Development of anti-HIV agents using chemical genomics based on viral self-regulation mechanism

• Project/Area Number: 22659021
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Single-year Grants
• Research Field: Drug development chemistry
• Research Institution: Tokyo Medical and Dental University
• Principal Investigator: TAMAMURA Hirokazu 東京医科歯科大学, 生体材料工学研究所, 教授 (80217182)
• Project Period (FY): 2010 – 2011
• Project Status: Completed (Fiscal Year 2011)
• Budget Amount: ¥3,000,000 (Direct Cost: ¥2,700,000、Indirect Cost: ¥300,000); Fiscal Year 2011: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000); Fiscal Year 2010: ¥1,700,000 (Direct Cost: ¥1,700,000)
• Keywords: インテグラーゼ阻害剤 / マトリックス蛋白 / CD4ミミック / アンタゴニスト / HIV / CXCR4

Research Abstract

Several anti-HIV agents have been developed using forward and reverse chemical gemomics. 1) Helical mimetics and staple peptides of Vpr-fragments were synthesized and found to have potent integrase inhibitory activity. 2) Several matrix fragments with cell membrane penetrating signal having anti-HIV activity were developed. 3) Novel CD4 mimic derivatives having potent anti-HIV activity which cause conformational change of gp120 were found. 4) New CXCR4 antagonists with xylene scaffold were developed.

Research Products

• [Journal Article] Development of Anti-HIV Agents Based on Chemical Biology (2012)
  • Author(s): 玉村啓和
  • Journal Title: YAKUGAKU ZASSHI Volume: 132 Issue: 1 Pages: 69-78
  • DOI: 10.1248/yakushi.132.69
  • NAID: 130001871964
  • ISSN: 0031-6903, 1347-5231
  • Year and Date: 2012-01-01
  • Peer Reviewed
• [Journal Article] Pharmacophore-basedSmall Molecule CXCR4 Ligand (2012)
  • Author(s): Narumi T, Nomura W, Tamamura H(他8人、11番目)
  • Journal Title: Bioorg. Med. Chem. Lett Volume: (in press)
  • Peer Reviewed
• [Journal Article] Evaluation of aSynthetic C34 Trimer of HIV-1 gp41 asAIDS Vaccines (2012)
  • Author(s): Hashimoto C, Nomura W, Tamamura H(他7人、10番目)
  • Journal Title: Bioorg. Med. Chem Volume: (in press)
  • Peer Reviewed
• [Journal Article] ケミカルバイオロジーを基盤とした抗HIV剤の創製 (2012)
  • Author(s): 玉村啓和(他0人、1番目)
  • Journal Title: 薬学雑誌(日本薬学会) Volume: 31(1)巻 Pages: 69-78
  • NAID: 130001871964
• [Journal Article] Synthetic C34Trimer of HIV-1 gp41 Shows Significant Increase of Inhibition Potency (2012)
  • Author(s): Nomura W, Yamamoto N, Tamamura H(他8人、11番目)
  • Journal Title: Chem Med Chem Volume: 7巻 Pages: 205-208
  • Peer Reviewed
• [Journal Article] Conjugation of Cell-penetrating Peptides Leads to Identification of Anti-HIV Peptidesfrom Matrix Proteins (2012)
  • Author(s): Narumi T, Nomura W, Tamamura H(他8人、11番目)
  • Journal Title: Bioorg. Med. Chem Volume: 20巻 Pages: 1468-1474
  • Peer Reviewed
• [Journal Article] Effects of DNABinding of Zinc Finger and Linkers for Domain Fusion on Catalytic Activity of Sequence-Specific Chimeric Recombinases Determined by a Facile Fluorescent System (2012)
  • Author(s): Nomura W, Yamamoto N, Tamamura H(他5人、8番目)
  • Journal Title: Fluorescent System Pages: 1510-1517
  • Peer Reviewed
• [Journal Article] Evaluation of a Synthetic C34 Trimer of HIV-1 gp41 as AIDS Vaccines (2012)
  • Author(s): Hashimoto, C., Nomura, W., Ohya, A., Urano, E., Miyauchi, K., Narumi, T., Aikawa, H., Komano, J.A., Yamamoto, N., Tamamura, H.
  • Journal Title: Bioorg.Med.Chem. Volume: (in press) Issue: 10 Pages: 3287-3291
  • DOI: 10.1016/j.bmc.2012.03.050
  • Peer Reviewed
• [Journal Article] Effects of DNA Binding of Zinc Finger and Linkers for Domain Fusion on Catalytic Activity of Sequence-Specific Chimeric Recombinases Determined by a Facile Fluorescent System (2012)
  • Author(s): Nomura, W., Masuda, A., Ohba, K., Urabe, A., Ito, N., Ryo, A., Yamamoto, N., Tamamura, H.
  • Journal Title: Biochemistry Volume: 51 Issue: 7 Pages: 1510-1517
  • DOI: 10.1021/bi201878x
  • Peer Reviewed
• [Journal Article] Synthetic C34 Trimer of HIV-1 gp41 Shows Significant Increase of Inhibition Potency (2012)
  • Author(s): W.Nomura, T.Tanaka, et.al.
  • Journal Title: Chem Med Chem Volume: 7 Issue: 2 Pages: 205-208
  • DOI: 10.1002/cmdc.201100542
  • Peer Reviewed
• [Journal Article] Conjugation of Cell-penetrating Peptides Leads to Identification of Anti-HIV Peptides from Matrix Proteins (2012)
  • Author(s): T.Narumi, T.Tanaka, et al
  • Journal Title: Biochemistry & Medicinal Chemistry Volume: 20 Issue: 4 Pages: 1468-1474
  • DOI: 10.1016/j.bmc.2011.12.055
  • Peer Reviewed
• [Journal Article] Small Molecular CD4Mimics as HIV Entry Inhibitors (2011)
  • Author(s): T. Narumi, W. Nomura, H. Tamamura(他4人、7番目)
  • Journal Title: Bioorg. Med. Chem. Volume: 19巻 Pages: 6735-6742
  • Peer Reviewed
• [Journal Article] The Successand Failures of HIV Drug Discovery (2011)
  • Author(s): C. Hashimoto, W. Nomura, H. Tamamura(他2人、5番目)
  • Journal Title: Expert Opin. Drug Discovery Volume: 6巻 Pages: 1067-1090
  • Peer Reviewed
• [Journal Article] Azamacrocyclic-metal Complexes as CXCR4 Antagonists (2011)
  • Author(s): T. Tanaka, W. Nomura, N. Yamamoto, H. Tamamura(他7人、11番目)
  • Journal Title: Chem Med Chem Volume: 6巻 Pages: 834-839
  • Peer Reviewed
• [Journal Article] Fluorescence-Quenching Screening of Protein Kinase C Ligands with an Environmentally Sensitive Fluorophore (2011)
  • Author(s): W. Nomura, H. Tamamura(他5人、7番目)
  • Journal Title: Bioconjugate Chem Volume: 22巻 Pages: 923-930
  • Peer Reviewed
• [Journal Article] Synthetic Caged DAG-lactones for Photochemically-controlled Activation of Protein Kinase C (2011)
  • Author(s): W. Nomura, T. H. Tamamura(他6人、8番目)
  • Journal Title: Chem Bio Chem Volume: 12巻 Pages: 535-539
  • Peer Reviewed
• [Journal Article] Fluorescent-responsive Synthetic C1b Domains of ProteinKinase Cδas Reporters of Specific High Affinity Ligand Binding (2011)
  • Author(s): N. Ohashi, W. Nomura, H. Tamamura(他4人、7番目)
  • Journal Title: Bioconjugate Chem Volume: 22巻 Pages: 82-87
  • Peer Reviewed
• [Journal Article] Intense Blue Fluorescence in a Leucine Zipper Assembly (2011)
  • Author(s): H. Tsutsumi, W. Nomura, H. Tamamura(他2人、5番目)
  • Journal Title: Chem Bio Chem Volume: 12巻 Pages: 691-694
  • Peer Reviewed
• [Journal Article] Fluorescence-Quenching Screening of Protein Kinase C Ligands with an Environ mentally Sensitive Fluorophore (2011)
  • Author(s): Nomura, Wataru
  • Journal Title: Bioconjugate Chem Volume: VOL.22 Issue: 5 Pages: 923-930
  • DOI: 10.1021/bc100567k
  • Peer Reviewed
• [Journal Article] Azamacrocyclic-metal Complexes as CXCR4 Antagonists (2011)
  • Author(s): T.Tanaka, et.al.
  • Journal Title: ChemMedChem Volume: 6 Issue: 5 Pages: 834-839
  • DOI: 10.1002/cmdc.201000548
  • Peer Reviewed
• [Journal Article] Intense blue fluorescence in a leucine zipper assembly (2011)
  • Author(s): Tsutsumi H, Abe S, Mino T, Nomura W, Tamamura H
  • Journal Title: ChemBioChem Volume: 12 Issue: 5 Pages: 691-694
  • DOI: 10.1002/cbic.201000692
  • Peer Reviewed
• [Journal Article] Synthetic Caged DAG-lactones for Photochemically-controlled Activation of Protein Kinase C (2011)
  • Author(s): Nomura, Wataru
  • Journal Title: ChemBioChem Volume: VOL.12 Issue: 4 Pages: 535-539
  • DOI: 10.1002/cbic.201000670
  • Peer Reviewed
• [Journal Article] Fluorescent-responsive Synthetic C1b Domains of Protein Kinase Cδ as Reporters of Specific High Affinity Ligand Binding (2011)
  • Author(s): Ohashi N, Nomura W, Tamamura H, et al.
  • Journal Title: Bioconjugate Chem Volume: 22 Issue: 1 Pages: 82-87
  • DOI: 10.1021/bc100414a
  • Peer Reviewed
• [Journal Article] Small Molecular CD4 Mimics as HIV Entry Inhibitors (2011)
  • Author(s): Narumi T, Nomura W, Matsushita S, Tamamura H, et al.
  • Journal Title: Bioorg Med Chem Volume: 19 Issue: 22 Pages: 6735-6742
  • DOI: 10.1016/j.bmc.2011.09.045
  • Peer Reviewed
• [Journal Article] The Success and Failures of HIV Drug Discovery (2011)
  • Author(s): C.Hashimoto, T.Tanaka, et.al.
  • Journal Title: Expert Opinion in Drug Discovery Volume: 6 Issue: 10 Pages: 1067-1090
  • DOI: 10.1517/17460441.2011.611129
  • Peer Reviewed
• [Journal Article] HIV-1 gp120 Enhances Outward Potassium Current via CXCR4 and cAMP-Dependent Protein Kinase a Signaling in Cultured Rat Microglia (2011)
  • Author(s): Xu C, Liu J, Chen L, Liang S, Fujii N, Tamamura H, Xiong H
  • Journal Title: Glia Volume: 59 Issue: 6 Pages: 997-1007
  • DOI: 10.1002/glia.21171
  • Peer Reviewed
• [Journal Article] The Increase in Surface CXCR4 Expression on Lung Extravascular Neutrophils and its Effects on Neutrophils During Endotoxin-Induced Lung Injury (2011)
  • Author(s): Yamada M, Kitagawa M, Yano H, Tamamura H, Fujii N, Kaku M, et al.
  • Journal Title: Cell Mol Immunol Volume: 8 Issue: 4 Pages: 305-314
  • DOI: 10.1038/cmi.2011.8
  • Peer Reviewed
• [Journal Article] Fluorescence-Quenching Screening of Protein Kinase C Ligands withan Environmentally Sensitive Fluorophore (2011)
  • Author(s): Nomura W, Ikura T, Ito N, Tamamura H
  • Journal Title: Bioconjugate Chem Volume: (in press)
  • Peer Reviewed
• [Journal Article] Azamacrocyclic-metal Complexes as CXCR4 Antagonists (2011)
  • Author(s): Tanaka T, Nomura W, Murakami T, Yamamoto N , Tamamura H, et al.
  • Journal Title: ChemMedChem Volume: (in press)
  • Peer Reviewed
• [Journal Article] Synthetic Caged DAG-lactones for Photochemically-controlled Activation of Protein Kinase C (2011)
  • Author(s): Nomura W, Lewin NE, Blumberg PM, Furuta T, Tamamura H, et al.
  • Journal Title: ChemBioChem Volume: (in press)
  • Peer Reviewed
• [Journal Article] Fluorescent-responsive Synthetic Clb Domains of Protein Kinase Cδ as Reporters of Specific High Affinity Ligand Binding (2011)
  • Author(s): Ohashi N, Nomura W, Tamamura H, et al.
  • Journal Title: Bioconjugate Chem Volume: 22 Pages: 82-87
  • Peer Reviewed
• [Journal Article] Peptidic HIV integrase inhibitors derived from HIV gene products: Structure-activity relationship studies (2011)
  • Author(s): Suzuki S, Yamamoto N, Pommier Y, Nomura W, Tamamura H, et al.
  • Journal Title: Bioorg Med Chem Volume: 18 Pages: 6771-6775
  • Peer Reviewed
• [Journal Article] Development of Crosslink-Type Tag-Probe Pairs for Fluorescent Imaging of Proteins (2010)
  • Author(s): W. Nomura, H. Tamamura(他6人、8番目)
  • Journal Title: Biopolymers Volume: 94巻 Pages: 843-852
  • Peer Reviewed
• [Journal Article] Peptide HIV-1 Integrase Inhibitors from HIV-1 Gene Products (2010)
  • Author(s): S. Suzuki, E. W. Nomura, H. Tamamura(他19人、22番目)
  • Journal Title: J. Med. Chem Volume: 53(14)巻 Pages: 5356-5360
  • Peer Reviewed
• [Journal Article] Peptidic HIV Integrase Inhibitors Derived from HIV Gene Products : Structure-Activity Relationship Studies (2010)
  • Author(s): S. Suzuki, W. Nomura, N. Yamamoto, H. Tamamura(他11人、15番目)
  • Journal Title: Bioorg. Med. Chem Volume: 18巻 Pages: 6771-6775
  • Peer Reviewed
• [Journal Article] CD4Mimics Targeting the HIV Entry Mechanism and their Hybrid Moleculeswith a CXCR4 Antagonist (2010)
  • Author(s): T. Narumi, W. Nomura, H. Arai, T. Ozaki, N. Ohashi, S. Matsushita, H. Tamamura(他4人、11番目)
  • Journal Title: Bioorg. Med. Chem. Lett Volume: 20巻 Pages: 5853-5858
  • Peer Reviewed
• [Journal Article] Remodeling of Dynamic Structures of HIV-1 Envelope Proteins Leads to Synthetic Antigen Molecules Inducing Neutralizing Antibodies (2010)
  • Author(s): T. Nakahara, W. Nomura, T. Narumi, N. Yamamoto, H. Tamamura(他5人、10番目)
  • Journal Title: Bioconjugate Chem Volume: 21(4)巻 Pages: 709-714
  • Peer Reviewed
• [Journal Article] CD4 Mimics Targetingthe Mechanism of HIV (2010)
  • Author(s): Y. Yamada, W. Nomura, H. Tamamura(他7人、10番目)
  • Journal Title: Bioorg. Med. Chem. Lett Volume: 20巻 Pages: 354-358
  • Peer Reviewed
• [Journal Article] ペプチドミメティックによる創薬研究 (2010)
  • Author(s): 鳴海哲夫、玉村啓和(他0人、2番目)
  • Journal Title: 生化学特集号 Volume: 82巻6号 Pages: 515-523
  • NAID: 10026900008
• [Journal Article] エピジェネティクな遺伝子発現制御のためのDNAメチル化酵素の創製 (2010)
  • Author(s): 野村渉、玉村啓和(他1人、3番目)
  • Journal Title: 生化学ミニレビュウ Volume: 82巻5号 Pages: 393-397
  • NAID: 10026425888
• [Journal Article] CD4 mimics targeting the mechanism of HIV (2010)
  • Author(s): Yamada Y, Nomura W, Matsushita S, Tamamura H, et al.
  • Journal Title: Bioorg Med Chem Lett Volume: 20 Pages: 354-358
  • Peer Reviewed
• [Journal Article] Remodeling of dynamic structures of HIV-1 envelope proteins leads to synthetic antigen molecules inducing neutralizing antibodies (2010)
  • Author(s): Nakahara T, Nomura W, Yamamoto N, Tamamura H, et al.
  • Journal Title: Bioconjugate Chem Volume: 21(4) Pages: 709-714
  • Peer Reviewed
• [Journal Article] Induction of myogenic differentiation by SDF-1 via CXCR4 andCXCR7 receptors (2010)
  • Author(s): Melchionna R, Carlo AD, Fujii N, Tamamura H, Napolitano CM, Germani A, et al.
  • Journal Title: Muscle Nerve Volume: 41(6) Pages: 828-835
  • Peer Reviewed
• [Journal Article] Enhanced exposure of human immunodeficiency virus type 1 primary isolate neutralization epitopes through binding of CD4 mimetic compounds (2010)
  • Author(s): Yoshimura K, Tamamura H, Matsushita S, et al.
  • Journal Title: J Virol Volume: 84(15) Pages: 7558-7568
  • Peer Reviewed
• [Journal Article] Peptide HIV-1 integrase inhibitors from HIV-1 gene products (2010)
  • Author(s): Suzuki S, Yamamoto N, Tamamura H, et al.
  • Journal Title: J Med Chem Volume: 53(14) Pages: 5356-5360
  • Peer Reviewed
• [Journal Article] CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist (2010)
  • Author(s): Narumi T, Nomura W, Matsushita S, Tamamura H, et al.
  • Journal Title: Bioorg Med Chem Lett Volume: 20 Pages: 5853-5858
  • Peer Reviewed
• [Journal Article] Bivalent ligands of CXCR4 with rigid linkers for elucidation of dimerization state in cells (2010)
  • Author(s): Tanaka T, Nomura W, Narumi T, Masuda A, Tamamura H
  • Journal Title: J Am Chem Soc Volume: 132(45) Pages: 15899-15901
  • Peer Reviewed
• [Journal Article] Development of Crosslink-Type Tag-Probe Pairs for Fluorescent Imaging of Proteins (2010)
  • Author(s): Nomura W, Tsutsumi H, Tamamura H, et al.
  • Journal Title: Biopolymers : Peptide Science Volume: 94 Pages: 843-852
  • Peer Reviewed
• [Journal Article] Improvement of lentiviral vector-mediated gene transduction bygenetic engineering of the structural protein Pr55Gag (2010)
  • Author(s): Aoki T, Tamamura H, Yamamoto N, Komano J, et al.
  • Journal Title: Gene Ther Volume: 17(9) Pages: 1124-1133
  • Peer Reviewed
• [Journal Article] Fluorogenically Active Leucine Zipper Peptides as New Tag-Probe Pairs for Protein Imaging in Living Cells (2009)
  • Author(s): H. Tsutsumi, W. Nomura, H. Tamamura(他8人、11番目)
  • Journal Title: Angew. Chem., Int. Ed Volume: 48巻 Pages: 9164-9166
  • Peer Reviewed
• [Journal Article] A NewClass of Vitamin D Analogues that Induce Structural Rearrangement of the Ligand-Binding Pocket of the Receptor (2009)
  • Author(s): Y. Inaba, N. H. Tamamura, K. Yamamoto(他6人、6番目)
  • Journal Title: J. Med. Chem Volume: 52(5)巻 Pages: 1438-1449
  • Peer Reviewed
• [Journal Article] Structure-Activity Relationship Study on Artificial CXCR4 Ligands Possessing the Cyclic Pentapeptide Scaffold : the Exploration of AminoAcid Residues of Pentapeptides by Substitutions of Several Aromatic Amino Acids (2009)
  • Author(s): T. Tanaka, W. Nomura, H. Tamamura(他9人、12番目)
  • Journal Title: Org. Biomol. Chem Volume: 7巻 Pages: 3805-3809
  • Peer Reviewed
• [Journal Article] Synthesis of Protein Kinase CδC1b Domain by Native Chemical Ligation Methodologyand Characterization of its Folding andLigand Binding (2009)
  • Author(s): N. Ohashi, W. Nomura, H. Tamamura(他4人、7番目)
  • Journal Title: J. Pept. Sci Volume: 15(10)巻 Pages: 642-646
  • Peer Reviewed
• [Journal Article] 種々の作用点をターゲットとした抗HIV剤の創製 (2009)
  • Author(s): 玉村啓和(他0人、1番目)
  • Journal Title: 日本エイズ学会誌 Volume: 11巻2号 Pages: 100-101
• [Presentation] ペプチド化学を基盤としたケミカルバイオロジー (2011)
  • Author(s): 玉村啓和
  • Organizer: 第14回ペプチドフォーラム
  • Place of Presentation: 鹿児島
  • Year and Date: 2011-12-16
• [Presentation] Vpr由来インテグラーゼ阻害剤の構造活性相関 (2011)
  • Author(s): 尾崎太郎,野村渉,山本直樹など
  • Organizer: 第25回日本エイズ学会学術集会・総会日本エイズ学会
  • Place of Presentation: 東京
  • Year and Date: 2011-11-30
• [Presentation] SAR Studies of Small Molecular CD4Mimics Targeting the HIV Entry Mechanism (2011)
  • Author(s): Narumi T, Nomura W, Tamamura H, et. al.
  • Organizer: 8th AFMC International Medicinal Chemistry Symposium
  • Place of Presentation: Tokyo, Japan
  • Year and Date: 2011-11-29
• [Presentation] HIV外被タンパク質gp120の構造変化を誘起する低分子CD4ミミックの構造活性相関研究 (2011)
  • Author(s): 新井啓之,野村渉,玉村啓和など
  • Organizer: 第55回日本薬学会関東支部大会
  • Place of Presentation: 東京
  • Year and Date: 2011-10-08
• [Presentation] HIVタンパク質Vprを基にしたインテグラーゼ阻害剤の構造活性相関研究 (2011)
  • Author(s): 尾崎太郎, 野村渉, 山本直樹、玉村啓和, など
  • Organizer: 第55回日本薬学会関東支部大会
  • Place of Presentation: 東京
  • Year and Date: 2011-10-08
• [Presentation] CXCR4二量化状態解析のための2価結合型リガンドの合成 (2011)
  • Author(s): 相馬晃, 玉村啓和, など
  • Organizer: 第55回日本薬学会関東支部大会
  • Place of Presentation: 東京
  • Year and Date: 2011-10-08
• [Presentation] HIV-1エンベロープ蛋白質を標的とした治療を評価するためのサル/ヒト免疫不全ウイルスの作製とin vitroにおける中和感受性の評価 (2011)
  • Author(s): 大附寛幸, 三浦智行, 玉村啓和, 松下修三, 五十嵐樹彦, など
  • Organizer: 第25回近畿エイズ研究会学術集会
  • Place of Presentation: 京都
  • Year and Date: 2011-06-18
• [Presentation] Design Synthesis and BiologicalEvaluation of CD4 Mimics Targetingthe Interaction with Asp368 and Val430in Gp120 (2011)
  • Author(s): Arai H, Narumi T, Tamamura H, et. al.
  • Organizer: The 12th Kumamoto AIDSSeminar・GCOE Joint International Symposium. Kumamoto
  • Place of Presentation: Japan
• [Presentation] ケミカルバイオロジーを基盤とした抗HIV剤の創製.シンポジウム「新しい抗感染症剤研究の最前線-発見、ケミカルバイオロジーそして創薬へ (2011)
  • Author(s): 玉村啓和
  • Organizer: 日本薬学会第131年会(中止)
  • Place of Presentation: 静岡
• [Presentation] 二核亜鉛錯体型CXCR4アンタゴニストの構造活性相関研究.日本ケミカルバイオロジー学会 (2011)
  • Author(s): 尾崎太郎,野村渉,玉村啓和など
  • Organizer: 第6回年会
  • Place of Presentation: 東京
• [Presentation] Synthesis of HIV Gp41 Trimer Mimics Inducing Neutralizing Antibodies Based on Remodeling of Dynamic Structures of HIV-1 Envelope Proteins (2011)
  • Author(s): Nomura W, Nakahara T, Narumi T, Yamamoto N, Tamamura T, et al
  • Organizer: 22nd American Peptide Symposium
  • Place of Presentation: Southern California, USA
• [Presentation] Development of Bivalent Ligands for CXCR4 with Rigid Linkers and Application to Detection of Cancer Cells (2011)
  • Author(s): Nomura W, Tanaka T, Masuda A, Narumi T, Tamamura H
  • Organizer: 22nd American Peptide Symposium
  • Place of Presentation: Southern California, USA
• [Presentation] Identification of Anti-HIV Peptides Derived from Matrix Proteins (2011)
  • Author(s): Narumi T, Murakami T, Tamamura H, et al
  • Organizer: ACS Meeting Fall2011
  • Place of Presentation: Denver, Colorado, USA
• [Presentation] HIV-1 Co-Receptor CXCR4-Derived Peptides Targeting AIDS Vaccines (2011)
  • Author(s): Hashimoto C, Narumi T, Nomura W, Yamamoto N, Tamamura H
  • Organizer: The 9th Australian Peptide Conference
  • Place of Presentation: Hamilton Island, Queensland, Australia
• [Presentation] SAR Study of Small Molecular CD4 Mimics Targeting the Dynamic Supramolecular Mechanism of HIV Entry and Their Hybrid Molecules with a CXCR4 Antagonist (2011)
  • Author(s): Narumi T, Arai H, Nomura W, Matsushita S, Tamamura H, et al.
  • Organizer: The 12th Kumamoto AIDS Seminar・GCOE Joint International Symposium
  • Place of Presentation: Kumamoto, Japan
• [Presentation] Design, Synthesis and Biological Evaluation of CD4 Mimics Targeting the Interaction with Asp368 and Val430 in Gp120 (2011)
  • Author(s): Arai H, Nomura W, Matsushita S, Tamamura H, et al
  • Organizer: The 12th Kumamoto AIDS Seminar・GCOE Joint International Symposium
  • Place of Presentation: Kumamoto, Japan
• [Presentation] SAR Studies of Small Molecular CD4 Mimics Targeting the HIV Entry Mechanism (2011)
  • Author(s): Narumi T, Arai H, Nomura W, Matsushita S, Tamamura H, et al
  • Organizer: 8th AFMC International Medicinal Chemistry Symposium
  • Place of Presentation: Tokyo, Japan
• [Presentation] Synthetic Antigens for Induction of Structure-Specific Antibodies against Trimer-Form of gp41 (2011)
  • Author(s): Nomura W, Yamamoto N, Tamamura H, et al.
  • Organizer: 8th AFMC International Medicinal Chemistry Symposium
  • Place of Presentation: Tokyo, Japan
• [Presentation] CXCR4-Derived Peptides Targeting AIDS Vaccines (2011)
  • Author(s): Hashimoto C, Yamamoto N, Tamamura H, et al
  • Organizer: 8th AFMC International Medicinal Chemistry Symposium
  • Place of Presentation: Tokyo, Japan
• [Presentation] Several HIV Inhibitors Targeting Entry, Fusion, Integrase and Matrix (2011)
  • Author(s): Narumi T, Nomura W, Tamamura H
  • Organizer: 8th AFMC International Medicinal Chemistry Symposium
  • Place of Presentation: Tokyo, Japan
• [Presentation] 新規HIV侵入阻害剤の創製研究:低分子型CD4ミミック-CXCR4アンタゴニストのハイブリッド分子の設計と合成 (2011)
  • Author(s): 鳴海哲夫, 野村渉, 松下修三, 玉村啓和, など
  • Organizer: 日本ケミカルバイオロジー学会第6回年会
  • Place of Presentation: 東京
• [Presentation] HIV外被タンパク質gp120の構造変化を誘起する低分子CD4ミミックの構造活性相関研究 (2011)
  • Author(s): 鳴海哲夫, 新井啓之, 野村渉, 松下修三, 玉村啓和, など
  • Organizer: 日本ケミカルバイオロジー学会第6回年会
  • Place of Presentation: 東京
• [Presentation] HIV外被タンパク質gp41-C34 3量体の合成とその抗HIV作用 (2011)
  • Author(s): 橋本知恵, 野村渉, 山本直樹, 玉村啓和, など
  • Organizer: 日本ケミカルバイオロジー学会第6回年会
  • Place of Presentation: 東京
• [Presentation] 二核亜鉛錯体型CXCR4アンタゴニストの構造活性相関研究 (2011)
  • Author(s): 尾崎太郎, 野村渉, 村上努, 山本直樹, 玉村啓和, など
  • Organizer: 日本ケミカルバイオロジー学会第6回年会
  • Place of Presentation: 東京
• [Presentation] 細胞表面におけるCXCR4二量体構造解析のための堅固なリンカーを有する二価型リガンドの開発 (2011)
  • Author(s): 野村渉, 田中智博, 相馬晃, 鳴海哲夫, 増田朱美, 玉村啓和
  • Organizer: 日本ケミカルバイオロジー学会第6回年会
  • Place of Presentation: 東京
• [Presentation] HIV外被タンパク質gp120の構造変化を誘起する低分子CD4ミミックの構造活性相関研究 (2011)
  • Author(s): 鳴海哲夫, 野村渉, 玉村啓和, 吉村和久, 松下修三, など
  • Organizer: 創薬懇話会
  • Place of Presentation: 岡山
• [Presentation] HIV-1遺伝子産物由来のインテグラーゼ阻害剤 (2011)
  • Author(s): 玉村啓和
  • Organizer: 第16回日本病態プロテアーゼ学会学術集会
  • Place of Presentation: 大阪
• [Presentation] 2価結合型リガンドの新規デザインによるCXCR4の細胞表面における機能解析 (2011)
  • Author(s): 野村渉, 田中智博, 増田朱美, 鳴海哲夫, 玉村啓和
  • Organizer: 第5回バイオ関連化学シンポジウム
  • Place of Presentation: 筑波
• [Presentation] 2価型CXCR4リガンドの開発と受容体結合機能の解析 (2011)
  • Author(s): 野村渉, 玉村啓和, など
  • Organizer: 第48回ペプチド討論会
  • Place of Presentation: 札幌
• [Presentation] HIVワクチンを指向したgp41の動的構造変化を模倣した抗原ペプチドの開発研究 (2011)
  • Author(s): 野村渉, 駒野淳, 山本直樹, 玉村啓和, など
  • Organizer: 第48回ペプチド討論会
  • Place of Presentation: 札幌
• [Presentation] 蛍光ラベル化した二価結合型CXCR4リガンドの創製と応用 (2011)
  • Author(s): 相川春夫, 玉村啓和, など
  • Organizer: 第37回反応と合成の進歩シンポジウム
  • Place of Presentation: 徳島
• [Presentation] 低分子型CD4ミミック:HIV外被タンパク質の構造変化を促すHIV侵入阻害剤 (2011)
  • Author(s): 鳴海哲夫, 野村渉, 松下修三, 玉村啓和, など
  • Organizer: 第25回日本エイズ学会学術集会・総会日本エイズ学会
  • Place of Presentation: 東京
• [Presentation] HIV-1第二受容体CXCR4の細胞外ドメインを基にしたエイズワクチンの開発研究 (2011)
  • Author(s): 橋本知恵, 鳴海哲夫, 野村渉, 山本直樹, 玉村啓和, など
  • Organizer: 第25回日本エイズ学会学術集会・総会日本エイズ学会
  • Place of Presentation: 東京
• [Presentation] HIV外被タンパク質gp120の構造変化誘起を指向した低分子CD4ミミックの構造活性相関研究 (2011)
  • Author(s): 鳴海哲夫, 吉村和久, 野村渉, 松下修三, 玉村啓和, など
  • Organizer: 第25回日本エイズ学会学術集会・総会日本エイズ学会
  • Place of Presentation: 東京
• [Presentation] HrV外被タンパク質gp120の構造変化誘起を指向した低分子CD4ミミックの創製 (2010)
  • Author(s): 鳴海哲夫, 新井啓之, 落合千裕, 松下修三, 玉村啓和, など
  • Organizer: 第54回日本薬学会関東支部大会
  • Place of Presentation: 東京
  • Year and Date: 2010-10-02
• [Presentation] HIV 1マトリックスタンパク質を基にした新規抗HIVペプチドめ創出 (2010)
  • Author(s): 小森谷真央, 村上努, 野村渉, 山本直樹, 玉村啓和, など
  • Organizer: 第54回日本薬学会関東支部大会
  • Place of Presentation: 東京
  • Year and Date: 2010-10-02
• [Presentation] 二核亜鉛錯体型CXCR4アンタゴニストの構造活性相関研究 (2010)
  • Author(s): 尾崎太郎, 田中智博, 野村渉, 村上努, 玉村啓和, など
  • Organizer: 第54回日本薬学会関東支部大会
  • Place of Presentation: 東京
  • Year and Date: 2010-10-02
• [Presentation] GPCR 2量体構造解析を指向したツールの開発 (2010)
  • Author(s): 田中智博
  • Organizer: 第9回バイオテクノロジー国際会議
  • Place of Presentation: 東京
  • Year and Date: 2010-06-30
• [Presentation] Peptidic HIV IntegraseInhibitors Derived from HIV GeneProducts (2010)
  • Author(s): Tamamura H
  • Organizer: 11th KUMAMOTO AIDSSeminer・GCOE Joint International Symposium
  • Place of Presentation: Kumamoto, Japan
• [Presentation] Anti-HIV Inhibitors and AIDS Vaccines (2010)
  • Author(s): Tamamura H
  • Organizer: International Summer Program 2010
  • Place of Presentation: Tokyo, Japan
• [Presentation] Elucidation of a Dimerization State of a Chemokine Receptor CXCR4 via Chemical Biology Approach Utilizing Novel Bivalent Ligands with Rigid Polyproline Linkers (2010)
  • Author(s): Tanaka T, Nomura W, Narumi T, Tamamura H
  • Organizer: The 13th Akabori Conference Leipzig 2010 : Japanese-German Symposium on PeptideScience
  • Place of Presentation: Leipzig, Germany
• [Presentation] Peptidic HIV Integrase Inhibitors Derived from HIV Gene Products (2010)
  • Author(s): Tamamura H
  • Organizer: 11th KUMAMOTO AIDS Seminer-GCOE Joint International Symposium
  • Place of Presentation: Kumamoto, Japan
• [Presentation] Structure-Activity Relationships of CXCR4 Antagonists Having the Dipicolylamine/Azamacro- Cyclic-Metal Complex Structures (2010)
  • Author(s): Ozaki T, Yamamoto N, Tamamura H, et al.
  • Organizer: 11th KUMAMOTO AIDS Seminer-GCOEJoint International Symposium
  • Place of Presentation: Kumamoto, Japan
• [Presentation] Development of Small CD4 Mimic Molecules that Induce Conformational Changes in gp120 (2010)
  • Author(s): Arai H, Matsushita S, Tamamura H, et al.
  • Organizer: 11th KUMAMOTO AIDS Seminer-GCOEJoint International Symposium
  • Place of Presentation: Kumamoto, Japan
• [Presentation] Development of a Bivalent Ligand for a Chemokine Receptor CXCR4 by Utilizing Polyproline Helix as a Linker (2010)
  • Author(s): Nomura W, Tanaka T, Masuda A, Narumi T, Tamamura H
  • Organizer: 5th International Peptide Symposium
  • Place of Presentation: Kyoto, Japan
• [Presentation] ケミカルバイオロジーを基盤とした抗HIV剤の創製 (2010)
  • Author(s): 玉村啓和
  • Organizer: 創薬懇話会2010in蔵王、次世代を担う若手のためのメディシナルケミストリーフォーラム
  • Place of Presentation: 宮城
• [Presentation] リバースからフォワードへケミカルゲノミクスを活用した抗HIV創製 (2010)
  • Author(s): 田中智博, 山本直樹, 玉村啓和, など
  • Organizer: 日本ケミカルバイオロジー学会 第5回年会
  • Place of Presentation: 横浜
• [Presentation] 堅固なリンカーを有する二価結合型CXCR4リガンドの開発と応用 (2010)
  • Author(s): 田中智博, 野村渉, 鳴海哲夫, 増田朱美, 玉村啓和
  • Organizer: 日本ケミカルバイオロジー学会 第5回年会
  • Place of Presentation: 横浜
• [Presentation] HIV-1マトリックスタンパク質を基にした新規抗HIVペプチドの創出 (2010)
  • Author(s): 小森谷真央, 山本直樹, 玉村啓, など
  • Organizer: 日本ケミカルバイオロジー学会 第5回年会
  • Place of Presentation: 横浜
• [Presentation] 2価結合型リガンドの新規デザインによるCXCR4の細胞表面における機能解析 (2010)
  • Author(s): 野村渉, 田中智博, 増田朱美, 鳴海哲夫, 玉村啓和
  • Organizer: 第4回バイオ関連化学シンポジウム
  • Place of Presentation: 大阪
• [Presentation] マトリックスタンパク質を基にした新規抗HIVペプチド (2010)
  • Author(s): 小森谷真央, 野村渉, 山本直樹, 玉村啓和, など
  • Organizer: 第29回メディシナルケミストリーシンポジウム
  • Place of Presentation: 京都
• [Presentation] HIV-1外被タンパク質gp120の構造変化誘起を指向した低分子CD4ミミックの構造活性相関研究 (2010)
  • Author(s): 鳴海哲夫, 新井啓之, 落合千裕, 吉村和久, 野村渉, 松下修三, 玉村啓和, など
  • Organizer: 第29回メディシナルケミストリーシンポジウム
  • Place of Presentation: 京都
• [Presentation] 細胞膜透過性MA部分ペプチドライブラリーを用いた新規抗HIV-1ペプチドの探索と創出 (2010)
  • Author(s): 村上努, 小森谷真央, 野村渉, 山本直樹, 玉村啓和, など
  • Organizer: 第58回日本ウイルス学会学術集会
  • Place of Presentation: 徳島
• [Presentation] HIV-1遺伝子産物由来のインテグラーゼ阻害剤の創出 (2010)
  • Author(s): 橋本知恵, 野村渉, Maddali K、Pommier Y, 山本直樹, 駒野淳, 玉村啓和, など
  • Organizer: 第24回日本エイズ学会学術集会・総会
  • Place of Presentation: 東京
• [Presentation] HIV外被タンパク質gp120の構造変化誘起を指向した低分子CD4ミミックの創製 (2010)
  • Author(s): 鳴海哲夫, 新井啓之, 野村渉, 松下修三, 玉村啓和, など
  • Organizer: 第24回日本エイズ学会学術集会・総会
  • Place of Presentation: 東京
• [Presentation] HIV-1マトリックスタンパク質を基にした新規抗HIVペプチドの創出 (2010)
  • Author(s): 小森谷真央, 野村渉, 山本直樹, 玉村啓和, など
  • Organizer: 第24回日本エイズ学会学術集会・総会
  • Place of Presentation: 東京
• [Presentation] gp120のCD4結合サイトを模倣した新規抗原分子の創製 (2010)
  • Author(s): 尾崎太郎, 田中智博, 宮内浩典, 野村渉, 山本直樹, 駒野淳, 玉村啓和, など
  • Organizer: 第24回日本エイズ学会学術集会・総会
  • Place of Presentation: 東京
• [Book] Development of Bivalent Ligands forCXCR4 with Rigid Linkers and Application to Detection of Cancer Cells. Proceedings of the Twenty-Second American Peptide Symposium, Michal Lebl(Eds.) (2011)
  • Author(s): Nomura W, Tamamura H, et. al.
  • Publisher: American Peptide Society, San Diego
• [Book] Development of a Bivalent Ligand for a Chemokine Receptor CXCR4 by Utilizing Polyproline Helix as a Linker. Proceedings of the 5th InternationalPeptide Symposium in conjunction with the 47th Japanese Peptide Symposium (2011)
  • Author(s): Nomura W, Tamamura H, et. al.
  • Total Pages: 220
  • Publisher: The Japanese Peptide Society, Kyoto, Japan
• [Book] Studies for Optimum Design of Artificial Zinc Finger Recombinases by Evaluation of Effects of DNA Binding Affinity and Linker Components on Recombination Efficiency. Proceedings of the Twenty-Second American Peptide Symposium (2011)
  • Author(s): Masuda A, Nomura, W, Ohba K, Yamamoto N, Tamamura H
  • Total Pages: 2
  • Publisher: Michal Lebl (Eds.), American Peptide Society, San Diego
• [Book] Synthesis of HIV Gp41 Trimer Mimics Inducing Neutralizing Antibodies Based on Remodeling of Dynamic Structures of HIV-1 Envelope Proteins. Proceedings of the Twenty-Second American Peptide Symposium (2011)
  • Author(s): Nomura W, Yamamoto N, Tamamura T, et al.
  • Total Pages: 2
  • Publisher: Michal Lebl (Eds.), American Peptide Society, San Diego
• [Book] Development of Bivalent Ligands for CXCR4 with Rigid Linkers and Application to Detection of Cancer Cells. Proceedings of the Twenty-Second American Peptide Symposium (2011)
  • Author(s): Nomura W, Tanaka T, Tamamura H, et al.
  • Total Pages: 2
  • Publisher: Michal Lebl (Eds.), American Peptide Society, San Diego
• [Book] Novel Tag-probe Pairs for Fluorescent Imaging of Proteins in Living Cells. Proceedings of the 5th International Peptide Symposium in conjunction with the 47th Japanese Peptide Symposium (2011)
  • Author(s): Nomura W, Ohashi N, Tamamura H, et al.
  • Total Pages: 1
  • Publisher: Nobutaka Fujii and Yoshiaki Kiso (Eds.), The Japanese Peptide Society, Kyoto, Japan
• [Book] Development of a Bivalent Ligand for a Chemokine Receptor CXCR4 by Utilizing Polyp roline Helix as a Linker. Proceedings of the 5th International Peptide Symposium in conjunction with the 47th Japanese Peptide Symposium (2011)
  • Author(s): Nomura W, Tanaka T, Tamamura H, et al.
  • Total Pages: 1
  • Publisher: Nobutaka Fujii and Yoshiaki Kiso (Eds.), The Japanese Peptide Society, Kyoto, Japan
• [Book] Synthesis and Evaluation of CXCR4-derived Peptides Targeting the Development of AIDS Vaccines. Proceedings of the 5th International Peptide Symposium in conjunction with the 47th Japanese Peptide Symposium (2011)
  • Author(s): Hashimoto C, Narumi T, Nomura W, Yamamoto N, Tamamura H
  • Total Pages: 1
  • Publisher: Nobutaka Fujii and Yoshiaki Kiso (Eds.), The Japanese Peptide Society, Kyoto, Japan
• [Book] ペプチドミメティックによる創薬研究,生化学特集号「ペプチド科学と生化学の接点」 (2010)
  • Author(s): 鳴海哲夫,玉村啓和
  • Publisher: 日本生化学会
• [Book] ペプチド科学と生化学の接点(ペプチドミメティックによる創薬研究, 生化学特集号)(82巻6号) (2010)
  • Author(s): 鳴海哲夫, 玉村啓和
  • Total Pages: 9
  • Publisher: 日本生化学会 東京
• [Book] エピジェネティクな遺伝子発現制御のためのDNAメチル化酵素の創製,生化学ミニレビュウ(82巻 5巻) (2010)
  • Author(s): 野村渉, 増田朱美, 玉村啓和
  • Total Pages: 5
  • Publisher: 日本生化学会 東京
• [Book] From Reverse to Forward Chemical Genomics: Development of Anti-HIVAgent.Peptide Science 2009 (2010)
  • Author(s): Tanaka T, Nomura W, Yamamoto N, Tamamura H, et al.
  • Total Pages: 2
  • Publisher: Kouji Okamoto (Eds.), The Japanese peptide Society, Osaka
• [Book] Synthesis and Evaluation of Artificial Antigen Peptide Based on theTrimeric Form of HIV Fusion Protein.Peptide Science 2009 (2010)
  • Author(s): Ohya A, Nakahara T, Nomura W, Yamamoto N, Tamamura H, et al.
  • Total Pages: 3
  • Publisher: Kouji Okamoto (Eds.), The Japanese peptide Society, Osaka
• [Book] Caged DAG-Lactones for Study of Cellular Signaling in a Spatial-andTemporal Specific Manner.Peptide Science 2009 (2010)
  • Author(s): Nomura W, Furuta T, Tamamura H, et al.
  • Total Pages: 2
  • Publisher: Kouji Okamoto (Eds.), The Japanese peptide Society, Osaka
• [Book] Fluorescnt-Based Orthogonal Sensing Methods for Double Ealuation in PKC Ligands Screening.Peptide Science 2009 (2010)
  • Author(s): Ohashi N, Nomura W, Lewin NE, Blumberg PM, Tamamura H, et al.
  • Total Pages: 2
  • Publisher: Kouji Okamoto (Eds.), The Japanese peptide Society, Osaka
• [Book] 種々の作用点をターゲットとした抗HIV剤の創製 (2009)
  • Author(s): 玉村啓和
  • Publisher: 日本エイズ学会
• [Patent(Industrial Property Rights)] HIV立体構造認識抗体誘導ペプチド抗原、及びその合成方法 (2011)
  • Inventor(s): 玉村啓和、中原徹、野村渉
  • Industrial Property Rights Holder: 東京医科歯科大学
  • Filing Date: 2011-11-11
  • Overseas
• [Patent(Industrial Property Rights)] HIV立体構造認識抗体誘導ペプチド抗原、及びその合成方法 (2011)
  • Inventor(s): 玉村啓和、中原徹、野村渉
  • Industrial Property Rights Holder: 国立大学法人東京医科歯科大学
  • Filing Date: 2011-11-10
  • Overseas
• [Patent(Industrial Property Rights)] HIV立体構造認識抗体誘導ペプチド抗原、及びその合成方法 (2011)
  • Inventor(s): 玉村啓和、中原徹、野村渉
  • Industrial Property Rights Holder: 国立大学法人東京医科歯科大学
  • Filing Date: 2011-11-04
• [Patent(Industrial Property Rights)] HIV立体構造認識抗体誘導ペプチド (2011)
  • Inventor(s): 玉村啓和、鳴海哲夫、野村渉
  • Industrial Property Rights Holder: 国立大学法人東京医科歯科大学
  • Filing Date: 2011-04-04
• [Patent(Industrial Property Rights)] HIV立体構造認識抗体誘導ペプチド (2011)
  • Inventor(s): 玉村啓和、鳴海哲夫、野村渉、橋本知恵、駒野淳、宮内浩典
  • Industrial Property Rights Holder: 国立大学法人東京医科歯科大学
  • Industrial Property Number: 2011-082813
  • Filing Date: 2011-04-04
• [Patent(Industrial Property Rights)] HIV立体構造認識抗体誘導ペプチド抗原、及びその合成方法 (2011)
  • Inventor(s): 玉村啓和、中原徹、野村渉
  • Industrial Property Rights Holder: 国立大学法人東京医科歯科大学
  • Industrial Property Number: 2011-514322
  • Filing Date: 2011-11-04
• [Patent(Industrial Property Rights)] HIV立体構造認識抗体誘導ペプチド抗原、及びその合成方法 (2011)
  • Inventor(s): 玉村啓和、中原徹、野村渉
  • Industrial Property Rights Holder: 国立大学法人東京医科歯科大学
  • Filing Date: 2011-11-10
  • Overseas
• [Patent(Industrial Property Rights)] HIV立体構造認識抗体誘導ペプチド抗原、及びその合成方法 (2011)
  • Inventor(s): 玉村啓和、中原徹、野村渉
  • Industrial Property Rights Holder: 国立大学法人東京医科歯科大学
  • Filing Date: 2011-11-11
  • Overseas
• [Patent(Industrial Property Rights)] HIV立体構造認識抗体誘導ペプチド抗原、及びその合成方法 (2010)
  • Inventor(s): 玉村啓和、中原徹、野村渉
  • Industrial Property Rights Holder: 国立大学法人東京医科歯科大学
  • Filing Date: 2010-11-25
  • Overseas
• [Patent(Industrial Property Rights)] HIV立体構造認識抗体誘導ペプチド抗原、及びその合成方法 (2010)
  • Inventor(s): 玉村啓和、中原徹、野村渉
  • Industrial Property Rights Holder: 国立大学法人東京医科歯科大学
  • Filing Date: 2010-05-14
  • Overseas
• [Patent(Industrial Property Rights)] IV立体構造認識抗体誘導ペプチド抗原、及びその合成方法 (2010)
  • Inventor(s): 玉村啓和、中原徹、野村渉
  • Industrial Property Rights Holder: 国立大学法人東京医科歯科大学
  • Filing Date: 2010-05-14
• [Patent(Industrial Property Rights)] CXCR4多量体を認識する多価型CXCR4リガンド、及びその合成方法 (2009)
  • Inventor(s): 玉村啓和、野村渉、鳴海哲夫
  • Industrial Property Rights Holder: 国立大学法人東京医科歯科大学
  • Filing Date: 2009-07-06
• [Patent(Industrial Property Rights)] HIV立体構造認識抗体誘導ペプチド抗原、及びその合成方法 (2009)
  • Inventor(s): 玉村啓和、中原徹、野村渉
  • Industrial Property Rights Holder: 国立大学法人東京医科歯科大学
  • Filing Date: 2009-05-18