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An F876L mutation in androgen receptor confers genetic and phenotypic resistance to MDV3100 (enzalutamide).

Korpal M, Korn JM, Gao X, Rakiec DP, Ruddy DA, Doshi S, Yuan J, Kovats SG, Kim S, Cooke VG, Monahan JE, Stegmeier F, Roberts TM, Sellers WR, Zhou W, Zhu P.

Cancer Discov. 2013 Sep;3(9):1030-43. doi: 10.1158/2159-8290.CD-13-0142.


A clinically relevant androgen receptor mutation confers resistance to second-generation antiandrogens enzalutamide and ARN-509.

Joseph JD, Lu N, Qian J, Sensintaffar J, Shao G, Brigham D, Moon M, Maneval EC, Chen I, Darimont B, Hager JH.

Cancer Discov. 2013 Sep;3(9):1020-9. doi: 10.1158/2159-8290.CD-13-0226.


Resistance emerges to second-generation antiandrogens in prostate cancer.

Nelson WG, Yegnasubramanian S.

Cancer Discov. 2013 Sep;3(9):971-4. doi: 10.1158/2159-8290.CD-13-0405.


A novel antiandrogen, Compound 30, suppresses castration-resistant and MDV3100-resistant prostate cancer growth in vitro and in vivo.

Kuruma H, Matsumoto H, Shiota M, Bishop J, Lamoureux F, Thomas C, Briere D, Los G, Gleave M, Fanjul A, Zoubeidi A.

Mol Cancer Ther. 2013 May;12(5):567-76. doi: 10.1158/1535-7163.MCT-12-0798.


Enzalutamide, an androgen receptor signaling inhibitor, induces tumor regression in a mouse model of castration-resistant prostate cancer.

Guerrero J, Alfaro IE, Gómez F, Protter AA, Bernales S.

Prostate. 2013 Sep;73(12):1291-305. doi: 10.1002/pros.22674.


Niclosamide inhibits androgen receptor variants expression and overcomes enzalutamide resistance in castration-resistant prostate cancer.

Liu C, Lou W, Zhu Y, Nadiminty N, Schwartz CT, Evans CP, Gao AC.

Clin Cancer Res. 2014 Jun 15;20(12):3198-210. doi: 10.1158/1078-0432.CCR-13-3296.


PMA induces androgen receptor downregulation and cellular apoptosis in prostate cancer cells.

Itsumi M, Shiota M, Yokomizo A, Takeuchi A, Kashiwagi E, Dejima T, Inokuchi J, Tatsugami K, Uchiumi T, Naito S.

J Mol Endocrinol. 2014 Aug;53(1):31-41. doi: 10.1530/JME-13-0303.


Enzalutamide as a second generation antiandrogen for treatment of advanced prostate cancer.

Semenas J, Dizeyi N, Persson JL.

Drug Des Devel Ther. 2013 Aug 27;7:875-81. doi: 10.2147/DDDT.S45703. Review.


Inhibition of RSK/YB-1 signaling enhances the anti-cancer effect of enzalutamide in prostate cancer.

Shiota M, Yokomizo A, Takeuchi A, Itsumi M, Imada K, Kashiwagi E, Inokuchi J, Tatsugami K, Uchiumi T, Naito S.

Prostate. 2014 Jun;74(9):959-69. doi: 10.1002/pros.22813.


Cotargeting Androgen Receptor and Clusterin Delays Castrate-Resistant Prostate Cancer Progression by Inhibiting Adaptive Stress Response and AR Stability.

Matsumoto H, Yamamoto Y, Shiota M, Kuruma H, Beraldi E, Matsuyama H, Zoubeidi A, Gleave M.

Cancer Res. 2013 Aug 15;73(16):5206-17. doi: 10.1158/0008-5472.CAN-13-0359.


Small-Molecule-Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging.

Gustafson JL, Neklesa TK, Cox CS, Roth AG, Buckley DL, Tae HS, Sundberg TB, Stagg DB, Hines J, McDonnell DP, Norris JD, Crews CM.

Angew Chem Int Ed Engl. 2015 Aug 10;54(33):9659-62. doi: 10.1002/anie.201503720.


Enzalutamide (Xtandi) for patients with metastatic, resistant prostate cancer.

Bennett LL, Ingason A.

Ann Pharmacother. 2014 Apr;48(4):530-7. doi: 10.1177/1060028013518899. Review.


Characterization of a new class of androgen receptor antagonists with potential therapeutic application in advanced prostate cancer.

Li H, Hassona MD, Lack NA, Axerio-Cilies P, Leblanc E, Tavassoli P, Kanaan N, Frewin K, Singh K, Adomat H, Böhm KJ, Prinz H, Guns ET, Rennie PS, Cherkasov A.

Mol Cancer Ther. 2013 Nov;12(11):2425-35. doi: 10.1158/1535-7163.MCT-13-0267.


Methylselenol prodrug enhances MDV3100 efficacy for treatment of castration-resistant prostate cancer.

Zhan Y, Cao B, Qi Y, Liu S, Zhang Q, Zhou W, Xu D, Lu H, Sartor O, Kong W, Zhang H, Dong Y.

Int J Cancer. 2013 Nov;133(9):2225-33. doi: 10.1002/ijc.28202.


Cross-resistance between taxanes and new hormonal agents abiraterone and enzalutamide may affect drug sequence choices in metastatic castration-resistant prostate cancer.

van Soest RJ, van Royen ME, de Morrée ES, Moll JM, Teubel W, Wiemer EA, Mathijssen RH, de Wit R, van Weerden WM.

Eur J Cancer. 2013 Dec;49(18):3821-30. doi: 10.1016/j.ejca.2013.09.026.


Mechanisms of drug resistance that target the androgen axis in castration resistant prostate cancer (CRPC).

Penning TM.

J Steroid Biochem Mol Biol. 2015 Sep;153:105-13. doi: 10.1016/j.jsbmb.2015.05.010. Review.


Androgen receptor splice variants mediate enzalutamide resistance in castration-resistant prostate cancer cell lines.

Li Y, Chan SC, Brand LJ, Hwang TH, Silverstein KA, Dehm SM.

Cancer Res. 2013 Jan 15;73(2):483-9. doi: 10.1158/0008-5472.CAN-12-3630.


Enzalutamide: targeting the androgen signalling pathway in metastatic castration-resistant prostate cancer.

Schalken J, Fitzpatrick JM.

BJU Int. 2016 Feb;117(2):215-25. doi: 10.1111/bju.13123. Review.


Metastatic castration-resistant prostate cancer: targeting the mechanisms of resistance to abiraterone acetate and enzalutamide.

Modena A, Ciccarese C, Fantinel E, Bimbatti D, Tortora G, Massari F.

Expert Rev Anticancer Ther. 2015;15(9):1037-48. doi: 10.1586/14737140.2015.1063423. Review.

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