Exploratory Studies of Effective Inhibitors against the SARS-CoV-2 Main Protease by Halogen Incorporation and Amide Bond Replacement K Tsuji, T Kobayakawa, T Ishii, N Higashi-Kuwata, C Azuma, K Shinohara, ... Chemical and Pharmaceutical Bulletin 71 (12), 879-886, 2023 | 1 | 2023 |
Structure–Activity Relationship Studies of SARS-CoV-2 Main Protease Inhibitors Containing 4-Fluorobenzothiazole-2-carbonyl Moieties K Tsuji, T Ishii, T Kobayakawa, N Higashi-Kuwata, K Shinohara, C Azuma, ... Journal of Medicinal Chemistry 66 (19), 13516-13529, 2023 | 4 | 2023 |
GRL-142 binds to and impairs HIV-1 integrase nuclear localization signal and potently suppresses highly INSTI-resistant HIV-1 variants M Aoki, H Aoki-Ogata, H Bulut, H Hayashi, N Takamune, N Kishimoto, ... Science advances 9 (28), eadg2955, 2023 | 1 | 2023 |
Identification of SARS-CoV-2 Mpro inhibitors containing P1’ 4-fluorobenzothiazole moiety highly active against SARS-CoV-2 N Higashi-Kuwata, K Tsuji, H Hayashi, H Bulut, M Kiso, M Imai, ... Nature Communications 14 (1), 1076, 2023 | 19 | 2023 |
Synthesis of novel entecavir analogues having 4′-cyano-6′′-fluoromethylenecyclopentene skeletons as an aglycone moiety as highly potent and long-acting anti-hepatitis B … H Kumamoto, N Higashi-Kuwata, S Hayashi, D Das, H Bulut, R Tokuda, ... RSC advances 13 (23), 15999-16011, 2023 | 2 | 2023 |
Design, Synthesis and Evaluation of Anti-Hepatitis B Virus (Hbv) Activity of Novel Entecavir Analogues Having 4′-Cyano-6 ″-Fluoromethylenecyclopentene Skeletons as an … H Kumamoto, N Higashi-Kuwata, S Hayashi, D Das, H Bulut, R Tokuda, ... Available at SSRN 4329576, 2023 | | 2023 |
Drug development targeting SARS-CoV-2 main protease H Bulut Global Health & Medicine 4 (6), 296-300, 2022 | 2 | 2022 |
Potent and biostable inhibitors of the main protease of SARS-CoV-2 K Tsuji, T Ishii, T Kobayakawa, N Higashi-Kuwata, C Azuma, ... Iscience 25 (11), 2022 | 10 | 2022 |
Regulation of retroviral and SARS-CoV-2 protease dimerization and activity through reversible oxidation DA Davis, H Bulut, P Shrestha, H Mitsuya, R Yarchoan Antioxidants 11 (10), 2054, 2022 | 4 | 2022 |
Regulation of the dimerization and activity of SARS-CoV-2 main protease through reversible glutathionylation of cysteine 300 DA Davis, H Bulut, P Shrestha, A Yaparla, HK Jaeger, S Hattori, ... Mbio 12 (4), 10.1128/mbio. 02094-21, 2021 | 18 | 2021 |
Identification of a novel long-acting 4’-modified nucleoside reverse transcriptase inhibitor against HBV N Higashi-Kuwata, S Hayashi, H Kumamoto, H Ogata-Aoki, D Das, ... Journal of hepatology 74 (5), 1075-1086, 2021 | 29 | 2021 |
A small molecule compound with an indole moiety inhibits the main protease of SARS-CoV-2 and blocks virus replication S Hattori, N Higashi-Kuwata, H Hayashi, SR Allu, J Raghavaiah, H Bulut, ... Nature communications 12 (1), 668, 2021 | 155 | 2021 |
GRL-0920, an indole chloropyridinyl ester, completely blocks SARS-CoV-2 infection S Hattori, N Higshi-Kuwata, J Raghavaiah, D Das, H Bulut, DA Davis, ... MBio 11 (4), 10.1128/mbio. 01833-20, 2020 | 54 | 2020 |
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 H Bulut, S Hattori, H Aoki-Ogata, H Hayashi, D Das, M Aoki, DA Davis, ... Scientific Reports 10 (1), 10664, 2020 | 12 | 2020 |
GRL-0920, an indole chloropyridinyl ester, completely blocks SARS-CoV-2 infection. mBio 11: e01833-20 SI Hattori, N Higshi-Kuwata, J Raghavaiah, D Das, H Bulut, DA Davis, ... | 6 | 2020 |
Novel Protease Inhibitors Containing C-5-Modified bis-Tetrahydrofuranylurethane and Aminobenzothiazole as P2 and P2′ Ligands That Exert Potent Antiviral … Y Takamatsu, M Aoki, H Bulut, D Das, M Amano, VR Sheri, LC Kovari, ... Antimicrobial agents and chemotherapy 63 (8), 10.1128/aac. 00372-19, 2019 | 14 | 2019 |
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 M Amano, H Bulut, S Tamiya, T Nakamura, Y Koh, H Mitsuya Scientific Reports 9 (1), 9806, 2019 | 8 | 2019 |
Disruption of endocytosis through chemical inhibition of clathrin heavy chain function W Dejonghe, I Sharma, B Denoo, S De Munck, Q Lu, K Mishev, H Bulut, ... Nature chemical biology 15 (6), 641-649, 2019 | 87 | 2019 |
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 … S Hattori, H Hayashi, H Bulut, KV Rao, PR Nyalapatla, K Hasegawa, ... Antimicrobial Agents and Chemotherapy 63 (6), 10.1128/aac. 02635-18, 2019 | 15 | 2019 |
Novel protease inhibitors markedly adapting to the structural plasticity of HIV-1 protease exert extreme potency with high genetic barrier H Bulut, M Aoki, H Hayashi, H Aoki-Ogata, S Hattori, AK Ghosh, H Mitsuya ACTA CRYSTALLOGRAPHICA A-FOUNDATION AND ADVANCES 74, A169-A169, 2018 | | 2018 |