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  1. Article ; Online: Correction for Nakajima et al., "Biochemical and Structural Properties of Entecavir-Resistant Hepatitis B Virus Polymerase with L180M/M204V Mutations".

    Nakajima, Shogo / Watashi, Koichi / Kato, Takanobu / Muramatsu, Masamichi / Wakita, Takaji / Tamura, Noriko / Hattori, Shin-Ichiro / Maeda, Kenji / Mitsuya, Hiroaki / Yasutake, Yoshiaki / Toyoda, Tetsuya

    Journal of virology

    2024  Volume 98, Issue 3, Page(s) e0182323

    Language English
    Publishing date 2024-02-02
    Publishing country United States
    Document type Journal Article ; Published Erratum
    ZDB-ID 80174-4
    ISSN 1098-5514 ; 0022-538X
    ISSN (online) 1098-5514
    ISSN 0022-538X
    DOI 10.1128/jvi.01823-23
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  2. Article ; Online: Fibroblast growth factor receptor 1 as a potential marker of terminal effector peripheral T helper cells in rheumatoid arthritis patients.

    Etori, Keishi / Tanaka, Shigeru / Tamura, Jun / Hattori, Koto / Kagami, Shin-Ichiro / Nakamura, Junichi / Ohtori, Seiji / Nakajima, Hiroshi

    Rheumatology (Oxford, England)

    2023  Volume 62, Issue 11, Page(s) 3763–3769

    Abstract: Objectives: RA is an autoimmune disease characterized by destructive polyarthritis. CD4+ T cells are pivotal to its pathogenesis, and our previous study revealed the expression of fibroblast growth factor receptor 1 (FGFR1) is modulated by MTX treatment ...

    Abstract Objectives: RA is an autoimmune disease characterized by destructive polyarthritis. CD4+ T cells are pivotal to its pathogenesis, and our previous study revealed the expression of fibroblast growth factor receptor 1 (FGFR1) is modulated by MTX treatment in CD4+ T cells of RA patients; however, the roles of FGFR1 in CD4+ T cells in the pathogenesis of RA is unclear. Therefore, in this study, we aimed to characterize FGFR1-positive CD4+ T cells in RA patients.
    Methods: The abundance of FGFR1-positive CD4+ T cells in peripheral blood and synovium was determined. Single-cell RNA sequencing (scRNA-seq) was performed on synovial CD4+ T cells to characterize FGFR1-positive cells. In addition, T cell activation status and cytokine production were determined using flow cytometry.
    Results: The percentage of FGFR1-positive CD4+ T cells in the peripheral blood was higher in RA patients than in healthy controls (P =0.0035). They were also present in the synovium of active RA patients. The results of scRNA-seq revealed that peripheral Th (Tph) cells preferentially expressed FGFR1. Additionally, these FGFR1-positive Tph cells displayed a terminal effector cell phenotype. Consistent with this finding, FGFR1-positive CD4+ T cells in peripheral blood expressed IL-21 and IFN-γ.
    Conclusion: Our study provides evidence that FGFR1 marks terminal effector Tph cells in patients with RA.
    MeSH term(s) Humans ; Receptor, Fibroblast Growth Factor, Type 1/metabolism ; T-Lymphocytes, Helper-Inducer ; Arthritis, Rheumatoid ; CD4-Positive T-Lymphocytes/metabolism ; Synovial Membrane/pathology
    Chemical Substances Receptor, Fibroblast Growth Factor, Type 1 (EC 2.7.10.1)
    Language English
    Publishing date 2023-05-13
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1464822-2
    ISSN 1462-0332 ; 1462-0324
    ISSN (online) 1462-0332
    ISSN 1462-0324
    DOI 10.1093/rheumatology/kead220
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  3. Article ; Online: Exploration of P1 and P4 modifications of nirmatrelvir: Design, synthesis, biological evaluation, and X-ray structural studies of SARS-CoV-2 Mpro inhibitors.

    Ghosh, Arun K / Yadav, Monika / Iddum, Satyanarayana / Ghazi, Somayeh / Lendy, Emma K / Jayashankar, Uttara / Beechboard, Sydney N / Takamatsu, Yuki / Hattori, Shin-Ichiro / Aamano, Masayuki / Higashi-Kuwata, Nobuyo / Mitsuya, Hiroaki / Mesecar, Andrew D

    European journal of medicinal chemistry

    2024  Volume 267, Page(s) 116132

    Abstract: We report the synthesis, biological evaluation, and X-ray structural studies of a series of SARS-CoV-2 Mpro inhibitors based upon the X-ray crystal structure of nirmatrelvir, an FDA approved drug that targets the main protease of SARS-CoV-2. The studies ... ...

    Abstract We report the synthesis, biological evaluation, and X-ray structural studies of a series of SARS-CoV-2 Mpro inhibitors based upon the X-ray crystal structure of nirmatrelvir, an FDA approved drug that targets the main protease of SARS-CoV-2. The studies involved examination of various P4 moieties, P1 five- and six-membered lactam rings to improve potency. In particular, the six-membered P1 lactam ring analogs exhibited high SARS-CoV-2 Mpro inhibitory activity. Several compounds effectively blocked SARS-CoV-2 replication in VeroE6 cells. One of these compounds maintained good antiviral activity against variants of concern including Delta and Omicron variants. A high-resolution X-ray crystal structure of an inhibitor bound to SARS-CoV-2 Mpro was determined to gain insight into the ligand-binding properties in the Mpro active site.
    MeSH term(s) Humans ; X-Rays ; SARS-CoV-2 ; COVID-19 ; Lactams ; Leucine ; Nitriles ; Protease Inhibitors/pharmacology ; Antiviral Agents/pharmacology ; Molecular Docking Simulation
    Chemical Substances Lactams ; Leucine (GMW67QNF9C) ; Nitriles ; Protease Inhibitors ; Antiviral Agents
    Language English
    Publishing date 2024-02-01
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2024.116132
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  4. Article ; Online: Structure-Activity Relationship Studies of SARS-CoV-2 Main Protease Inhibitors Containing 4-Fluorobenzothiazole-2-carbonyl Moieties.

    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

    Journal of medicinal chemistry

    2023  Volume 66, Issue 19, Page(s) 13516–13529

    Abstract: The main protease ( ... ...

    Abstract The main protease (M
    Language English
    Publishing date 2023-09-27
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.3c00777
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    Zs.MB 1: Show issues

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  5. Article ; Online: Generation of Angiotensin-Converting Enzyme 2/Transmembrane Protease Serine 2-Double-Positive Human Induced Pluripotent Stem Cell-Derived Spheroids for Anti-Severe Acute Respiratory Syndrome Coronavirus 2 Drug Evaluation.

    Higashi-Kuwata, Nobuyo / Yabe, Shigeharu G / Fukuda, Satsuki / Nishida, Junko / Tamura-Nakano, Miwa / Hattori, Shin-Ichiro / Okochi, Hitoshi / Mitsuya, Hiroaki

    Microbiology spectrum

    2022  , Page(s) e0349022

    Abstract: We newly generated two human induced pluripotent stem cell (hiPSC)-derived spheroid lines, termed ... ...

    Abstract We newly generated two human induced pluripotent stem cell (hiPSC)-derived spheroid lines, termed Spheroids_
    Language English
    Publishing date 2022-10-31
    Publishing country United States
    Document type Journal Article
    ZDB-ID 2807133-5
    ISSN 2165-0497 ; 2165-0497
    ISSN (online) 2165-0497
    ISSN 2165-0497
    DOI 10.1128/spectrum.03490-22
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  6. Article ; Online: Exploratory Studies of Effective Inhibitors against the SARS-CoV-2 Main Protease by Halogen Incorporation and Amide Bond Replacement.

    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

    Chemical & pharmaceutical bulletin

    2023  Volume 71, Issue 12, Page(s) 879–886

    Abstract: In the development of anti-severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) drugs, its main protease ( ... ...

    Abstract In the development of anti-severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) drugs, its main protease (M
    MeSH term(s) Animals ; Mice ; COVID-19 ; SARS-CoV-2 ; Amides/pharmacology ; Halogens ; Protease Inhibitors/chemistry ; Viral Nonstructural Proteins ; Antiviral Agents/chemistry
    Chemical Substances 3C-like proteinase, SARS-CoV-2 (EC 3.4.22.-) ; Amides ; Halogens ; ensitrelvir (PX665RAA3H) ; Protease Inhibitors ; Viral Nonstructural Proteins ; Antiviral Agents
    Language English
    Publishing date 2023-12-03
    Publishing country Japan
    Document type Journal Article
    ZDB-ID 213307-6
    ISSN 1347-5223 ; 0009-2363
    ISSN (online) 1347-5223
    ISSN 0009-2363
    DOI 10.1248/cpb.c23-00562
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    Zs.A 770: Show issues Location:
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  7. Article: Standard strategies for diagnosis and treatment of patients with newly diagnosed Parkinson disease: JAPAN.

    Kubo, Shin-Ichiro / Hatano, Taku / Oyama, Genko / Hattori, Nobutaka

    Neurology. Clinical practice

    2018  Volume 3, Issue 6, Page(s) 477–478

    Language English
    Publishing date 2018-08-13
    Publishing country United States
    Document type Journal Article
    ZDB-ID 2645818-4
    ISSN 2163-0933 ; 2163-0402
    ISSN (online) 2163-0933
    ISSN 2163-0402
    DOI 10.1212/01.CPJ.0000437021.22294.25
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  8. Article ; Online: SARS-CoV-2 papain-like protease (PLpro) inhibitory and antiviral activity of small molecule derivatives for drug leads.

    Ghosh, Arun K / Shahabi, Dana / Imhoff, Mackenzie E C / Kovela, Satish / Sharma, Ashish / Hattori, Shin-Ichiro / Higashi-Kuwata, Nobuyo / Mitsuya, Hiroaki / Mesecar, Andrew D

    Bioorganic & medicinal chemistry letters

    2023  Volume 96, Page(s) 129489

    Abstract: We report here the synthesis and biological evaluation of a series of small molecule SARS-CoV-2 PLpro inhibitors. We compared the activity of selected compounds in both SARS-CoV-1 and SARS-CoV-2 PLpro inhibitory and antiviral assays. We have synthesized ... ...

    Abstract We report here the synthesis and biological evaluation of a series of small molecule SARS-CoV-2 PLpro inhibitors. We compared the activity of selected compounds in both SARS-CoV-1 and SARS-CoV-2 PLpro inhibitory and antiviral assays. We have synthesized and evaluated several new structural variants of previous leads against SARS-CoV-2 PLpro. The replacement of the carboxamide functionality with sulfonamide derivatives resulted in PLpro inhibitors with potent PLpro inhibitory and antiviral activity in VeroE6 cells similar to GRL0617. To obtain molecular insight, we created an optimized model of a potent sulfonamide derivative in the SARS-CoV-2 PLpro active site.
    MeSH term(s) Humans ; SARS-CoV-2 ; COVID-19 ; Antiviral Agents/pharmacology ; Antiviral Agents/chemistry ; Sulfonamides/pharmacology
    Chemical Substances papain-like protease, SARS-CoV-2 (EC 3.4.22.2) ; Antiviral Agents ; Sulfonamides
    Language English
    Publishing date 2023-09-27
    Publishing country England
    Document type Journal Article ; Research Support, N.I.H., Intramural ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2023.129489
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  9. Article ; Online: A colossal barocaloric effect induced by the creation of a high-pressure phase.

    Zhang, Zhao / Jiang, Xiaoming / Hattori, Takanori / Xu, Xiong / Li, Min / Yu, Chenyang / Zhang, Zhe / Yu, Dehong / Mole, Richard / Yano, Shin-Ichiro / Chen, Jie / He, Lunhua / Wang, Chin-Wei / Wang, Hui / Li, Bing / Zhang, Zhidong

    Materials horizons

    2023  Volume 10, Issue 3, Page(s) 977–982

    Abstract: As a promising environment-friendly alternative to current vapor-compression refrigeration, solid-state refrigeration based on the barocaloric effect has been attracting worldwide attention. Generally, both phases in which a barocaloric effect occurs are ...

    Abstract As a promising environment-friendly alternative to current vapor-compression refrigeration, solid-state refrigeration based on the barocaloric effect has been attracting worldwide attention. Generally, both phases in which a barocaloric effect occurs are present at ambient pressure. Here, instead, we demonstrate that KPF
    Language English
    Publishing date 2023-03-06
    Publishing country England
    Document type Journal Article
    ZDB-ID 2744250-0
    ISSN 2051-6355 ; 2051-6347
    ISSN (online) 2051-6355
    ISSN 2051-6347
    DOI 10.1039/d2mh00905f
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  10. Article ; Online: 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.

    Ghosh, Arun K / Mishevich, Jennifer L / Kovela, Satish / Shaktah, Ryan / Ghosh, Ajay K / Johnson, Megan / Wang, Yuan-Fang / Wong-Sam, Andres / Agniswamy, Johnson / Amano, Masayuki / Takamatsu, Yuki / Hattori, Shin-Ichiro / Weber, Irene T / Mitsuya, Hiroaki

    European journal of medicinal chemistry

    2023  Volume 255, Page(s) 115385

    Abstract: Structure-based design, synthesis, X-ray structural studies, and biological evaluation of a new series of potent HIV-1 protease inhibitors are described. These inhibitors contain various pyridyl-pyrimidine, aryl thiazole or alkylthiazole derivatives as ... ...

    Abstract Structure-based design, synthesis, X-ray structural studies, and biological evaluation of a new series of potent HIV-1 protease inhibitors are described. These inhibitors contain various pyridyl-pyrimidine, aryl thiazole or alkylthiazole derivatives as the P2 ligands in combination with darunavir-like hydroxyethylamine sulfonamide isosteres. These heterocyclic ligands are inherent to kinase inhibitor drugs, such as nilotinib and imatinib. These ligands are designed to make hydrogen bonding interactions with the backbone atoms in the S2 subsite of HIV-1 protease. Various benzoic acid derivatives have been synthesized and incorporation of these ligands provided potent inhibitors that exhibited subnanomolar level protease inhibitory activity and low nanomolar level antiviral activity. Two high resolution X-ray structures of inhibitor-bound HIV-1 protease were determined. These structures provided important ligand-binding site interactions for further optimization of this class of protease inhibitors.
    MeSH term(s) HIV Protease Inhibitors/chemistry ; HIV-1/metabolism ; Imatinib Mesylate/pharmacology ; Ligands ; X-Rays ; HIV Protease/metabolism ; Crystallography, X-Ray ; Drug Design ; Structure-Activity Relationship
    Chemical Substances HIV Protease Inhibitors ; Imatinib Mesylate (8A1O1M485B) ; Ligands ; HIV Protease (EC 3.4.23.-)
    Language English
    Publishing date 2023-04-21
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2023.115385
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