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. 2023 Dec 9;14:8177. doi: 10.1038/s41467-023-44031-2

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© The Author(s) 2023

Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.

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Fig. 1 — a The crystal structure of DEX and GR in a complex with bile acid (PDB: 4UDC). b Schematic representation of GR-PROTACs (upper row) and the catalytic mode of action of PROTACs (lower row). c GR-PROTAC candidates and their individual linker lengths. d Representative image and e quantification of immunoblots of GR in HEK293 cells following GR-PROTAC treatments (n = 4). (two-way ANOVA main effects for time (F(4, 60) = 34.73, p = <0.0001) and for GR-PROTACs (F(3, 60) = 106.10, p = <0.0001); significant interaction (F(12, 60) = 7.81, p = <0.0001); follow-up Dunnett’s multiple comparisons between compounds vs. DMSO at 24 h KH-102 (p = <0.0001) and KH-103 (p = <0.0001). f Representative immunoblot and (g) quantification of HEK cells treated with various concentrations of KH-103 (n = 3). Two-way ANOVA: significant main effects for concentration (F(4, 30) = 22.91, p = <0.0001) and time (F(2, 30) = 14.43, p = <0.0001). h Representative immunoblot and quantifications of GR degradation by KH-103 in presence of MG-132 (n = 3). Two-way ANOVA: significant main effects for MG-132 (F(1, 8) = 13.90, p = 0.0058) and KH-103 (F(1, 8) = 29.70, p = 0.0006); significant interaction (F(1, 8) = 38.20, p = 0.0003). i Representative immunoblot and band quantification of GR in HEK293 cells following medium exchange (n = 3). Ordinary one-way ANOVA significant difference (F(2, 6) = 14.40, p = 0.0051). Follow-up Tukey’s multiple comparisons showed significant differences for DMSO vs. KH-103 (p = 0.0102) and KH-103 vs. washed (p = 0.0070). j Representative immunoblot and quantification of GR in HEK293 cells treated with KH-103 for up to four days. DMSO n = 6 (pooled 48 h and 96 h DMSO), all other conditions n = 3. Ordinary one-way ANOVA: significant difference (F(4, 13) = 100.00, p =<0.0001). P-values *<0.05, **<0.01, ***<0.001, ****<0.0001. Data are presented as mean values ± SEM. Source data are provided as a Source Data file.