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Galiellalactone is a direct inhibitor of the transcription factor STAT3 in prostate cancer cells.

Don-Doncow N, Escobar Z, Johansson M, Kjellström S, Garcia V, Munoz E, Sterner O, Bjartell A, Hellsten R.

J Biol Chem. 2014 Jun 6;289(23):15969-78. doi: 10.1074/jbc.M114.564252. Epub 2014 Apr 22.


The STAT3 Inhibitor Galiellalactone Effectively Reduces Tumor Growth and Metastatic Spread in an Orthotopic Xenograft Mouse Model of Prostate Cancer.

Canesin G, Evans-Axelsson S, Hellsten R, Sterner O, Krzyzanowska A, Andersson T, Bjartell A.

Eur Urol. 2016 Mar;69(3):400-4. doi: 10.1016/j.eururo.2015.06.016. Epub 2015 Jul 2.


Galiellalactone is a novel therapeutic candidate against hormone-refractory prostate cancer expressing activated Stat3.

Hellsten R, Johansson M, Dahlman A, Dizeyi N, Sterner O, Bjartell A.

Prostate. 2008 Feb 15;68(3):269-80. doi: 10.1002/pros.20699.


Galiellalactone inhibits stem cell-like ALDH-positive prostate cancer cells.

Hellsten R, Johansson M, Dahlman A, Sterner O, Bjartell A.

PLoS One. 2011;6(7):e22118. doi: 10.1371/journal.pone.0022118. Epub 2011 Jul 11.


Galiellalactone induces cell cycle arrest and apoptosis through the ATM/ATR pathway in prostate cancer cells.

García V, Lara-Chica M, Cantarero I, Sterner O, Calzado MA, Muñoz E.

Oncotarget. 2016 Jan 26;7(4):4490-506. doi: 10.18632/oncotarget.6606.


Identification of galiellalactone-based novel STAT3-selective inhibitors with cytotoxic activities against triple-negative breast cancer cell lines.

Kim HS, Kim T, Ko H, Lee J, Kim YS, Suh YG.

Bioorg Med Chem. 2017 Oct 1;25(19):5032-5040. doi: 10.1016/j.bmc.2017.06.036. Epub 2017 Jun 23.


Cryptotanshinone inhibits constitutive signal transducer and activator of transcription 3 function through blocking the dimerization in DU145 prostate cancer cells.

Shin DS, Kim HN, Shin KD, Yoon YJ, Kim SJ, Han DC, Kwon BM.

Cancer Res. 2009 Jan 1;69(1):193-202. doi: 10.1158/0008-5472.CAN-08-2575.


Penta-1,2,3,4,6-O-galloyl-beta-D-glucose induces p53 and inhibits STAT3 in prostate cancer cells in vitro and suppresses prostate xenograft tumor growth in vivo.

Hu H, Lee HJ, Jiang C, Zhang J, Wang L, Zhao Y, Xiang Q, Lee EO, Kim SH, Lü J.

Mol Cancer Ther. 2008 Sep;7(9):2681-91. doi: 10.1158/1535-7163.MCT-08-0456. Erratum in: Mol Cancer Ther. 2008 Nov;7(11):3654.


Inhibition of STAT3 signaling targets both tumor-initiating and differentiated cell populations in prostate cancer.

Han Z, Wang X, Ma L, Chen L, Xiao M, Huang L, Cao Y, Bai J, Ma D, Zhou J, Hong Z.

Oncotarget. 2014 Sep 30;5(18):8416-28.


Preclinical Characterization of 3β-(N-Acetyl l-cysteine methyl ester)-2aβ,3-dihydrogaliellalactone (GPA512), a Prodrug of a Direct STAT3 Inhibitor for the Treatment of Prostate Cancer.

Escobar Z, Bjartell A, Canesin G, Evans-Axelsson S, Sterner O, Hellsten R, Johansson MH.

J Med Chem. 2016 May 26;59(10):4551-62. doi: 10.1021/acs.jmedchem.5b01814. Epub 2016 May 3.


Scoparone exerts anti-tumor activity against DU145 prostate cancer cells via inhibition of STAT3 activity.

Kim JK, Kim JY, Kim HJ, Park KG, Harris RA, Cho WJ, Lee JT, Lee IK.

PLoS One. 2013 Nov 15;8(11):e80391. doi: 10.1371/journal.pone.0080391. eCollection 2013.


Ginkgetin inhibits the growth of DU-145 prostate cancer cells through inhibition of signal transducer and activator of transcription 3 activity.

Jeon YJ, Jung SN, Yun J, Lee CW, Choi J, Lee YJ, Han DC, Kwon BM.

Cancer Sci. 2015 Apr;106(4):413-20. doi: 10.1111/cas.12608. Epub 2015 Feb 20.


Inhibition of constitutively active Stat3 reverses enzalutamide resistance in LNCaP derivative prostate cancer cells.

Liu C, Zhu Y, Lou W, Cui Y, Evans CP, Gao AC.

Prostate. 2014 Feb;74(2):201-9. doi: 10.1002/pros.22741. Epub 2013 Oct 16.


Silibinin inhibits constitutive activation of Stat3, and causes caspase activation and apoptotic death of human prostate carcinoma DU145 cells.

Agarwal C, Tyagi A, Kaur M, Agarwal R.

Carcinogenesis. 2007 Jul;28(7):1463-70. Epub 2007 Mar 6.


Inhibition of Stat3 activation by sanguinarine suppresses prostate cancer cell growth and invasion.

Sun M, Liu C, Nadiminty N, Lou W, Zhu Y, Yang J, Evans CP, Zhou Q, Gao AC.

Prostate. 2012 Jan;72(1):82-9. doi: 10.1002/pros.21409. Epub 2011 May 2.


The fungal metabolite galiellalactone interferes with the nuclear import of NF-κB and inhibits HIV-1 replication.

Pérez M, Soler-Torronteras R, Collado JA, Limones CG, Hellsten R, Johansson M, Sterner O, Bjartell A, Calzado MA, Muñoz E.

Chem Biol Interact. 2014 May 5;214:69-76. doi: 10.1016/j.cbi.2014.02.012. Epub 2014 Mar 11.


A cell-permeable Stat3 SH2 domain mimetic inhibits Stat3 activation and induces antitumor cell effects in vitro.

Zhao W, Jaganathan S, Turkson J.

J Biol Chem. 2010 Nov 12;285(46):35855-65. doi: 10.1074/jbc.M110.154088. Epub 2010 Aug 31.


Mild oxidative stress induces S-glutathionylation of STAT3 and enhances chemosensitivity of tumoural cells to chemotherapeutic drugs.

Butturini E, Carcereri de Prati A, Chiavegato G, Rigo A, Cavalieri E, Darra E, Mariotto S.

Free Radic Biol Med. 2013 Dec;65:1322-30. doi: 10.1016/j.freeradbiomed.2013.09.015. Epub 2013 Oct 1.


Diallyl trisulfide inhibits activation of signal transducer and activator of transcription 3 in prostate cancer cells in culture and in vivo.

Chandra-Kuntal K, Singh SV.

Cancer Prev Res (Phila). 2010 Nov;3(11):1473-83. doi: 10.1158/1940-6207.CAPR-10-0123. Epub 2010 Oct 19.

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