Beyond darunavir: recent development of next generation HIV-1 protease inhibitors to combat drug resistance

AK Ghosh, IT Weber, H Mitsuya - Chemical Communications, 2022 - pubs.rsc.org
We report our recent development of a conceptually new generation of exceptionally potent
non-peptidic HIV-1 protease inhibitors that displayed excellent pharmacological and drug …

[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 …

[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 …

[HTML][HTML] Synthesis, computational and experimental pharmacological studies for (thio) ether-triazine 5-HT6R ligands with noticeable action on AChE/BChE and …

K Czarnota-Łydka, S Sudoł-Tałaj… - European Journal of …, 2023 - Elsevier
Alzheimer's disease is becoming a growing problem increasing at a tremendous rate.
Serotonin 5-HT 6 receptors appear to be a particularly attractive target from a therapeutic …

A direct entry to polycyclic quinoxaline derivatives via I 2-DMSO mediated oxidative decarboxylation of α-amino acids and the subsequent Pictet–Spengler cyclization …

SK Samanta, R Sarkar, U Sengupta, S Das… - Organic & …, 2022 - pubs.rsc.org
A facile and highly efficient iodine-promoted strategy has been delineated for the synthesis
of indolo and pyrrolo [1, 2-a] quinoxaline derivatives via an oxidative Pictet–Spengler type …

Advanced molecular mechanisms of modified DRV compounds in targeting HIV-1 protease mutations and interrupting monomer dimerization

B Tang, S Luo, Q Wang, P Gao, L Duan - Physical Chemistry Chemical …, 2024 - pubs.rsc.org
HIV-1 protease (PR) plays a crucial role in the treatment of HIV as a key target. The global
issue of emerging drug resistance is escalating, and PR mutations pose a substantial …

[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 …

Selection of HIV-1 for resistance to fifth-generation protease inhibitors reveals two independent pathways to high-level resistance

E Spielvogel, SK Lee, S Zhou, GJ Lockbaum, M Henes… - Elife, 2023 - elifesciences.org
Darunavir (DRV) is exceptional among potent HIV-1 protease inhibitors (PIs) in high drug
concentrations that are achieved in vivo. Little is known about the de novo resistance …

An update on antiretroviral therapy

L Menéndez-Arias, S Martín-Alonso… - Antiviral drug discovery …, 2021 - Springer
Human immunodeficiency virus (HIV) infection and acquired immune deficiency syndrome
(AIDS) still claim many lives across the world. However, research efforts during the last 40 …

Design of soft x-ray fluorescence microscopy beyond 100-nm spatial resolution with ultrashort Kirkpatrick-Baez mirror

T Shimamura, Y Takeo, F Moriya… - Advances in X-Ray …, 2022 - spiedigitallibrary.org
A Kirkpatrick-Baez (KB) mirror is a reflective focusing device that sequentially positions a
pair of crossed mirrors in a grazing-incidence setup. Typically, this type of device offers a …