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  1. Potent HIV‑1 protease inhibitors containing oxabicyclo octanol-derived P2-ligands: Design, synthesis, and X‑ray structural studies of inhibitor-HIV-1 protease complexes

    Article • Bioorganic & Medicinal Chemistry Letters, May 2025, Elsevier

    Dr Masayuki Amano

  2. Covalent anti-HIV compound that induces HIV-1 capsid multimerization and degradation decomposes the viral core

    Article • April 2025, Cold Spring Harbor Laboratory Press

    Dr Masayuki Amano

  3. A high-throughput, fully automated competition assay to evaluate SARS-CoV-2 neutralizing responses and epitope specificity in clinical samples

    Article • Scientific Reports, April 2025, Springer Science + Business Media

    Dr Masayuki Amano

  4. Neutralization activity of HCWs’ sera after Omicron XBB.1.5-adapted monovalent COVID-19 mRNA vaccination

    Article • Journal of Infection, July 2024, Elsevier

    Dr Masayuki Amano

  5. Exploration of P1 and P4 modifications of nirmatrelvir: Design, synthesis, biological evaluation, and X-ray structural studies of SARS-CoV-2 Mpro inhibitors

    Article • European Journal of Medicinal Chemistry, March 2024, Elsevier

    Dr Masayuki Amano

  6. Design of substituted tetrahydrofuran derivatives for HIV-1 protease inhibitors: synthesis, biological evaluation, and X-ray structural studies

    Article • Organic & Biomolecular Chemistry, January 2024, Royal Society of Chemistry

    Dr Masayuki Amano

  7. Longitudinal analysis of neutralization in sera from HCWs receiving 2 doses of Omicron BA.4/5-adapted bivalent vaccine

    Article • Journal of Infection, November 2023, Elsevier

    Dr Masayuki Amano

  8. Neutralization against Omicron sublineages (BA.2/BA.5/BQ.1.1/XBB/XBB.1.5) in bivalent BNT162b2-vaccinated HCWs with or without risk factors, or following BT infection with Omicron

    Article • Scientific Reports, October 2023, Springer Science + Business Media

    Dr Masayuki Amano

  9. Exploration of imatinib and nilotinib-derived templates as the P2-Ligand for HIV-1 protease inhibitors: Design, synthesis, protein X-ray structural studies, and biological evaluation

    Article • European Journal of Medicinal Chemistry, July 2023, Elsevier

    Dr Masayuki Amano

  10. Evaluation of darunavir-derived HIV-1 protease inhibitors incorporating P2′ amide-derivatives: Synthesis, biological evaluation and structural studies

    Article • Bioorganic & Medicinal Chemistry Letters, March 2023, Elsevier

    Dr Masayuki Amano

  11. Comparison of neutralization activity against Omicron BA.2/BA.5 in sera from HCWs receiving heterologous/homologous COVID-19 vaccines

    Article • Journal of Infection, February 2023, Elsevier

    Dr Masayuki Amano

  12. Development of anti-HBV agents targeting HBV capsid proteins

    Article • RSC Medicinal Chemistry, January 2023, Royal Society of Chemistry

    Dr Masayuki Amano

  13. Synthesis of Selenoesters via Aldol Condensation and/or Conjugate Reduction and Their Antiviral Activities

    Article • ACS Omega, December 2022, American Chemical Society (ACS)

    Dr Masayuki Amano

  14. Restoration of Neutralization Activity Against Omicron BA.2 and BA.5 in Older Adults and Individuals With Risk Factors Following the Fourth Dose of Severe Acute Respiratory Syndrome Coronavirus 2 BNT162b2 Vaccine

    Article • The Journal of Infectious Diseases, September 2022, Oxford University Press (OUP)

    Dr Masayuki Amano

  15. Neutralization activity of sera/IgG preparations from fully BNT162b2 vaccinated individuals against SARS-CoV-2 Alpha, Beta, Gamma, Delta, and Kappa variants

    Article • Scientific Reports, August 2022, Springer Science + Business Media

    Dr Masayuki Amano

  16. Third-Dose BNT162b2 Vaccination Elicits Markedly High-Level SARS-CoV-2–Neutralizing Antibodies in Vaccinees Who Responded Poorly to a Second Dose in Japan

    Article • The Journal of Infectious Diseases, May 2022, Oxford University Press (OUP)

    Dr Masayuki Amano

  17. Neutralization-activity of Sera/IgG Obtained from Fully BNT162b2- Vaccinated Individuals Against 10 Clinical SARS-CoV-2 isolates Including Various VOCs (Alpha/Beta/Gamma/Delta) and VUM (Kappa)

    Article • March 2022, Research Square

    Dr Masayuki Amano

  18. Design, Synthesis and X‐Ray Structural Studies of Potent HIV‐1 Protease Inhibitors Containing C‐4 Substituted Tricyclic Hexahydro‐Furofuran Derivatives as P2 Ligands

    Article • ChemMedChem, March 2022, Wiley

    Dr Masayuki Amano

  19. Fluorine Modifications Contribute to Potent Antiviral Activity against Highly Drug-Resistant HIV-1 and Favorable Blood-Brain Barrier Penetration Property of Novel Central Nervous System-Targeting HIV-1 Protease Inhibitors In Vitro

    Article • Antimicrobial Agents and Chemotherapy, February 2022, ASM Journals

    Dr Masayuki Amano

  20. Correlates of neutralizing/SARS-CoV-2-S1-binding antibody response with adverse effects and immune kinetics in BNT162b2-vaccinated individuals

    Article • Scientific Reports, November 2021, Springer Science + Business Media

    Dr Masayuki Amano

  21. A Small Molecule, ACAi-028, with Anti-HIV-1 Activity Targets a Novel Hydrophobic Pocket on HIV-1 Capsid

    Article • Antimicrobial Agents and Chemotherapy, September 2021, ASM Journals

    Dr Masayuki Amano

  22. Correlates of Neutralizing/SARS-CoV-2-S1-binding Antibody Response with Adverse Effects and Immune Kinetics in BNT162b2-Vaccinated Individuals

    Article • July 2021, Cold Spring Harbor Laboratory Press

    Dr Masayuki Amano

  23. A small molecule, ACAi-028, with anti-HIV-1 activity targets a novel hydrophobic pocket on HIV-1 capsid

    Article • May 2021, Cold Spring Harbor Laboratory Press

    Dr Masayuki Amano

  24. Human retroviral antisense mRNAs are retained in the nuclei of infected cells for viral persistence

    Article • Proceedings of the National Academy of Sciences, April 2021, Proceedings of the National Academy of Sciences

    Dr Masayuki Amano, Professor Masao Matsuoka

  25. Correlates of Neutralizing/SARS-CoV-2-S1-Binding Antibody Response With Adverse Effects and Immune Kinetics in BNT162b2-Vaccinated Individuals

    Article • SSRN Electronic Journal, January 2021, Elsevier

    Dr Masayuki Amano

  26. A Conformational Escape Reaction of HIV-1 against an Allosteric Integrase Inhibitor

    Article • Journal of Virology, July 2020, ASM Journals

    Dr Masayuki Amano, Teruya Nakamura

  27. Structure-Based Design of Highly Potent HIV-1 Protease Inhibitors Containing New Tricyclic Ring P2-Ligands: Design, Synthesis, Biological, and X-ray Structural Studies

    Article • Journal of Medicinal Chemistry, April 2020, American Chemical Society (ACS)

    Dr Masayuki Amano

  28. A unique conformational escape reaction of HIV-1 against an allosteric integrase inhibitor

    Article • November 2019, Cold Spring Harbor Laboratory Press

    Dr Masayuki Amano

  29. Synthesis and evaluation of the anti-hepatitis B virus activity of 4′-Azido-thymidine analogs and 4′-Azido-2′-deoxy-5-methylcytidine analogs: structural insights for the development of a novel anti-HBV agent

    Article • Nucleosides Nucleotides & Nucleic Acids, September 2019, Taylor & Francis

    Dr Masayuki Amano, Kazuhiro Haraguchi, Hiroaki Mitsuya

  30. Novel p97/ VCP inhibitor induces endoplasmic reticulum stress and apoptosis in both bortezomib‐sensitive and ‐resistant multiple myeloma cells

    Article • Cancer Science, August 2019, Wiley

    Dr Masayuki Amano

  31. Amino-acid inserts of HIV-1 capsid (CA) induce CA degradation and abrogate viral infectivity: Insights for the dynamics and mechanisms of HIV-1 CA decomposition

    Article • Scientific Reports, July 2019, Springer Science + Business Media

    Dr Masayuki Amano

  32. Novel Protease Inhibitors Containing C-5-Modified bis-Tetrahydrofuranylurethane and Aminobenzothiazole as P2 and P2′ Ligands That Exert Potent Antiviral Activity against Highly Multidrug-Resistant HIV-1 with a High Genetic Barrier against the Emergence...

    Article • Antimicrobial Agents and Chemotherapy, May 2019, ASM Journals

    Dr Masayuki Amano

  33. Novel Central Nervous System (CNS)-Targeting Protease Inhibitors for Drug-Resistant HIV Infection and HIV-Associated CNS Complications

    Article • Antimicrobial Agents and Chemotherapy, May 2019, ASM Journals

    Dr Masayuki Amano

  34. Synthesis, Anti-HBV, and Anti-HIV Activities of 3′-Halogenated Bis(hydroxymethyl)-cyclopentenyladenines

    Article • ACS Medicinal Chemistry Letters, November 2018, American Chemical Society (ACS)

    Dr Masayuki Amano

  35. Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure–Activity Studies, Biological and X-ray Structural Analysis

    Article • Journal of Medicinal Chemistry, May 2018, American Chemical Society (ACS)

    Dr Masayuki Amano

  36. Synthesis of 4′-Substituted Purine 2′-Deoxynucleosides and Their Activity against Human Immunodeficiency Virus Type 1 and Hepatitis B Virus

    Article • ChemistrySelect, March 2018, Wiley

    Dr Masayuki Amano

  37. Design, Synthesis, Biological Evaluation, and X-ray Studies of HIV-1 Protease Inhibitors with Modified P2′ Ligands of Darunavir

    Article • ChemMedChem, November 2017, Wiley

    Dr Masayuki Amano

  38. Design of novel HIV-1 protease inhibitors incorporating isophthalamide-derived P2-P3 ligands: Synthesis, biological evaluation and X-ray structural studies of inhibitor-HIV-1 protease complex

    Article • Bioorganic & Medicinal Chemistry, October 2017, Elsevier

    Dr Masayuki Amano

  39. GRL-09510, a Unique P2-Crown-Tetrahydrofuranylurethane -Containing HIV-1 Protease Inhibitor, Maintains Its Favorable Antiviral Activity against Highly-Drug-Resistant HIV-1 Variants in vitro

    Article • Scientific Reports, September 2017, Nature

    Dr Masayuki Amano

  40. Design, synthesis, X-ray studies, and biological evaluation of novel macrocyclic HIV-1 protease inhibitors involving the P1′-P2′ ligands

    Article • Bioorganic & Medicinal Chemistry Letters, September 2017, Elsevier

    Dr Masayuki Amano

  41. A novel entecavir analogue constructing with a spiro[2.4]heptane core structure in the aglycon moiety: Its synthesis and evaluation for anti-hepatitis B virus activity

    Article • Nucleosides Nucleotides & Nucleic Acids, June 2017, Taylor & Francis

    Dr Masayuki Amano

  42. A Modified P1 Moiety Enhancesin vitroAntiviral Activity against Various Multi-Drug-Resistant HIV-1 Variants andin vitroCNS Penetration Properties of a Novel Nonpeptidic Protease Inhibitor, GRL-10413

    Article • Antimicrobial Agents and Chemotherapy, September 2016, ASM Journals

    Dr Masayuki Amano

  43. Diastereoselective Synthesis of 6″-( Z )- and 6″-( E )-Fluoro Analogues of Anti-hepatitis B Virus Agent Entecavir and Its Evaluation of the Activity and Toxicity Profile of the Diastereomers

    Article • The Journal of Organic Chemistry, April 2016, American Chemical Society (ACS)

    Dr Masayuki Amano

  44. Immunomodulatory drugs act as inhibitors of DNA methyltransferases and induce PU.1 up-regulation in myeloma cells

    Article • Biochemical and Biophysical Research Communications, January 2016, Elsevier

    Dr Masayuki Amano

  45. Structure-based design, synthesis, X-ray studies, and biological evaluation of novel HIV-1 protease inhibitors containing isophthalamide-derived P2-ligands

    Article • Bioorganic & Medicinal Chemistry Letters, November 2015, Elsevier

    Dr Masayuki Amano

  46. 4′-modified nucleoside analogs: Potent inhibitors active against entecavir-resistant hepatitis B virus

    Article • Hepatology, August 2015, Wiley

    Dr Masayuki Amano

  47. Design, Synthesis, and Evaluation of Anti-HBV Activity of Hybrid Molecules of Entecavir and Adefovir: Exomethylene Acycloguanine Nucleosides and Their Monophosphate Derivatives

    Article • Nucleosides Nucleotides & Nucleic Acids, July 2015, Taylor & Francis

    Dr Masayuki Amano

  48. Structure-Based Design of Potent HIV-1 Protease Inhibitors with Modified P1-Biphenyl Ligands: Synthesis, Biological Evaluation, and Enzyme–Inhibitor X-ray Structural Studies

    Article • Journal of Medicinal Chemistry, July 2015, American Chemical Society (ACS)

    Dr Masayuki Amano

  49. A Novel Tricyclic Ligand-Containing Nonpeptidic HIV-1 Protease Inhibitor, GRL-0739, Effectively Inhibits the Replication of Multidrug-Resistant HIV-1 Variants and Has a Desirable Central Nervous System Penetration PropertyIn Vitro

    Article • Antimicrobial Agents and Chemotherapy, February 2015, ASM Journals

    Dr Masayuki Amano

  50. Design, synthesis, biological evaluation and X-ray structural studies of HIV-1 protease inhibitors containing substituted fused-tetrahydropyranyl tetrahydrofuran as P2-ligands

    Article • Organic & Biomolecular Chemistry, January 2015, Royal Society of Chemistry

    Dr Masayuki Amano

  51. Design of gem‐Difluoro‐bis‐Tetrahydrofuran as P2 Ligand for HIV‐1 Protease Inhibitors to Improve Brain Penetration: Synthesis, X‐ray Studies, and Biological Evaluation

    Article • ChemMedChem, October 2014, Wiley

    Dr Masayuki Amano

  52. Design and synthesis of potent macrocyclic HIV-1 protease inhibitors involving P1–P2 ligands

    Article • Organic & Biomolecular Chemistry, January 2014, Royal Society of Chemistry

    Dr Masayuki Amano

  53. Comparative analysis of ER stress response into HIV protease inhibitors: Lopinavir but not darunavir induces potent ER stress response via ROS/JNK pathway

    Article • Free Radical Biology and Medicine, December 2013, Elsevier

    Dr Masayuki Amano

  54. GRL-04810 and GRL-05010, Difluoride-Containing Nonpeptidic HIV-1 Protease Inhibitors (PIs) That Inhibit the Replication of Multi-PI-Resistant HIV-1In Vitroand Possess Favorable Lipophilicity That May Allow Blood-Brain Barrier Penetration

    Article • Antimicrobial Agents and Chemotherapy, September 2013, ASM Journals

    Dr Masayuki Amano

  55. Highly Potent HIV-1 Protease Inhibitors with Novel Tricyclic P2 Ligands: Design, Synthesis, and Protein–Ligand X-ray Studies

    Article • Journal of Medicinal Chemistry, August 2013, American Chemical Society (ACS)

    Dr Masayuki Amano

  56. GRL-0519, a Novel Oxatricyclic Ligand-Containing Nonpeptidic HIV-1 Protease Inhibitor (PI), Potently Suppresses Replication of a Wide Spectrum of Multi-PI-Resistant HIV-1 VariantsIn Vitro

    Article • Antimicrobial Agents and Chemotherapy, February 2013, ASM Journals

    Dr Masayuki Amano

  57. Loss of the Protease Dimerization Inhibition Activity of Tipranavir (TPV) and Its Association with the Acquisition of Resistance to TPV by HIV-1

    Article • Journal of Virology, September 2012, ASM Journals

    Dr Masayuki Amano

  58. Substituent effects on P2-cyclopentyltetrahydrofuranyl urethanes: Design, synthesis, and X-ray studies of potent HIV-1 protease inhibitors

    Article • Bioorganic & Medicinal Chemistry Letters, March 2012, Elsevier

    Dr Masayuki Amano

  59. Loss of Protease Dimerization Inhibition Activity of Darunavir Is Associated with the Acquisition of Resistance to Darunavir by HIV-1

    Article • Journal of Virology, August 2011, ASM Journals

    Dr Masayuki Amano

  60. Design of HIV-1 Protease Inhibitors with C3-Substituted Hexahydrocyclopentafuranyl Urethanes as P2-Ligands: Synthesis, Biological Evaluation, and Protein–Ligand X-ray Crystal Structure

    Article • Journal of Medicinal Chemistry, July 2011, American Chemical Society (ACS)

    Dr Masayuki Amano

  61. Novel HIV-1 Protease Inhibitors (PIs) Containing a Bicyclic P2 Functional Moiety, Tetrahydropyrano-Tetrahydrofuran, That Are Potent against Multi-PI-Resistant HIV-1 Variants

    Article • Antimicrobial Agents and Chemotherapy, January 2011, ASM Journals

    Dr Masayuki Amano

  62. Design, Synthesis, and X-ray Structure of Substituted Bis-tetrahydrofuran (Bis-THF)-Derived Potent HIV-1 Protease Inhibitors

    Article • ACS Medicinal Chemistry Letters, January 2011, American Chemical Society (ACS)

    Dr Masayuki Amano

  63. Design and Synthesis of Potent HIV-1 Protease Inhibitors Incorporating Hexahydrofuropyranol-Derived High Affinity P2 Ligands: Structure−Activity Studies and Biological Evaluation

    Article • Journal of Medicinal Chemistry, December 2010, American Chemical Society (ACS)

    Dr Masayuki Amano

  64. Cover Picture: Probing Multidrug‐Resistance and Protein–Ligand Interactions with Oxatricyclic Designed Ligands in HIV‐1 Protease Inhibitors (ChemMedChem 11/2010)

    Article • ChemMedChem, October 2010, Wiley

    Dr Masayuki Amano

  65. Probing Multidrug‐Resistance and Protein–Ligand Interactions with Oxatricyclic Designed Ligands in HIV‐1 Protease Inhibitors

    Article • ChemMedChem, September 2010, Wiley

    Dr Masayuki Amano

  66. In Vitro Selection of Highly Darunavir-Resistant and Replication-Competent HIV-1 Variants by Using a Mixture of Clinical HIV-1 Isolates Resistant to Multiple Conventional Protease Inhibitors

    Article • Journal of Virology, September 2010, ASM Journals

    Dr Masayuki Amano

  67. Novel Protease Inhibitors (PIs) Containing Macrocyclic Components and 3(R),3a(S),6a(R)-bis-Tetrahydrofuranylurethane That Are Potent against Multi-PI-Resistant HIV-1 Variants In Vitro

    Article • Antimicrobial Agents and Chemotherapy, May 2010, ASM Journals

    Dr Masayuki Amano

  68. Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands

    Article • Bioorganic & Medicinal Chemistry Letters, February 2010, Elsevier

    Dr Masayuki Amano, Dr sandra gemma

  69. Design, Synthesis, Protein−Ligand X-ray Structure, and Biological Evaluation of a Series of Novel Macrocyclic Human Immunodeficiency Virus-1 Protease Inhibitors to Combat Drug Resistance

    Article • Journal of Medicinal Chemistry, September 2009, American Chemical Society (ACS)

    Dr Masayuki Amano

  70. GRL-02031, a Novel Nonpeptidic Protease Inhibitor (PI) Containing a Stereochemically Defined Fused Cyclopentanyltetrahydrofuran Potent against Multi-PI-Resistant Human Immunodeficiency Virus Type 1 In Vitro

    Article • Antimicrobial Agents and Chemotherapy, October 2008, ASM Journals

    Dr Masayuki Amano

  71. Potent Inhibition of HIV-1 Replication by Novel Non-peptidyl Small Molecule Inhibitors of Protease Dimerization

    Article • Journal of Biological Chemistry, July 2007, American Society for Biochemistry & Molecular Biology (ASBMB)

    Dr Masayuki Amano

  72. Activity against Human Immunodeficiency Virus Type 1, Intracellular Metabolism, and Effects on Human DNA Polymerases of 4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine

    Article • Antimicrobial Agents and Chemotherapy, June 2007, ASM Journals

    Dr Masayuki Amano, Professor Masao Matsuoka

  73. A Novel Bis-Tetrahydrofuranylurethane-Containing Nonpeptidic Protease Inhibitor (PI), GRL-98065, Is Potent against Multiple-PI-Resistant Human Immunodeficiency Virus In Vitro

    Article • Antimicrobial Agents and Chemotherapy, March 2007, ASM Journals

    Dr Masayuki Amano