A small molecule compound with an indole moiety inhibits the main protease of SARS-CoV-2 and blocks virus replication von Hattori, Shin-ichiro, Higashi-Kuwata, Nobuyo, Hayashi, Hironori, Allu, Srinivasa Rao, Raghavaiah, Jakka, Bulut, Haydar, Das, Debananda, Anson, Brandon J., Lendy, Emma K., Takamatsu, Yuki, Takamune, Nobutoki, Kishimoto, Naoki, Murayama, Kazutaka, Hasegawa, Kazuya, Li, Mi, Davis, David A., Kodama, Eiichi N., Yarchoan, Robert, Wlodawer, Alexander, Misumi, Shogo, Mesecar, Andrew D., Ghosh, Arun K., Mitsuya, Hiroaki

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Syrian hamsters as a small animal model for SARS-CoV-2 infection and countermeasure development von Imai, Masaki, Iwatsuki-Horimoto, Kiyoko, Hatta, Masato, Loeber, Samantha, Halfmann, Peter J., Nakajima, Noriko, Watanabe, Tokiko, Ujie, Michiko, Takahashi, Kenta, Ito, Mutsumi, Yamada, Shinya, Fan, Shufang, Chiba, Shiho, Kuroda, Makoto, Guan, Lizheng, Takada, Kosuke, Armbrust, Tammy, Balogh, Aaron, Furusawa, Yuri, Okuda, Moe, Ueki, Hiroshi, Yasuhara, Atsuhiro, Sakai-Tagawa, Yuko, Lopes, Tiago J. S., Kiso, Maki, Yamayoshi, Seiya, Kinoshita, Noriko, Ohmagari, Norio, Hattori, Shin-ichiro, Takeda, Makoto, Mitsuya, Hiroaki, Krammer, Florian, Suzuki, Tadaki, Kawaoka, Yoshihiro

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Structure–Activity Relationship Studies of SARS-CoV‑2 Main Protease Inhibitors Containing 4‑Fluorobenzothiazole-2-carbonyl Moieties von Tsuji, Kohei, Ishii, Takahiro, Kobayakawa, Takuya, Higashi-Kuwata, Nobuyo, Shinohara, Kouki, Azuma, Chika, Miura, Yutaro, Nakano, Hiroki, Wada, Naoya, Hattori, Shin-ichiro, Bulut, Haydar, Mitsuya, Hiroaki, Tamamura, Hirokazu

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GRL-0920, an Indole Chloropyridinyl Ester, Completely Blocks SARS-CoV-2 Infection von Hattori, Shin-ichiro, Higshi-Kuwata, Nobuyo, Raghavaiah, Jakka, Das, Debananda, Bulut, Haydar, Davis, David A., Takamatsu, Yuki, Matsuda, Kouki, Takamune, Nobutoki, Kishimoto, Naoki, Okamura, Tadashi, Misumi, Shogo, Yarchoan, Robert, Maeda, Kenji, Ghosh, Arun K., Mitsuya, Hiroaki

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Structural features in common of HBV and HIV-1 resistance against chirally-distinct nucleoside analogues entecavir and lamivudine von Yasutake, Yoshiaki, Hattori, Shin-ichiro, Tamura, Noriko, Matsuda, Kouki, Kohgo, Satoru, Maeda, Kenji, Mitsuya, Hiroaki

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Design of Highly Potent, Dual‐Acting and Central‐Nervous‐System‐Penetrating HIV‐1 Protease Inhibitors with Excellent Potency against Multidrug‐Resistant HIV‐1 Variants... von Ghosh, Arun K., Rao, Kalapala Venkateswara, Nyalapatla, Prasanth R., Kovela, Satish, Brindisi, Margherita, Osswald, Heather L., Sekhara Reddy, Bhavanam, Agniswamy, Johnson, Wang, Yuan‐Fang, Aoki, Manabu, Hattori, Shin‐ichiro, Weber, Irene T., Mitsuya, Hiroaki

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Exploratory Studies of Effective Inhibitors against the SARS-CoV-2 Main Protease by Halogen Incorporation and Amide Bond Replacement von Tsuji, Kohei, Kobayakawa, Takuya, Ishii, Takahiro, Higashi-Kuwata, Nobuyo, Azuma, Chika, Shinohara, Kouki, Miura, Yutaro, Yamamoto, Kenichi, Nishimura, Soshi, Hattori, Shin-ichiro, Bulut, Haydar, Mitsuya, Hiroaki, Tamamura, Hirokazu

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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 von Bulut, Haydar, Hattori, Shin-ichiro, Aoki-Ogata, Hiromi, Hayashi, Hironori, Das, Debananda, Aoki, Manabu, Davis, David A., Rao, Kalapala Venkateswara, Nyalapatla, Prasanth R., Ghosh, Arun K., Mitsuya, Hiroaki

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Design and Synthesis of Potent HIV‑1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure–Activity Studies and Biological and X‑ray Structura... von Ghosh, Arun K, Williams, Jacqueline N, Ho, Rachel Y, Simpson, Hannah M, Hattori, Shin-ichiro, Hayashi, Hironori, Agniswamy, Johnson, Wang, Yuan-Fang, Weber, Irene T, Mitsuya, Hiroaki

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A novel central nervous system-penetrating protease inhibitor overcomes human immunodeficiency virus 1 resistance with unprecedented aM to pM potency von Aoki, Manabu, Hayashi, Hironori, Rao, Kalapala Venkateswara, Das, Debananda, Higashi-Kuwata, Nobuyo, Bulut, Haydar, Aoki-Ogata, Hiromi, Takamatsu, Yuki, Yedidi, Ravikiran S, Davis, David A, Hattori, Shin-Ichiro, Nishida, Noriko, Hasegawa, Kazuya, Takamune, Nobutoki, Nyalapatla, Prasanth R, Osswald, Heather L, Jono, Hirofumi, Saito, Hideyuki, Yarchoan, Robert, Misumi, Shogo, Ghosh, Arun K, Mitsuya, Hiroaki

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Potent HIV-1 protease inhibitors incorporating squaramide-derived P2 ligands: Design, synthesis, and biological evaluation von Ghosh, Arun K., Williams, Jacqueline N., Kovela, Satish, Takayama, Jun, Simpson, Hannah M., Walters, D. Eric, Hattori, Shin-ichiro, Aoki, Manabu, Mitsuya, Hiroaki

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Chloropyridinyl Esters of Nonsteroidal Anti-Inflammatory Agents and Related Derivatives as Potent SARS-CoV-2 3CL Protease Inhibitors von Ghosh, Arun K., Shahabi, Dana, Yadav, Monika, Kovela, Satish, Anson, Brandon J., Lendy, Emma K., Bonham, Connie, Sirohi, Devika, Brito-Sierra, Carlos A., Hattori, Shin-Ichiro, Kuhn, Richard, Mitsuya, Hiroaki, Mesecar, Andrew D.

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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 von Delino, Nicole S, Aoki, Manabu, Hayashi, Hironori, Hattori, Shin-Ichiro, Chang, Simon B, Takamatsu, Yuki, Martyr, Cuthbert D, Das, Debananda, Ghosh, Arun K, Mitsuya, Hiroaki

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Neutralising activity and antibody titre in 10 patients with breakthrough infections of the SARS-CoV-2 Omicron variant in Japan von Okumura, Nobumasa, Tsuzuki, Shinya, Saito, Sho, Hattori, Shin-ichiro, Takeuchi, Junko S., Saito, Tomoya, Ujiie, Mugen, Hojo, Masayuki, Iwamoto, Noriko, Sugiura, Wataru, Mitsuya, Hiroaki, Ohmagari, Norio

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Generation of Angiotensin-Converting Enzyme 2/Transmembrane Protease Serine 2-Double-Positive Human Induced Pluripotent Stem Cell-Derived Spheroids for Anti-Severe Acute Respirator... von Higashi-Kuwata, Nobuyo, Yabe, Shigeharu G, Fukuda, Satsuki, Nishida, Junko, Tamura-Nakano, Miwa, Hattori, Shin-Ichiro, Okochi, Hitoshi, Mitsuya, Hiroaki

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Indole Chloropyridinyl Ester-Derived SARS-CoV‑2 3CLpro Inhibitors: Enzyme Inhibition, Antiviral Efficacy, Structure–Activity Relationship, and X‑ray Structural Studies von Ghosh, Arun K, Raghavaiah, Jakka, Shahabi, Dana, Yadav, Monika, Anson, Brandon J, Lendy, Emma K, Hattori, Shin-ichiro, Higashi-Kuwata, Nobuyo, Mitsuya, Hiroaki, Mesecar, Andrew D

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Potent and biostable inhibitors of the main protease of SARS-CoV-2 von Tsuji, Kohei, Ishii, Takahiro, Kobayakawa, Takuya, Higashi-Kuwata, Nobuyo, Azuma, Chika, Nakayama, Miyuki, Onishi, Takato, Nakano, Hiroki, Wada, Naoya, Hori, Miki, Shinohara, Kouki, Miura, Yutaro, Kawada, Takuma, Hayashi, Hironori, Hattori, Shin-ichiro, Bulut, Haydar, Das, Debananda, Takamune, Nobutoki, Kishimoto, Naoki, Saruwatari, Junji, Okamura, Tadashi, Nakano, Kenta, Misumi, Shogo, Mitsuya, Hiroaki, Tamamura, Hirokazu

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Early phase dynamics of traceable mCherry fluorescent protein-carrying HIV-1 infection in human peripheral blood mononuclear cells-transplanted NOD/SCID/Jak3-/- mice von Higashi-Kuwata, Nobuyo, Ogata-Aoki, Hiromi, Hattori, Shin-ichiro, Hayashi, Hironori, Danish, Matthew, Aoki, Manabu, Shiotsu, Chiemi, Kawamura, Tatsuyoshi, Ihn, Hironobu, Kobayashi, Hisataka, Okada, Seiji, Mitsuya, Hiroaki

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Active-site deformation in the structure of HIV-1 RT with HBV-associated septuple amino acid substitutions rationalizes the differential susceptibility of HIV-1 and HBV against 4ʹ-... von Yasutake, Yoshiaki, Hattori, Shin-ichiro, Tamura, Noriko, Matsuda, Kouki, Kohgo, Satoru, Maeda, Kenji, Mitsuya, Hiroaki

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HIV-1 with HBV-associated Q151M substitution in RT becomes highly susceptible to entecavir: structural insights into HBV-RT inhibition by entecavir von Yasutake, Yoshiaki, Hattori, Shin-ichiro, Hayashi, Hironori, Matsuda, Kouki, Tamura, Noriko, Kohgo, Satoru, Maeda, Kenji, Mitsuya, Hiroaki

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