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Isoflavones as Ah Receptor Agonists in Colon-Derived Cell Lines: Structure-Activity Relationships.

Park H, Jin UH, Orr AA, Echegaray SP, Davidson LA, Allred CD, Chapkin R, Jayaraman A, Lee K, Tamamis P, Safe SH.

Chem Res Toxicol. 2019 Oct 17. doi: 10.1021/acs.chemrestox.9b00352. [Epub ahead of print]


Strong adsorption of Polychlorinated Biphenyls by processed montmorillonite clays: Potential applications as toxin enterosorbents during disasters and floods.

Wang M, Safe S, Hearon SE, Phillips TD.

Environ Pollut. 2019 Sep 7;255(Pt 1):113210. doi: 10.1016/j.envpol.2019.113210. [Epub ahead of print]


Inhibition of NR4A1 Promotes Ros Accumulation and IL24-Dependent Growth Arrest in Rhabdomyosarcoma.

Hedrick E, Mohankumar K, Lacey A, Safe S.

Mol Cancer Res. 2019 Aug 28. doi: 10.1158/1541-7786.MCR-19-0408. [Epub ahead of print]


Aryl Hydrocarbon Receptor (AhR) Ligands as Selective AhR Modulators: Genomic Studies.

Safe S, Han H, Goldsby J, Mohankumar K, Chapkin RS.

Curr Opin Toxicol. 2018 Oct-Dec;11-12:10-20. doi: 10.1016/j.cotox.2018.11.005. Epub 2018 Nov 22.


The aryl hydrocarbon receptor is a tumor suppressor-like gene in glioblastoma.

Jin UH, Karki K, Cheng Y, Michelhaugh SK, Mittal S, Safe S.

J Biol Chem. 2019 Jul 19;294(29):11342-11353. doi: 10.1074/jbc.RA119.008882. Epub 2019 Jun 6.


Potent inhibition of breast cancer by bis-indole-derived nuclear receptor 4A1 (NR4A1) antagonists.

Hedrick E, Li X, Cheng Y, Lacey A, Mohankumar K, Zarei M, Safe S.

Breast Cancer Res Treat. 2019 Aug;177(1):29-40. doi: 10.1007/s10549-019-05279-9. Epub 2019 May 22.


Structure-dependent activation of gene expression by bis-indole and quinoline-derived activators of nuclear receptor 4A2.

Li X, Tjalkens RB, Shrestha R, Safe S.

Chem Biol Drug Des. 2019 Oct;94(4):1711-1720. doi: 10.1111/cbdd.13564. Epub 2019 Jul 21. Review.


Nuclear receptor 4A1 (NR4A1) antagonists induce ROS-dependent inhibition of mTOR signaling in endometrial cancer.

Mohankumar K, Li X, Sridharan S, Karki K, Safe S.

Gynecol Oncol. 2019 Jul;154(1):218-227. doi: 10.1016/j.ygyno.2019.04.678. Epub 2019 Apr 30.


Activation of COUP-TFI by a Novel Diindolylmethane Derivative.

Yoon K, Chen CC, Orr AA, Barreto PN, Tamamis P, Safe S.

Cells. 2019 Mar 7;8(3). pii: E220. doi: 10.3390/cells8030220.


Reactive Oxygen Species (ROS)-Inducing Triterpenoid Inhibits Rhabdomyosarcoma Cell and Tumor Growth through Targeting Sp Transcription Factors.

Kasiappan R, Jutooru I, Mohankumar K, Karki K, Lacey A, Safe S.

Mol Cancer Res. 2019 Mar;17(3):794-805. doi: 10.1158/1541-7786.MCR-18-1071. Epub 2019 Jan 4.


Dual targeting of Nur77 and AMPKα by isoalantolactone inhibits adipogenesis in vitro and decreases body fat mass in vivo.

Jung YS, Lee HS, Cho HR, Kim KJ, Kim JH, Safe S, Lee SO.

Int J Obes (Lond). 2019 May;43(5):952-962. doi: 10.1038/s41366-018-0276-x. Epub 2018 Dec 11.


Protective effects of ghrelin on fasting-induced muscle atrophy in aging mice.

Wu CS, Wei Q, Wang H, Kim DM, Balderas M, Wu G, Lawler J, Safe S, Guo S, Devaraj S, Chen Z, Sun Y.

J Gerontol A Biol Sci Med Sci. 2018 Nov 8. doi: 10.1093/gerona/gly256. [Epub ahead of print]


Interleukin-24 (IL24) Is Suppressed by PAX3-FOXO1 and Is a Novel Therapy for Rhabdomyosarcoma.

Lacey A, Hedrick E, Cheng Y, Mohankumar K, Warren M, Safe S.

Mol Cancer Ther. 2018 Dec;17(12):2756-2766. doi: 10.1158/1535-7163.MCT-18-0118. Epub 2018 Sep 6.


Bortezomib Targets Sp Transcription Factors in Cancer Cells.

Karki K, Harishchandra S, Safe S.

Mol Pharmacol. 2018 Oct;94(4):1187-1196. doi: 10.1124/mol.118.112797. Epub 2018 Aug 16.


Compensatory Expression of Nur77 and Nurr1 Regulates NF-κB-Dependent Inflammatory Signaling in Astrocytes.

Popichak KA, Hammond SL, Moreno JA, Afzali MF, Backos DS, Slayden RD, Safe S, Tjalkens RB.

Mol Pharmacol. 2018 Oct;94(4):1174-1186. doi: 10.1124/mol.118.112631. Epub 2018 Aug 15.


TGFβ-Induced Lung Cancer Cell Migration Is NR4A1-Dependent.

Hedrick E, Mohankumar K, Safe S.

Mol Cancer Res. 2018 Dec;16(12):1991-2002. doi: 10.1158/1541-7786.MCR-18-0366. Epub 2018 Aug 2.


A novel diindolylmethane analog, 1,1-bis(3'-indolyl)-1-(p-chlorophenyl) methane, inhibits the tumor necrosis factor-induced inflammatory response in primary murine synovial fibroblasts through a Nurr1-dependent mechanism.

Afzali MF, Popichak KA, Burton LH, Klochak AL, Wilson WJ, Safe S, Tjalkens RB, Legare ME.

Mol Immunol. 2018 Sep;101:46-54. doi: 10.1016/j.molimm.2018.05.024. Epub 2018 Jun 2.


Inhibition of pancreatic cancer Panc1 cell migration by omeprazole is dependent on aryl hydrocarbon receptor activation of JNK.

Jin UH, Karki K, Kim SB, Safe S.

Biochem Biophys Res Commun. 2018 Jun 27;501(3):751-757. doi: 10.1016/j.bbrc.2018.05.061.


Bis-Indole-Derived NR4A1 Ligands and Metformin Exhibit NR4A1-Dependent Glucose Metabolism and Uptake in C2C12 Cells.

Mohankumar K, Lee J, Wu CS, Sun Y, Safe S.

Endocrinology. 2018 May 1;159(5):1950-1963. doi: 10.1210/en.2017-03049.


The Nurr1 Ligand,1,1-bis(3'-Indolyl)-1-(p-Chlorophenyl)Methane, Modulates Glial Reactivity and Is Neuroprotective in MPTP-Induced Parkinsonism.

Hammond SL, Popichak KA, Li X, Hunt LG, Richman EH, Damale PU, Chong EKP, Backos DS, Safe S, Tjalkens RB.

J Pharmacol Exp Ther. 2018 Jun;365(3):636-651. doi: 10.1124/jpet.117.246389. Epub 2018 Apr 6.


Autophagy inhibition improves the chemotherapeutic efficacy of cruciferous vegetable-derived diindolymethane in a murine prostate cancer xenograft model.

Draz H, Goldberg AA, Tomlinson Guns ES, Fazli L, Safe S, Sanderson JT.

Invest New Drugs. 2018 Aug;36(4):718-725. doi: 10.1007/s10637-018-0595-8. Epub 2018 Apr 2.


Structure-Dependent Modulation of Aryl Hydrocarbon Receptor-Mediated Activities by Flavonoids.

Jin UH, Park H, Li X, Davidson LA, Allred C, Patil B, Jayaprakasha G, Orr AA, Mao L, Chapkin RS, Jayaraman A, Tamamis P, Safe S.

Toxicol Sci. 2018 Jul 1;164(1):205-217. doi: 10.1093/toxsci/kfy075.


Specificity Protein Transcription Factors and Cancer: Opportunities for Drug Development.

Safe S, Abbruzzese J, Abdelrahim M, Hedrick E.

Cancer Prev Res (Phila). 2018 Jul;11(7):371-382. doi: 10.1158/1940-6207.CAPR-17-0407. Epub 2018 Mar 15. Review.


Suppression of aberrant choroidal neovascularization through activation of the aryl hydrocarbon receptor.

Choudhary M, Safe S, Malek G.

Biochim Biophys Acta Mol Basis Dis. 2018 May;1864(5 Pt A):1583-1595. doi: 10.1016/j.bbadis.2018.02.015. Epub 2018 Feb 23.


Role of metastasis-associated lung adenocarcinoma transcript-1 (MALAT-1) in pancreatic cancer.

Cheng Y, Imanirad P, Jutooru I, Hedrick E, Jin UH, Rodrigues Hoffman A, Leal de Araujo J, Morpurgo B, Golovko A, Safe S.

PLoS One. 2018 Feb 1;13(2):e0192264. doi: 10.1371/journal.pone.0192264. eCollection 2018.


Metformin-induced anticancer activities: recent insights.

Safe S, Nair V, Karki K.

Biol Chem. 2018 Mar 28;399(4):321-335. doi: 10.1515/hsz-2017-0271. Review.


NR4A1 inhibition synergizes with ibrutinib in killing mantle cell lymphoma cells.

Li Y, Wang F, Lu L, Zhu F, Huang S, Nomie K, Zhang L, Yang DT, Huang W, Kahl BS, Safe S, Wang M, Rui L.

Blood Cancer J. 2017 Nov 23;7(12):632. doi: 10.1038/s41408-017-0005-z. No abstract available.


Carbidopa: a selective Ah receptor modulator (SAhRM).

Safe S.

Biochem J. 2017 Nov 6;474(22):3763-3765. doi: 10.1042/BCJ20170728.


Diindolylmethane and its halogenated derivatives induce protective autophagy in human prostate cancer cells via induction of the oncogenic protein AEG-1 and activation of AMP-activated protein kinase (AMPK).

Draz H, Goldberg AA, Titorenko VI, Tomlinson Guns ES, Safe SH, Sanderson JT.

Cell Signal. 2017 Dec;40:172-182. doi: 10.1016/j.cellsig.2017.09.006. Epub 2017 Sep 18.


Short Chain Fatty Acids Enhance Aryl Hydrocarbon (Ah) Responsiveness in Mouse Colonocytes and Caco-2 Human Colon Cancer Cells.

Jin UH, Cheng Y, Park H, Davidson LA, Callaway ES, Chapkin RS, Jayaraman A, Asante A, Allred C, Weaver EA, Safe S.

Sci Rep. 2017 Aug 31;7(1):10163. doi: 10.1038/s41598-017-10824-x.


Correction for Hedrick et al., "NR4A1 Antagonists Inhibit β1-Integrin-Dependent Breast Cancer Cell Migration".

Hedrick E, Lee SO, Doddapaneni R, Singh M, Safe S.

Mol Cell Biol. 2017 Aug 28;37(18). pii: e00197-17. doi: 10.1128/MCB.00197-17. Print 2017 Sep 15. No abstract available.


Inactivation of the orphan nuclear receptor NR4A1 contributes to apoptosis induction by fangchinoline in pancreatic cancer cells.

Lee HS, Safe S, Lee SO.

Toxicol Appl Pharmacol. 2017 Oct 1;332:32-39. doi: 10.1016/j.taap.2017.07.017. Epub 2017 Jul 25.


Erratum to: Role of the aryl hydrocarbon receptor in carcinogenesis and potential as an anti-cancer drug target.

Kolluri SK, Jin UH, Safe S.

Arch Toxicol. 2017 Sep;91(9):3209. doi: 10.1007/s00204-017-2026-6. No abstract available.


Piperlongumine Induces Reactive Oxygen Species (ROS)-Dependent Downregulation of Specificity Protein Transcription Factors.

Karki K, Hedrick E, Kasiappan R, Jin UH, Safe S.

Cancer Prev Res (Phila). 2017 Aug;10(8):467-477. doi: 10.1158/1940-6207.CAPR-17-0053. Epub 2017 Jul 3.


Role of the aryl hydrocarbon receptor in carcinogenesis and potential as an anti-cancer drug target.

Kolluri SK, Jin UH, Safe S.

Arch Toxicol. 2017 Jul;91(7):2497-2513. doi: 10.1007/s00204-017-1981-2. Epub 2017 May 15. Review. Erratum in: Arch Toxicol. 2017 Sep;91(9):3209.


The Aryl Hydrocarbon Receptor (AhR) as a Drug Target for Cancer Chemotherapy.

Safe S, Cheng Y, Jin UH.

Curr Opin Toxicol. 2017 Feb;2:24-29. doi: 10.1016/j.cotox.2017.01.012. Epub 2017 Feb 1.


The nuclear orphan receptor NR4A1 regulates β1-integrin expression in pancreatic and colon cancer cells and can be targeted by NR4A1 antagonists.

Hedrick E, Lee SO, Safe S.

Mol Carcinog. 2017 Sep;56(9):2066-2075. doi: 10.1002/mc.22662. Epub 2017 May 9.


CF3DODA-Me induces apoptosis, degrades Sp1, and blocks the transformation phase of the blebbishield emergency program.

Taoka R, Jinesh GG, Xue W, Safe S, Kamat AM.

Apoptosis. 2017 May;22(5):719-729. doi: 10.1007/s10495-017-1359-1.


Bardoxolone Methyl and a Related Triterpenoid Downregulate cMyc Expression in Leukemia Cells.

Jin UH, Cheng Y, Zhou B, Safe S.

Mol Pharmacol. 2017 May;91(5):438-450. doi: 10.1124/mol.116.106245. Epub 2017 Mar 8.


Benzyl Isothiocyanate (BITC) Induces Reactive Oxygen Species-dependent Repression of STAT3 Protein by Down-regulation of Specificity Proteins in Pancreatic Cancer.

Kasiappan R, Jutooru I, Karki K, Hedrick E, Safe S.

J Biol Chem. 2016 Dec 30;291(53):27122-27133. doi: 10.1074/jbc.M116.746339. Epub 2016 Nov 15.


PAX3-FOXO1A Expression in Rhabdomyosarcoma Is Driven by the Targetable Nuclear Receptor NR4A1.

Lacey A, Rodrigues-Hoffman A, Safe S.

Cancer Res. 2017 Feb 1;77(3):732-741. doi: 10.1158/0008-5472.CAN-16-1546. Epub 2016 Nov 18.


Editor's Highlight: Microbial-Derived 1,4-Dihydroxy-2-naphthoic Acid and Related Compounds as Aryl Hydrocarbon Receptor Agonists/Antagonists: Structure-Activity Relationships and Receptor Modeling.

Cheng Y, Jin UH, Davidson LA, Chapkin RS, Jayaraman A, Tamamis P, Orr A, Allred C, Denison MS, Soshilov A, Weaver E, Safe S.

Toxicol Sci. 2017 Feb;155(2):458-473. doi: 10.1093/toxsci/kfw230. Epub 2016 Nov 11.


Pharmacological Activators of the NR4A Nuclear Receptors Enhance LTP in a CREB/CBP-Dependent Manner.

Bridi MS, Hawk JD, Chatterjee S, Safe S, Abel T.

Neuropsychopharmacology. 2017 May;42(6):1243-1253. doi: 10.1038/npp.2016.253. Epub 2016 Nov 11.


Penfluridol Represses Integrin Expression in Breast Cancer through Induction of Reactive Oxygen Species and Downregulation of Sp Transcription Factors.

Hedrick E, Li X, Safe S.

Mol Cancer Ther. 2017 Jan;16(1):205-216. doi: 10.1158/1535-7163.MCT-16-0451. Epub 2016 Nov 3.


Natural Products as Mechanism-based Anticancer Agents: Sp Transcription Factors as Targets.

Safe S, Kasiappan R.

Phytother Res. 2016 Nov;30(11):1723-1732. doi: 10.1002/ptr.5669. Epub 2016 Jul 7. Review.


Novel diindolylmethane derivatives based NLC formulations to improve the oral bioavailability and anticancer effects in triple negative breast cancer.

Godugu C, Doddapaneni R, Safe SH, Singh M.

Eur J Pharm Biopharm. 2016 Nov;108:168-179. doi: 10.1016/j.ejpb.2016.08.006. Epub 2016 Aug 30.


Lipid-based oral delivery systems for skin deposition of a potential chemopreventive DIM derivative: characterization and evaluation.

Boakye CH, Patel K, Patel AR, Faria HA, Zucolotto V, Safe S, Singh M.

Drug Deliv Transl Res. 2016 Oct;6(5):526-39. doi: 10.1007/s13346-016-0302-2.


2,3,7,8-Tetrachlorodibenzo-p-dioxin has both pro-carcinogenic and anti-carcinogenic effects on neuroendocrine prostate carcinoma formation in TRAMP mice.

Moore RW, Fritz WA, Schneider AJ, Lin TM, Branam AM, Safe S, Peterson RE.

Toxicol Appl Pharmacol. 2016 Aug 15;305:242-249. doi: 10.1016/j.taap.2016.04.018. Epub 2016 May 3.


Nuclear receptor 4A1 (NR4A1) as a drug target for treating rhabdomyosarcoma (RMS).

Lacey A, Hedrick E, Li X, Patel K, Doddapaneni R, Singh M, Safe S.

Oncotarget. 2016 May 24;7(21):31257-69. doi: 10.18632/oncotarget.9112.

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