonists toward downsizing., Perspectives in medicinal chemistry, 2, 2008
  17. Fluorogenically active leucine zipper peptides as tag-probe pairs for protein imaging in living cells., Angewandte Chemie (International ed. in English), 48(48), 2009
  18. CD4 mimics targeting the mechanism of HIV entry., Bioorganic & medicinal chemistry letters, 20(1), 2010
  19. Remodeling of dynamic structures of HIV-1 envelope proteins leads to synthetic antigen molecules inducing neutralizing antibodies., Bioconjugate chemistry, 21(4), 2010
  20. [Development of site-specific DNA methylase for epigenetic regulation of gene expression]., Seikagaku. The Journal of Japanese Biochemical Society, 82(5), 2010
  21. Development of crosslink-type tag-probe pairs for fluorescent imaging of proteins., Biopolymers, 94(6), 2010
  22. Peptide HIV-1 integrase inhibitors from HIV-1 gene products., Journal of medicinal chemistry, 53(14), 2010
  23. Peptidic HIV integrase inhibitors derived from HIV gene products: structure-activity relationship studies., Bioorganic & medicinal chemistry, 18(18), 2010
  24. CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist., Bioorganic & medicinal chemistry letters, 20(19), 2010
  25. Bivalent ligands of CXCR4 with rigid linkers for elucidation of the dimerization state in cells., Journal of the American Chemical Society, 132(45), 2010
  26. Fluorescent-responsive synthetic C1b domains of protein kinase Cδ as reporters of specific high-affinity ligand binding., Bioconjugate chemistry, 22(1), 2011
  27. Azamacrocyclic metal complexes as CXCR4 antagonists., ChemMedChem, 6(5), 2011
  28. Intense blue fluorescence in a leucine zipper assembly., Chembiochem : a European journal of chemical biology, 12(5), 2011
  29. Fluorescence-quenching screening of protein kinase C ligands with an environmentally sensitive fluorophore., Bioconjugate chemistry, 22(5), 2011
  30. Small molecular CD4 mimics as HIV entry inhibitors., Bioorganic & medicinal chemistry, 19(22), 2011
  31. Synthetic caged DAG-lactones for photochemically controlled activation of protein kinase C., Chembiochem : a European journal of chemical biology, 12(4), 2011
  32. A synthetic C34 trimer of HIV-1 gp41 shows significant increase in inhibition potency., ChemMedChem, 7(2), 2012
  33. Conjugation of cell-penetrating peptides leads to identification of anti-HIV peptides from matrix proteins., Bioorganic & medicinal chemistry, 20(4), 2012
  34. 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
  35. Evaluation of a synthetic C34 trimer of HIV-1 gp41 as AIDS vaccines., Bioorganic & medicinal chemistry, 20(10), 2012
  36. Pharmacophore-based small molecule CXCR4 ligands., Bioorganic & medicinal chemistry letters, 22(12), 2012
  37. The successes and failures of HIV drug discovery., Expert opinion on drug discovery, 6(10), 2011
  38. Low-molecular-weight CXCR4 ligands with variable spacers., ChemMedChem, 8(1), 2013
  39. A future perspective on the development of chemokine receptor CXCR4 antagonists., Expert opinion on drug discovery, 3(10), 2008
  40. CD4 mimics as HIV entry inhibitors: lead optimization studies of the aromatic substituents., Bioorganic & medicinal chemistry, 21(9), 2013
  41. Multimerized CHR-derived peptides as HIV-1 fusion inhibitors., Bioorganic & medicinal chemistry, 21(15), 2013
  42. Peptide-based ligand screening and functional analysis of protein kinase C., Biopolymers, 100(6), 2013
  43. Cell-permeable stapled peptides based on HIV-1 integrase inhibitors derived from HIV-1 gene products., ACS chemical biology, 8(10), 2013
  44. Anti-HIV-1 peptide derivatives based on the HIV-1 Co-receptor CXCR4., ChemMedChem, 8(10), 2013
  45. CXCR4-derived synthetic peptides inducing anti-HIV-1 antibodies., Bioorganic & medicinal chemistry, 21(22), 2013
  46. A CD4 mimic as an HIV entry inhibitor: pharmacokinetics., Bioorganic & medicinal chemistry, 21(24), 2013
  47. 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
  48. Screening for protein kinase C ligands using fluorescence resonance energy transfer., Chemical & pharmaceutical bulletin, 62(10), 2014
  49. [Chemical biology for pharmaceutical science--integrative approaches for elucidation of biological phenomena]., Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan, 135(3), 2015
  50. [Application and potential of genome engineering by artificial enzymes]., Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan, 135(3), 2015
  51. An in-cell fluorogenic Tag-probe system for protein dynamics imaging enabled by cell-penetrating peptides., Bioconjugate chemistry, 26(6), 2015
  52. 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
  53. Trivalent ligands for CXCR4 bearing polyproline linkers show specific recognition for cells with increased CXCR4 expression., Organic & biomolecular chemistry, 13(32), 2015
  54. Exploration of labeling by near infrared dyes of the polyproline linker for bivalent-type CXCR4 ligands., Bioorganic & medicinal chemistry, 23(21), 2015
  55. Utilization of the Heavy Atom Effect for the Development of a Photosensitive 8-Azacoumarin-Type Photolabile Protecting Group., Organic letters, 17(21), 2015
  56. Multimerized HIV-gp41-derived peptides as fusion inhibitors and vaccines., Biopolymers, 106(4), 2016
  57. A minimally cytotoxic CD4 mimic as an HIV entry inhibitor., Bioorganic & medicinal chemistry letters, 26(2), 2016
  58. Small-Molecule CD4 Mimics Containing Mono-cyclohexyl Moieties as HIV Entry Inhibitors., ChemMedChem, 11(8), 2016
  59. Functional evaluation of fluorescein-labeled derivatives of a peptide inhibitor of the EGF receptor dimerization., Bioorganic & medicinal chemistry, 24(16), 2016
  60. Development of anti-HIV peptides based on a viral capsid protein., Biopolymers, 108(1), 2017
  61. 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
  62. Microwave-Assisted Synthesis of Azacoumarin Fluorophores and the Fluorescence Characterization., The Journal of organic chemistry, 82(5), 2017
  63. Synthesis and Evaluation of Dimeric Derivatives of Diacylglycerol-Lactones as Protein Kinase C Ligands., Bioconjugate chemistry, 28(8), 2017
  64. Synthesis of a Chloroalkene Dipeptide Isostere-Containing Peptidomimetic and Its Biological Application., ACS medicinal chemistry letters, 9(1), 2018
  65. [ZIP tag-probe system: A fluorescence imaging tool for intercellular proteins]., Seikagaku. The Journal of Japanese Biochemical Society, 89(1), 2017
  66. 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
  67. Development of Toolboxes for Precision Genome/Epigenome Editing and Imaging of Epigenetics., Chemical record (New York, N.Y.), 18(12), 2018
  68. Efficient and Orthogonal Transcription Regulation by Chemically Inducible Artificial Transcription Factors., Biochemistry, 57(45), 2018
  69. 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
  70. Design, synthesis and biological evaluation of low molecular weight CXCR4 ligands., Bioorganic & medicinal chemistry, 27(6), 2019
  71. Dimeric C34 Derivatives Linked through Disulfide Bridges as New HIV-1 Fusion Inhibitors., Chembiochem : a European journal of chemical biology, 20(16), 2019
  72. Introducing "Future of Biochemistry 2020: The Asia-Pacific Issue", BIOCHEMISTRY, 59(1), 1-7, 2020
  73. ★, TALEN-Based Chemically Inducible, Dimerization-Dependent, Sequence-Specific Nucleases, Biochemistry, 59(2), 197-204, 20200121
  74. Synthesis of hydrophilic caged DAG-lactones for chemical biology applications, Organic and Biomolecular Chemistry, 18(22), 4217-4223, 20200614
  75. Development of a NanoBRET-Based Sensitive Screening Method for CXCR4 Ligands, BIOCONJUGATE CHEMISTRY, 30(5), 1442-1450, 2019
  76. A minimally cytotoxic CD4 mimic as an HIV entry inhibitor, Bioorganic and Medicinal Chemistry Letters, 26(2), 397-400, 20160115
  77. Small-Molecule CD4 Mimics Containing Mono-cyclohexyl Moieties as HIV Entry Inhibitors, ChemMedChem, 11(8), 940-946, 20160419
  78. Multimerized HIV-gp41-derived peptides as fusion inhibitors and vaccines, Biopolymers, 622-628, 20161104
  79. Development of anti-HIV peptides based on a viral capsid protein, Biopolymers, 108(1), 20170101
  80. Microwave-Assisted Synthesis of Azacoumarin Fluorophores and the Fluorescence Characterization, Journal of Organic Chemistry, 82(5), 2739-2744, 20170303
  81. 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
  82. Synthesis and Evaluation of Dimeric Derivatives of Diacylglycerol-Lactones as Protein Kinase C Ligands, Bioconjugate Chemistry, 28(8), 2135-2144, 20170816
  83. Creation of functional molecules based on biomolecular interactions; development toward chemical biology, Yakugaku Zasshi, 137(10), 1223-1231, 20170101
  84. ZIP tag-probe system: A fluorescence imaging tool for intercellular proteins, Seikagaku, 89(1), 115-120, 20170101
  85. Synthesis of a Chloroalkene Dipeptide Isostere-Containing Peptidomimetic and Its Biological Application, ACS Medicinal Chemistry Letters, 9(1), 7-11, 20180111
  86. 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
  87. Development of Toolboxes for Precision Genome/Epigenome Editing and Imaging of Epigenetics, Chemical Record, 18(12), 1717-1726, 20181201
  88. 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
  89. Efficient and Orthogonal Transcription Regulation by Chemically Inducible Artificial Transcription Factors, Biochemistry, 57(45), 6452-6459, 20181113
  90. 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
  91. Design, synthesis and biological evaluation of low molecular weight CXCR4 ligands, Bioorganic and Medicinal Chemistry, 27(6), 1130-1138, 20190315
  92. Development of a NanoBRET-based sensitive screening method for CXCR4 ligands, Bioconjugate Chemistry, 30(5), 1442-1450, 20190515
  93. Dimeric C34 Derivatives Linked through Disulfide Bridges as New HIV-1 Fusion Inhibitors, ChemBioChem, 20(16), 2101-2108, 20190101
  94. ★, A cell cycle-dependent CRISPR-Cas9 activation system based on an anti-CRISPR protein shows improved genome editing accuracy, Communications Biology, 3(1), 20201201
  95. 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
  96. ★, Molecular Switch Engineering for Precise Genome Editing, BIOCONJUGATE CHEMISTRY, 32(4), 639-648, 20210421
    Link to Paper Search Results by DOI
  97. Fluorescence resonance energy transfer-based screening for protein kinase C ligands using 6-methoxynaphthalene-labeled 1,2-diacylglycerol-lactones, ORGANIC & BIOMOLECULAR CHEMISTRY, 19(38), 8264-8271, 20211006
    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