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- W2047919835 abstract "Previously, we reported that 22S-butyl-25,26,27-trinor-1α,24-dihydroxyvitamin D32 represents a new class of antagonist for the vitamin D receptor (VDR). The crystal structure of the ligand-binding domain (LBD) of VDR complexed with 2 showed the formation of a butyl pocket to accommodate the 22-butyl group and insufficient interactions between ligand 2 and the C-terminus of VDR. Here, we designed and synthesized new analogues 5a–c and evaluated their biological activities to probe whether agonistic activity is recovered when the analogue restores interactions with the C-terminus of VDR. Analogues 5a–c exhibited full agonistic activity in transactivation. Interestingly, 5c, which bears a 24-diethyl group, completely recovered agonistic activity, although 3c and 4c act as an antagonist and a weak agonist, respectively. The crystal structures of VDR-LBD complexed with 3a, 4a, 5a, and 5c were solved, and the results confirmed that butyl pocket formation in VDR strongly affects the agonistic or antagonistic behaviors of ligands." @default.
- W2047919835 created "2016-06-24" @default.
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- W2047919835 date "2012-04-27" @default.
- W2047919835 modified "2023-09-23" @default.
- W2047919835 title "Butyl Pocket Formation in the Vitamin D Receptor Strongly Affects the Agonistic or Antagonistic Behavior of Ligands" @default.
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- W2047919835 doi "https://doi.org/10.1021/jm300230a" @default.
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