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… - Science …, 2023 - science.org
Nuclear localization signal (NLS) of HIV-1 integrase (IN) is implicated in nuclear import of
HIV-1 preintegration complex (PIC). Here, we established a multiclass drug-resistant HIV-1 …

[HTML][HTML] Identification of a novel long-acting 4'-modified nucleoside reverse transcriptase inhibitor against HBV

N Higashi-Kuwata, S Hayashi, H Kumamoto… - Journal of …, 2021 - Elsevier
Background & Aims While certain nucleos (t) ide reverse transcriptase inhibitors (NRTIs) are
efficacious in treating HBV infection, their effects are yet to be optimized and the emergence …

FMO-guided design of darunavir analogs as HIV-1 protease inhibitors

H Chuntakaruk, K Hengphasatporn, Y Shigeta… - Scientific Reports, 2024 - nature.com
The prevalence of HIV-1 infection continues to pose a significant global public health issue,
highlighting the need for antiretroviral drugs that target viral proteins to reduce viral …

Self-assembled enzymatic nanowires with a “dry and wet” interface improve the catalytic performance of januvia transaminase in organic solvents

C Wei, J Zhou, T Liu, W Zhao, XE Zhang, D Men - ACS Catalysis, 2021 - ACS Publications
The use of organic solvents in enzymatic reactions is advantageous for industrial
bioprocesses. However, enzymes tend to denature in organic solvents. To solve this …

HIV-1 protease inhibitors and mechanisms of HIV-1's resistance

D Das - Global Health & Medicine, 2024 - jstage.jst.go.jp
Current anti-HIV drugs have significantly improved the prognosis of HIV infected patients so
much so that it is now considered a chronic disease, and adherence to medications keeps …

[HTML][HTML] A lipid index for risk of hyperlipidemia caused by anti-retroviral drugs

M Shimura, N Higashi-Kuwata, A Fujiwara… - Antiviral Research, 2024 - Elsevier
HIV-associated lipodystrophy has been reported in people taking anti-retroviral therapy
(ART). Lipodystrophy can cause cardiovascular diseases, affecting the quality of life of HIV …

7-Deaza-7-fluoro modification confers on 4′-cyano-nucleosides potent activity against entecavir/adefovir-resistant HBV variants and favorable safety

S Hayashi, N Higashi-Kuwata, D Das, K Tomaya… - Antiviral research, 2020 - Elsevier
We designed, synthesized and identified a novel nucleoside derivative, 4′-C-cyano-7-
deaza-7-fluoro-2′-deoxyadenosine (CdFA), which exerts potent anti-HBV activity (IC 50 …