Development of Noncovalent Small-Molecule Keap1-Nrf2 Inhibitors by Fragment-Based Drug Discovery

Autor: Dilip Narayanan, Kim T. Tran, Jakob S. Pallesen, Sara M. Ø. Solbak, Yuting Qin, Elina Mukminova, Martina Luchini, Kristina O. Vasilyeva, Dorleta González Chichón, Georgia Goutsiou, Cecilie Poulsen, Nanna Haapanen, Grzegorz M. Popowicz, Michael Sattler, David Olagnier, Michael Gajhede, Anders Bach

Publikováno v: Narayanan, D, Tran, K T, Pallesen, J S, Solbak, S M Ø, Qin, Y, Mukminova, E, Luchini, M, Vasilyeva, K O, González Chichón, D, Goutsiou, G, Poulsen, C, Haapanen, N, Popowicz, G M, Sattler, M, Olagnier, D, Gajhede, M & Bach, A 2022, ' Development of Noncovalent Small-Molecule Keap1-Nrf2 Inhibitors by Fragment-Based Drug Discovery ', Journal of Medicinal Chemistry, vol. 65, no. 21, pp. 14481–14526 . https://doi.org/10.1021/acs.jmedchem.2c00830

Targeting the protein-protein interaction (PPI) between the transcription factor nuclear factor erythroid 2-related factor 2 (Nrf2) and its repressor, Kelch-like ECH-associated protein 1 (Keap1), constitutes a promising strategy for treating diseases

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https://pubmed.ncbi.nlm.nih.gov/36263945