[HTML][HTML] 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… - Nature …, 2021 - nature.com
Except remdesivir, no specific antivirals for SARS-CoV-2 infection are currently available.
Here, we characterize two small-molecule-compounds, named GRL-1720 and 5h, containing …

[HTML][HTML] Characterization of monocyte/macrophage subsets in the skin and peripheral blood derived from patients with systemic sclerosis

N Higashi-Kuwata, M Jinnin, T Makino… - Arthritis research & …, 2010 - Springer
Introduction Recent accumulating evidence indicates a crucial involvement of macrophage
lineage in the pathogenesis of systemic sclerosis (SSc). To analyze the assembly of the …

Indole chloropyridinyl ester-derived SARS-CoV-2 3CLpro inhibitors: enzyme inhibition, antiviral efficacy, structure–activity relationship, and X-ray structural studies

…, EK Lendy, S Hattori, N Higashi-Kuwata… - Journal of medicinal …, 2021 - ACS Publications
Here, we report the synthesis, structure–activity relationship studies, enzyme inhibition,
antiviral activity, and X-ray crystallographic studies of 5-chloropyridinyl indole carboxylate …

[HTML][HTML] 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… - Nature …, 2023 - nature.com
COVID-19 caused by SARS-CoV-2 has continually been serious threat to public health
worldwide. While a few anti-SARS-CoV-2 therapeutics are currently available, their antiviral …

Alternatively activated macrophages (M2 macrophages) in the skin of patient with localized scleroderma

N HigashiKuwata, T Makino, Y Inoue… - Experimental …, 2009 - Wiley Online Library
Localized scleroderma is a connective tissue disorder that is limited to the skin and subcutaneous
tissue. Macrophages have been reported to be particularly activated in patients with …

Structure–Activity Relationship Studies of SARS-CoV-2 Main Protease Inhibitors Containing 4-Fluorobenzothiazole-2-carbonyl Moieties

…, T Ishii, T Kobayakawa, N Higashi-Kuwata… - Journal of Medicinal …, 2023 - ACS Publications
The main protease (M pro ) of SARS-CoV-2 is an attractive target for the development of
drugs to treat COVID-19. Here, we report the design, synthesis, and structure–activity …

[PDF][PDF] Potent and biostable inhibitors of the main protease of SARS-CoV-2

K Tsuji, T Ishii, T Kobayakawa, N Higashi-Kuwata… - Iscience, 2022 - cell.com
Potent and biostable inhibitors of the main protease (M pro ) of SARS-CoV-2 were designed
and synthesized based on an active hit compound 5h (2). Our strategy was based not only …

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

…, D Das, DJ Venzon, M Amano, N HigashiKuwata… - …, 2015 - Wiley Online Library
Certain nucleoside/nucleotide reverse transcriptase (RT) inhibitors (NRTIs) are effective
against human immunodeficiency virus type 1 (HIV‐1) and hepatitis B virus (HBV). However, …

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

M Aoki, H Hayashi, KV Rao, D Das, N Higashi-Kuwata… - Elife, 2017 - elifesciences.org
10.7554/eLife.28020.001 Antiretroviral therapy for HIV-1 infection/AIDS has significantly
extended the life expectancy of HIV-1-infected individuals and reduced HIV-1 transmission at …

Highly neutralizing COVID-19 convalescent plasmas potently block SARS-CoV-2 replication and pneumonia in Syrian hamsters

…, K Maeda, N Nakajima, N Higashi-Kuwata… - Journal of …, 2022 - Am Soc Microbiol
Despite various attempts to treat severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)-infected
patients with COVID-19 convalescent plasmas, neither appropriate approach …