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Open access Sep 2026

Inter-domain distance analysis reveals conformational changes in the Keap1-Nrf2 stress sensor system

The Keap1-Nrf2 system plays a central role in cellular defense against oxidative stress. Structural information on full-length Keap1 is essential for understanding the molecular basis of this regulation. However, its overall architecture has remained elusive due to pronounced conformational flexibility. In this study,...

Ritsumi Saito, Takeshi Kawabata, S. Yamashita et al. · 0 citations
Sep 2026

Exploiting Bridged Conformations for Precise Molecular Recognition in the Design of KRAS-Selective, Orally Available Macrocyclic Peptides

Macrocyclic peptides are attracting attention as a promising therapeutic modality for addressing intracellular targets that are traditionally difficult to address with conventional small molecules or antibodies. In this study, we present the chemical optimization process behind the development of AUBE00 (AP7400, comp...

M. Kage, Hatsuo Kawada, Koji Takano et al. · 0 citations

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