Efficient 5-LOX Species UGT1A1 inducers.Information AVAILABILITY STATEMENTThe original contributions presented inside the study are incorporated

Efficient 5-LOX Species UGT1A1 inducers.Information AVAILABILITY STATEMENTThe original contributions presented inside the study are incorporated in the article/Supplementary Material, further inquiries may be directed to the corresponding authors.AUTHOR CONTRIBUTIONSConception and style of study: X-QG and D-DW. Acquisition of information: Y-DZ, JC, Y-YZ, and R-MW. Drafting the manuscript: YDZ and X-QG. Evaluation and/or interpretation of data: SP, H-CB, and ML. Revising the manuscript critically for important intellectual content: MF, D-DW, and G-BG.FUNDINGThis perform was financially supported by the Outstanding Clinical Discipline Project of Shanghai Pudong (PWYgy2018-01), the NSF of China (82073813, 81922070, 81703604, 81773687), the National Key Research and Development Plan of China (2020YFC0845400, 2017YFC1700200, 2017YFC1702000), Program of Shanghai Academic/Technology Study Leader (18XD1403600), the Three-year Action Program of Shanghai TCM Improvement (ZY-(2018-2020)-CCCX-5001), the National Science and Technology Key Project of China (2018ZX09731016), the Shanghai Talent Improvement Fund (2019093) and Shuguang Program (18SG40) supported by Shanghai Education Improvement Foundation and Shanghai Municipal Education Commission.ACKNOWLEDGMENTS CONCLUSIONIn summary, this study reported an efficacious natural occurring UGT1A1 inducer and revealed its inductive mechanism. Following screening with the UGT1A1 inductive effects of 40 flavonoids, NBIF was found with all the most potent inductive effect on UGT1A1 and its potency was much more potent than the known UGT1A1 inducer chrysin in the transcription level. NBIF could induce UGT1A1 in both Caco2 cells and HepG2 cells, even though its inductive effects on UGT1A1 had been We would prefer to thank prof. Fei Li from Kunming Institute of Botany, Chinese Academy of DNA Methyltransferase custom synthesis Sciences, for FXR reporter assay.SUPPLEMENTARY MATERIALThe Supplementary Material for this short article might be located online at: https://www.frontiersin.org/articles/10.3389/fphar.2020.628314/ full#supplementary-material.Frontiers in Pharmacology | www.frontiersin.orgFebruary 2021 | Volume 11 | ArticleZhu et al.Neobavaisoflavone Induces UGT1A1 Enzyme
International Journal ofMolecular SciencesArticleThe Aryl Hydrocarbon Receptor Undergoes Chaperone-Mediated Autophagy in Triple-Negative Breast Cancer CellsJinyun Chen, Yujie Yang, Wade A. Russu and William K. Chan Department of Pharmaceutics Medicinal Chemistry, Thomas J. Lengthy College of Pharmacy, University with the Pacific, Stockton, CA 95211, USA; [email protected] (J.C.); [email protected] (Y.Y.); [email protected] (W.A.R.) Correspondence: [email protected]; Fax: +1-(209)-946-Abstract: The aryl hydrocarbon receptor (AHR) is really a ligand-activated signaling molecule expressed in many cell sorts, which includes triple-negative and non-triple-negative breast cancer cells. It affects breast cancer growth and crosstalk with estrogen receptor signaling. Ordinarily, this receptor is degraded shortly after ligand activation by means of the 26S proteasome. Here, we report that AHR undergoes chaperone-mediated autophagy in MDA-MB-468 triple-negative breast cancer cells. This lysosomal degradation of AHR exhibits the following characteristics: (1) it’s triggered by 6 amino-nicotinamide, starvation, and piperazinylpyrimidine compound Q18; (2) it is not observed in non-triple-negative breast cancer cells (MCF-7, T47D, and MDA-MB-361); (3) it could be inhibited by progesterone receptor B but not estrogen receptor alpha; (four) it can be reversed by chloroquine but.