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Direct regulation of androgen receptor activity by potent CYP17 inhibitors in prostate cancer cells.

Soifer HS, Souleimanian N, Wu S, Voskresenskiy AM, Collak FK, Cinar B, Stein CA.

J Biol Chem. 2012 Feb 3;287(6):3777-87. doi: 10.1074/jbc.M111.261933. Epub 2011 Dec 15.


Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.

Handratta VD, Vasaitis TS, Njar VC, Gediya LK, Kataria R, Chopra P, Newman D Jr, Farquhar R, Guo Z, Qiu Y, Brodie AM.

J Med Chem. 2005 Apr 21;48(8):2972-84.


Antiandrogenic effects of novel androgen synthesis inhibitors on hormone-dependent prostate cancer.

Long BJ, Grigoryev DN, Nnane IP, Liu Y, Ling YZ, Brodie AM.

Cancer Res. 2000 Dec 1;60(23):6630-40.


Resistance to CYP17A1 inhibition with abiraterone in castration-resistant prostate cancer: induction of steroidogenesis and androgen receptor splice variants.

Mostaghel EA, Marck BT, Plymate SR, Vessella RL, Balk S, Matsumoto AM, Nelson PS, Montgomery RB.

Clin Cancer Res. 2011 Sep 15;17(18):5913-25. doi: 10.1158/1078-0432.CCR-11-0728. Epub 2011 Aug 1.


Modeling androgen receptor flexibility: a binding mode hypothesis of CYP17 inhibitors/antiandrogens for prostate cancer therapy.

Gianti E, Zauhar RJ.

J Chem Inf Model. 2012 Oct 22;52(10):2670-83. doi: 10.1021/ci3002342. Epub 2012 Oct 1.


Amino acid containing thapsigargin analogues deplete androgen receptor protein via synthesis inhibition and induce the death of prostate cancer cells.

Vander Griend DJ, Antony L, Dalrymple SL, Xu Y, Christensen SB, Denmeade SR, Isaacs JT.

Mol Cancer Ther. 2009 May;8(5):1340-9. doi: 10.1158/1535-7163.MCT-08-1136. Epub 2009 May 5.


Androgen receptor inactivation contributes to antitumor efficacy of 17{alpha}-hydroxylase/17,20-lyase inhibitor 3beta-hydroxy-17-(1H-benzimidazole-1-yl)androsta-5,16-diene in prostate cancer.

Vasaitis T, Belosay A, Schayowitz A, Khandelwal A, Chopra P, Gediya LK, Guo Z, Fang HB, Njar VC, Brodie AM.

Mol Cancer Ther. 2008 Aug;7(8):2348-57. doi: 10.1158/1535-7163.MCT-08-0230.


Intratumoral de novo steroid synthesis activates androgen receptor in castration-resistant prostate cancer and is upregulated by treatment with CYP17A1 inhibitors.

Cai C, Chen S, Ng P, Bubley GJ, Nelson PS, Mostaghel EA, Marck B, Matsumoto AM, Simon NI, Wang H, Chen S, Balk SP.

Cancer Res. 2011 Oct 15;71(20):6503-13. doi: 10.1158/0008-5472.CAN-11-0532. Epub 2011 Aug 25.


Androgens up-regulate the insulin-like growth factor-I receptor in prostate cancer cells.

Pandini G, Mineo R, Frasca F, Roberts CT Jr, Marcelli M, Vigneri R, Belfiore A.

Cancer Res. 2005 Mar 1;65(5):1849-57.


Androgen receptor W741C and T877A mutations in AIDL cells, an androgen-independent subline of prostate cancer LNCaP cells.

Otsuka T, Iguchi K, Fukami K, Ishii K, Usui S, Sugimura Y, Hirano K.

Tumour Biol. 2011 Dec;32(6):1097-102. doi: 10.1007/s13277-011-0209-y. Epub 2011 Jul 20.


Androgen synthesis inhibitors in the treatment of castration-resistant prostate cancer.

Stein MN, Patel N, Bershadskiy A, Sokoloff A, Singer EA.

Asian J Androl. 2014 May-Jun;16(3):387-400. doi: 10.4103/1008-682X.129133. Review.


Interactions of abiraterone, eplerenone, and prednisolone with wild-type and mutant androgen receptor: a rationale for increasing abiraterone exposure or combining with MDV3100.

Richards J, Lim AC, Hay CW, Taylor AE, Wingate A, Nowakowska K, Pezaro C, Carreira S, Goodall J, Arlt W, McEwan IJ, de Bono JS, Attard G.

Cancer Res. 2012 May 1;72(9):2176-82. doi: 10.1158/0008-5472.CAN-11-3980. Epub 2012 Mar 12.


Changes in androgen receptor nongenotropic signaling correlate with transition of LNCaP cells to androgen independence.

Unni E, Sun S, Nan B, McPhaul MJ, Cheskis B, Mancini MA, Marcelli M.

Cancer Res. 2004 Oct 1;64(19):7156-68.


Differential effects of genistein on prostate cancer cells depend on mutational status of the androgen receptor.

Mahmoud AM, Zhu T, Parray A, Siddique HR, Yang W, Saleem M, Bosland MC.

PLoS One. 2013 Oct 22;8(10):e78479. doi: 10.1371/journal.pone.0078479. eCollection 2013.


Synthesis and biological evaluations of putative metabolically stable analogs of VN/124-1 (TOK-001): head to head anti-tumor efficacy evaluation of VN/124-1 (TOK-001) and abiraterone in LAPC-4 human prostate cancer xenograft model.

Bruno RD, Vasaitis TS, Gediya LK, Purushottamachar P, Godbole AM, Ates-Alagoz Z, Brodie AM, Njar VC.

Steroids. 2011 Nov;76(12):1268-79. doi: 10.1016/j.steroids.2011.06.002. Epub 2011 Jun 24.


Hedgehog/Gli supports androgen signaling in androgen deprived and androgen independent prostate cancer cells.

Chen M, Feuerstein MA, Levina E, Baghel PS, Carkner RD, Tanner MJ, Shtutman M, Vacherot F, Terry S, de la Taille A, Buttyan R.

Mol Cancer. 2010 Apr 26;9:89. doi: 10.1186/1476-4598-9-89.


Abiraterone acetate: oral androgen biosynthesis inhibitor for treatment of castration-resistant prostate cancer.

Rehman Y, Rosenberg JE.

Drug Des Devel Ther. 2012;6:13-8. doi: 10.2147/DDDT.S15850. Epub 2012 Jan 16. Review.


Transcriptional regulation of the androgen signaling pathway by the Wilms' tumor suppressor gene WT1.

Zaia A, Fraizer GC, Piantanelli L, Saunders GF.

Anticancer Res. 2001 Jan-Feb;21(1A):1-10.

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