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. 2021 Dec 14;40:392. doi: 10.1186/s13046-021-02199-9

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© The Author(s) 2021

Open AccessThis 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 licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence 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 licence, visit http://creativecommons.org/licenses/by/4.0/. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated in a credit line to the data.

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Fig. 1 — Kaempferol and quercetin bind NR4A1 and inhibit NR4A1-dependent transactivation. A Structures of kaempferol and quercetin. Different concentrations of kaempferol (B) and quercetin (C) were incubated with the ligand binding domain (LBD) of NR4A1 and binding was determined in fluorescent quenching direct binding or a competitive displacement (of bis-ANS) assay as outlined in the Materials and methods. Rh30 and Rh41 cells were transfected with D UAS-luc/Gal4-NR4A1 or E an NBRE-luc/flag-NR4A1 constructs and after treatment with kaempferol (K) or quercetin (Q) for 24 h, luciferase activity was determined and normalized to the DMSO values as outlined in the Materials and methods. Results are expressed as means ± SD for at least 3 replicated determinations and significant (p < 0.05) inhibition is indicated (*)