M. Aoki

发表

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.

Arun K. Ghosh, I. Weber, H. Mitsuya, 2018, Journal of medicinal chemistry.

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 of Drug Resistance

Arun K. Ghosh, H. Mitsuya, Y. Takamatsu, 2019, Antimicrobial Agents and Chemotherapy.

Raltegravir blocks the infectivity of red‐fluorescent‐protein (mCherry)‐labeled HIV‐1JR‐FL in the setting of post‐exposure prophylaxis in NOD/SCID/Jak3−/− mice transplanted with human PBMCs

Hisataka Kobayashi, H. Mitsuya, S. Okada, 2018, Antiviral research.

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

Arun K. Ghosh, I. Weber, H. Mitsuya, 2015, ChemMedChem.

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

David D. Anderson, Arun K. Ghosh, H. Mitsuya, 2010, Antimicrobial Agents and Chemotherapy.

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

Arun K. Ghosh, I. Weber, H. Mitsuya, 2022, ChemMedChem.

Halogen Bond Interactions of Novel HIV-1 Protease Inhibitors (PI) (GRL-001-15 and GRL-003-15) with the Flap of Protease Are Critical for Their Potent Activity against Wild-Type HIV-1 and Multi-PI-Resistant Variants

Arun K. Ghosh, H. Mitsuya, H. Bulut, 2019, Antimicrobial Agents and Chemotherapy.

The impact of highly active antiretroviral therapy by the oral route on the CD8 subset in monkeys infected chronically with SHIV 89.6P.

S. Matsushita, H. Mitsuya, H. Akiyama, 2003, Journal of virological methods.

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

H. Mitsuya, Shuhei Imoto, D. Das, 2020, Nucleosides, nucleotides & nucleic acids.

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.

H. Mitsuya, H. Abe, K. Fukuhara, 2016, The Journal of organic chemistry.

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

H. Mitsuya, Shuhei Imoto, H. Kumamoto, 2015, Nucleosides, nucleotides & nucleic acids.

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

Arun K. Ghosh, I. Weber, H. Mitsuya, 2015, Bioorganic & medicinal chemistry letters.

Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains.

H. Mitsuya, K. Maeda, A. Otaka, 2003, Journal of medicinal chemistry.

Novel Low Molecular Weight Spirodiketopiperazine Derivatives Potently Inhibit R5 HIV-1 Infection through Their Antagonistic Effects on CCR5*

Hiroaki Mitsuya, Kazuhisa Yoshimura, H. Mitsuya, 2001, The Journal of Biological Chemistry.

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

Y. Takamatsu, K. Maeda, Shuhei Imoto, 2018 .

4′‐modified nucleoside analogs: Potent inhibitors active against entecavir‐resistant hepatitis B virus

S. Sarafianos, D. Venzon, H. Mitsuya, 2015, Hepatology.

Delayed Emergence of HIV-1 Variants Resistant to 4′-Ethy Nyl-2-Fluoro-2′-Deoxyadenosine: Comparative Sequential Passage Study with Lamivudine, Tenofovir, Emtricitabine and BMS-986001

H. Mitsuya, K. Maeda, E. Kodama, 2014, Antiviral therapy.

Early phase dynamics of traceable mCherry fluorescent protein‐carrying HIV‐1 infection in human peripheral blood mononuclear cells‐transplanted NOD/SCID/Jak3‐/‐ mice

Hisataka Kobayashi, H. Mitsuya, S. Okada, 2017, Antiviral research.

Dimerization of HIV-1 protease occurs through two steps relating to the mechanism of protease dimerization inhibition by darunavir

Arun K. Ghosh, H. Mitsuya, Y. Koh, 2014, Proceedings of the National Academy of Sciences.

Identification of SARS-CoV-2 Mpro inhibitors containing P1’ 4-fluorobenzothiazole moiety highly active against SARS-CoV-2

M. Kiso, Y. Kawaoka, N. Kishimoto, 2023, Nature Communications.

Design of Highly Potent, Dual‐Acting and Central‐Nervous‐System‐Penetrating HIV‐1 Protease Inhibitors with Excellent Potency against Multidrug‐Resistant HIV‐1 Variants

Arun K. Ghosh, I. Weber, H. Mitsuya, 2018, ChemMedChem.

Mechanism of Darunavir (DRV)’s High Genetic Barrier to HIV-1 Resistance: A Key V32I Substitution in Protease Rarely Occurs, but Once It Occurs, It Predisposes HIV-1 To Develop DRV Resistance

Arun K. Ghosh, H. Mitsuya, Y. Takamatsu, 2018, mBio.

A novel central nervous system-penetrating protease inhibitor overcomes human immunodeficiency virus 1 resistance with unprecedented aM to pM potency

Arun K. Ghosh, H. Mitsuya, H. Jono, 2017, eLife.

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

Arun K. Ghosh, I. Weber, H. Mitsuya, 2010, ChemMedChem.

Genetic evidence of transmission of human T cell lymphotropic virus type 1 between spouses.

M. Matsuoka, H. Mitsuya, H. Tsubouchi, 2002, The Journal of infectious diseases.

Non-Cleavage Site Gag Mutations in Amprenavir-Resistant Human Immunodeficiency Virus Type 1 (HIV-1) Predispose HIV-1 to Rapid Acquisition of Amprenavir Resistance but Delay Development of Resistance to Other Protease Inhibitors

Hiroaki Mitsuya, Kazuhisa Yoshimura, D. Venzon, 2009, Journal of Virology.

Design of HIV-1 Protease Inhibitors with Amino-bis-tetrahydrofuran Derivatives as P2-Ligands to Enhance Backbone-Binding Interactions: Synthesis, Biological Evaluation, and Protein-Ligand X-ray Studies.

Arun K. Ghosh, I. Weber, H. Mitsuya, 2015, Journal of medicinal chemistry.

Potent HIV-1 protease inhibitors incorporating squaramide-derived P2 ligands: Design, synthesis, and biological evaluation.

Arun K. Ghosh, D. Walters, H. Mitsuya, 2019, Bioorganic & medicinal chemistry letters.

C-5-Modified Tetrahydropyrano-Tetrahydofuran-Derived Protease Inhibitors (PIs) Exert Potent Inhibition of the Replication of HIV-1 Variants Highly Resistant to Various PIs, including Darunavir

Arun K. Ghosh, H. Mitsuya, Teruya Nakamura, 2015, Journal of Virology.

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

Arun K. Ghosh, R. Shafer, H. Mitsuya, 2011, Journal of Virology.

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

Arun K. Ghosh, I. Weber, H. Mitsuya, 2020, Journal of medicinal chemistry.

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.

Arun K. Ghosh, I. Weber, H. Mitsuya, 2017, Bioorganic & medicinal chemistry.

P2′ Benzene Carboxylic Acid Moiety Is Associated with Decrease in Cellular Uptake: Evaluation of Novel Nonpeptidic HIV-1 Protease Inhibitors Containing P2 bis-Tetrahydrofuran Moiety

Arun K. Ghosh, P. Wingfield, S. Stahl, 2013, Antimicrobial Agents and Chemotherapy.

Single atom changes in newly synthesized HIV protease inhibitors reveal structural basis for extreme affinity, high genetic barrier, and adaptation to the HIV protease plasticity

Arun K. Ghosh, H. Mitsuya, D. Davis, 2020, Scientific Reports.

Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.

Irene T Weber, Yuan-Fang Wang, Debananda Das, 2017, Journal of medicinal chemistry.

A Conserved Hydrogen-Bonding Network of P2 bis-Tetrahydrofuran-Containing HIV-1 Protease Inhibitors (PIs) with a Protease Active-Site Amino Acid Backbone Aids in Their Activity against PI-Resistant HIV

Arun K. Ghosh, P. Wingfield, J. Kaufman, 2014, Antimicrobial Agents and Chemotherapy.

Probing Lipophilic Adamantyl Group as the P1-Ligand for HIV-1 Protease Inhibitors: Design, Synthesis, Protein X-ray Structural Studies, and Biological Evaluation.

Arun K. Ghosh, I. Weber, H. Mitsuya, 2016, Journal of medicinal chemistry.

GRL-079, a Novel HIV-1 Protease Inhibitor, Is Extremely Potent against Multidrug-Resistant HIV-1 Variants and Has a High Genetic Barrier against the Emergence of Resistant Variants

Arun K. Ghosh, H. Mitsuya, Y. Takamatsu, 2018, Antimicrobial Agents and Chemotherapy.

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 Variants In Vitro

Arun K. Ghosh, H. Mitsuya, Kalapala Venkateswara Rao, 2013, Antimicrobial Agents and Chemotherapy.

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

Arun K. Ghosh, I. Weber, H. Mitsuya, 2017, ChemMedChem.

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

H. Mitsuya, Y. Koh, M. Danish, 2012, Journal of Virology.

Potent HIV‐1 Protease Inhibitors Containing Carboxylic and Boronic Acids: Effect on Enzyme Inhibition and Antiviral Activity and Protein‐Ligand X‐ray Structural Studies

Arun K. Ghosh, I. Weber, H. Mitsuya, 2019, ChemMedChem.

4′‐modified nucleoside analogs: Potent inhibitors active against entecavir‐resistant hepatitis B virus

S. Sarafianos, D. Venzon, H. Mitsuya, 2015, Hepatology.

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

Arun K. Ghosh, I. Weber, H. Mitsuya, 2010, ChemMedChem.

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

Arun K. Ghosh, H. Mitsuya, Y. Koh, 2011, Antimicrobial Agents and Chemotherapy.

Conserved hydrogen-bonding network of P2 bis-tetrahydrofuran

Arun K. Ghosh, P. Wingfield, J. Kaufman, 2014 .

GRL-142 binds to and impairs HIV-1 integrase nuclear localization signal and potently suppresses highly INSTI-resistant HIV-1 variants

Arun K. Ghosh, N. Kishimoto, K. Murayama, 2023, Science advances.

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

Arun K. Ghosh, H. Mitsuya, Pedro Miguel, 2014 .

A novel HIV-1 protease inhibitor, GRL-044, has potent activity against various HIV-1s with an extremely high genetic barrier to the emergence of HIV-1 drug resistance.

Arun K. Ghosh, H. Mitsuya, Y. Takamatsu, 2019, Global health & medicine.