Development of novel therapeutics for human immunodeficiency virus infection
Using X-ray crystal structural analyses, we identified important interactions, which play key roles in highly potent activity of the novel compounds against both wild-type and drug-resistant HIV-1 strains and their substantially high genetic barrier.
Development of novel antibacterial compounds
We identified novel antibacterial drugs and analyzed their antibacterial mechanisms.
Oe C, et al. (2020) Pyrimidine analogs as a new class of Gram-positive antibiotics, mainly targeting thymineless-death related proteins. ACS Infectious Diseases, 6(6), 1490, doi: 10.1021/acsinfecdis.9b00305.
Tsukada K, et al. (2020) Synthetic biology based construction of biological activity-related library of fungal decalin-containing diterpenoid pyrones. Nature Communications, 11(1), 1830, doi: 10.1038/s41467-020-15664-4
Aoki M, et al. (2017) A novel central nervous system-penetrating protease inhibitor overcomes human immunodeficiency virus 1 resistance with unprecedented aM to pM potency. eLife, 6, e28020. doi:10.7554/eLife.28020.
Aoki M, et al. (2015) C-5-Modified Tetrahydropyrano-Tetrahydofuran-Derived Protease Inhibitors (PIs) Exert Potent Inhibition of the Replication of HIV-1 Variants Highly Resistant to Various PIs, including Darunavir. Journal of Virology, 90(5), 2180.
Hayashi H, et al. (2014) Dimerization of HIV-1 Protease Occurs through Two Steps Relating to the Mechanism of Protease Dimerization Inhibition by Darunavir. Proceedings of the National Academy of Sciences of the United States of America, 111(33), 12234, doi:10.1073/pnas.1400027111