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Identification of potent farnesoid X receptor (FXR) antagonist showing favorable PK profile and distribution toward target tissues: Comprehensive understanding of structure-activity relationship of FXR antagonists.
Teno N, Yamashita Y, Masuda A, Iguchi Y, Oda K, Fujimori K, Hiramoto T, Nishimaki-Mogami T, Une M, Gohda K. Teno N, et al. Bioorg Med Chem. 2019 Jun 1;27(11):2220-2227. doi: 10.1016/j.bmc.2019.04.029. Epub 2019 Apr 20. Bioorg Med Chem. 2019. PMID: 31029550
Design and identification of a new farnesoid X receptor (FXR) partial agonist by computational structure-activity relationship analysis: Ligand-induced H8 helix fluctuation in the ligand-binding domain of FXR may lead to partial agonism.
Gohda K, Iguchi Y, Masuda A, Fujimori K, Yamashita Y, Teno N. Gohda K, et al. Among authors: teno n. Bioorg Med Chem Lett. 2021 Jun 1;41:128026. doi: 10.1016/j.bmcl.2021.128026. Epub 2021 Apr 9. Bioorg Med Chem Lett. 2021. PMID: 33839252
51 results