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Development of a second-generation antiandrogen for treatment of advanced prostate cancer.
Open accessAbstract
Metastatic prostate cancer is treated with drugs that antagonize androgen action, but most patients progress to a more aggressive form of the disease called castration-resistant prostate cancer, driven by elevated expression of the androgen receptor. Here we characterize the diarylthiohydantoins RD162 and MDV3100, two compounds optimized from a screen for nonsteroidal antiandrogens that retain activity in the setting of increased androgen receptor expression. Both compounds bind to the androgen receptor with greater relative affinity than the clinically used antiandrogen bicalutamide, reduce the efficiency of its nuclear translocation, and impair both DNA binding to androgen response elements and recruitment of coactivators. RD162 and MDV3100 are orally available and induce tumor regression in mouse models of castration-resistant human prostate cancer. Of the first 30 patients treated with MDV3100 in a Phase I/II clinical trial, 13 of 30 (43%) showed sustained declines (by >50%) in serum concentrations of prostate-specific antigen, a biomarker of prostate cancer. These compounds thus appear to be promising candidates for treatment of advanced prostate cancer.
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“The ability of these molecules to inhibit AR transcriptional activity and demonstrate clinical efficacy in a phase I/II trial of patients with CR tumors, in the case of MDV 3100, suggests that ligand-directed therapeutics might still have a place in future treatment regimes.”
From Minireview: Alternative Activation Pathways for the Androgen Receptor in Prostate Cancer (2011) · cites this paper as [81]
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“The ability of these molecules to inhibit AR transcriptional activity and demonstrate clinical efficacy in a phase I/II trial of patients with CR tumors, in the case of MDV 3100, suggests that ligand-directed therapeutics might still have a place in future treatment regimes.”
From Minireview: Alternative Activation Pathways for the Androgen Receptor in Prostate Cancer (2011) · cites this paper as [81]
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“EPI-001 targets the NTD of the AR (80), whereas MDV 3100 binds to the LBD (81), similarly to bicalutamide.”
From Minireview: Alternative Activation Pathways for the Androgen Receptor in Prostate Cancer (2011) · cites this paper as [81]
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“The ARE repeat reporter (4X-ARE, firefly luciferase) has been previously described (Tran et al., 2009).”
From Allosteric interactions prime androgen receptor dimerization and activation (2022) · cites this paper as Tran et al., 2009
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Shiau, A. K., Barstad, D., Loria, P. M., Cheng, L., Kushner, P. J., Agard, D. A., & Greene, G. L. (1998) · Cell · doi:10.1016/s0092-8674(00)81717-1 · Cited by 2,759
Molecular determinants of resistance to antiandrogen therapy
Chen, C. D., Welsbie, D. S., Tran, C., Baek, S. H., Chen, R., Vessella, R., Rosenfeld, M. G., & Sawyers, C. L. (2004) · Nature Medicine · doi:10.1038/nm972 · Cited by 2,278
Self-citationScher, H. I., & Sawyers, C. L. (2005) · Journal of Clinical Oncology · doi:10.1200/jco.2005.03.4777 · Cited by 1,025
Self-citationStructural basis for antagonism and resistance of bicalutamide in prostate cancer
Bohl, C. E., Gao, W., Miller, D. D., Bell, C. E., & Dalton, J. T. (2005) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0500381102 · Cited by 426
Androgen receptor: A key molecule in the progression of prostate cancer to hormone independence
Taplin, M., & Balk, S. P. (2003) · Journal of Cellular Biochemistry · doi:10.1002/jcb.10653 · Cited by 392
Larson, S. M., Morris, M. J., Guenther, I., Beattie, B., Humm, J. L., Akhurst, T., Finn, R. D., Erdi, Y. E., Pentlow, K. S., Dyke, J., et al. (2004) · PubMed · Cited by 298
Self-citationMasiello, D., Cheng, S., Bubley, G. J., Lu, M. L., & Balk, S. P. (2002) · Journal of Biological Chemistry · doi:10.1074/jbc.m203310200 · Cited by 240
Yoshida, T., Kinoshita, H., Segawa, T., Nakamura, E., Inoue, T., Shimizu, Y., Kamoto, T., & Ogawa, O. (2005) · Cancer Research · doi:10.1158/0008-5472.can-05-0817 · Cited by 178
Hodgson, M. C., Astapova, I. I., Cheng, S., Lee, L. J., Verhoeven, M. C., Choi, E., Balk, S. P., & Hollenberg, A. N. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m408972200 · Cited by 143
Homozygous Deletions and Recurrent Amplifications Implicate New Genes Involved in Prostate Cancer
Liu, W., Xie, C., Zhu, Y., Li, T., Sun, J., Cheng, Y., Ewing, C. M., Dalrymple, S. L., Turner, A. R., Sun, J., et al. (2008) · Neoplasia · doi:10.1593/neo.08428 · Cited by 128
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Items 201–300 of 1,000
Hoang, D. T., Iczkowski, K. A., Kilari, D., See, W. A., & Nevalainen, M. T. (2016) · Oncotarget · doi:10.18632/oncotarget.12554 · Cited by 132
Androgen control of lipid metabolism in prostate cancer: novel insights and future applications
Butler, L. M., Centenera, M. M., & Swinnen, J. V. (2016) · Endocrine Related Cancer · doi:10.1530/erc-15-0556 · Cited by 127
Molecular Switch in the Glucocorticoid Receptor: Active and Passive Antagonist Conformations
Schoch, G., D’Arcy, B., Stihle, M., Burger, D., Bär, D., Benz, J., Thoma, R., & Ruf, A. (2009) · Journal of Molecular Biology · doi:10.1016/j.jmb.2009.11.011 · Cited by 127
Yamamoto, Y., Loriot, Y., Beraldi, E., Zhang, F., Wyatt, A. W., Nakouzi, N. A., Mo, F., Zhou, T., Kim, Y., Monia, B. P., et al. (2015) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-14-1108 · Cited by 129
Gardner, T. A., Elzey, B. D., & Hahn, N. M. (2012) · Human Vaccines & Immunotherapeutics · doi:10.4161/hv.19795 · Cited by 133
miR 488* inhibits androgen receptor expression in prostate carcinoma cells
Sikand, K., Slaibi, J. E., Singh, R., Slane, S. D., & Shukla, G. C. (2010) · International Journal of Cancer · doi:10.1002/ijc.25753 · Cited by 127
Castration-Resistant Prostate Cancer: AUA Guideline Amendment 2018
Lowrance, W. T., Murad, M. H., Oh, W. K., Jarrard, D. F., Resnick, M. J., & Cookson, M. S. (2018) · The Journal of Urology · doi:10.1016/j.juro.2018.07.090 · Cited by 124
James, N. D., Sydes, M. R., Mason, M. D., Clarke, N. W., Anderson, J., Dearnaley, D. P., Dwyer, J., Jovic, G., Ritchie, A. W., Russell, J. M., et al. (2012) · The Lancet Oncology · doi:10.1016/s1470-2045(12)70088-8 · Cited by 123
Novel therapies are changing treatment paradigms in metastatic prostate cancer
Powers, E., Karachaliou, G. S., Kao, C., Harrison, M. R., Hoimes, C. J., George, D. J., Armstrong, A. J., & Zhang, T. (2020) · Journal of Hematology & Oncology · doi:10.1186/s13045-020-00978-z · Cited by 128
Li, J., Alyamani, M., Zhang, A., Chang, K., Berk, M. P., Li, Z., Zhu, Z., Petro, M., Magi‐Galluzzi, C., Taplin, M., et al. (2017) · eLife · doi:10.7554/elife.20183 · Cited by 127
Androgen Receptor Promotes Ligand-Independent Prostate Cancer Progression through c-Myc Upregulation
Gao, L., Schwartzman, J. A., Gibbs, A., Lisac, R., Kleinschmidt, R., Wilmot, B., Bottomly, D., Coleman, I. M., Nelson, P. S., McWeeney, S. K., et al. (2013) · PLoS ONE · doi:10.1371/journal.pone.0063563 · Cited by 124
Recommandations en Onco-Urologie 2010 : Cancer de la prostate
Salomon, L., Azria, D., Bastide, C., Beuzeboc, P., Cormier, L., Cornud, F., Eiss, D., Eschwège, P., Gaschignard, N., Hennequin, C., et al. (2010) · The French Journal of Urology · doi:10.1016/s1166-7087(10)70042-7 · Cited by 121
The Role of the Androgen Receptor in Triple-Negative Breast Cancer
Shah, P. D., Gucalp, A., & Traina, T. A. (2013) · Women s Health · doi:10.2217/whe.13.33 · Cited by 121
Drug safety is a barrier to the discovery and development of new androgen receptor antagonists
Foster, W. R., Car, B. D., Shi, H., Lévesque, P., Obermeier, M. T., Gan, J., Arezzo, J. C., Powlin, S. S., Dinchuk, J. E., Balog, A., et al. (2010) · The Prostate · doi:10.1002/pros.21263 · Cited by 120
Therapeutic targeting of the prostate cancer microenvironment
Κάρλου, Μ., Tzelepi, V., & Efstathiou, E. (2010) · Nature Reviews Urology · doi:10.1038/nrurol.2010.134 · Cited by 122
Bono, J. S. D., Chowdhury, S., Feyerabend, S., Elliott, T., Grande, E., Melhem‐Bertrandt, A., Baron, B., Hirmand, M., Werbrouck, P., & Fizazi, K. S. (2017) · European Urology · doi:10.1016/j.eururo.2017.07.035 · Cited by 120
Rahim, B. G., & O'Regan, R. M. (2017) · Cancers · doi:10.3390/cancers9030021 · Cited by 122
Moses, M. A., Kim, Y. S., Rivera-Márquez, G. M., Oshima, N., Watson, M. J., Beebe, K. E., Wells, C., Lee, S., Zuehlke, A. D., Shao, H., et al. (2018) · Cancer Research · doi:10.1158/0008-5472.can-17-3728 · Cited by 119
Androgen Receptor Splice Variants in the Era of Enzalutamide and Abiraterone
Nakazawa, M., Antonarakis, E. S., & Luo, J. (2014) · Hormones and Cancer · doi:10.1007/s12672-014-0190-1 · Cited by 122
Brasso, K., Thomsen, F. B., Schrader, A. J., Schmid, S. C., Lorente, D., Retz, M. M., Merseburger, A. S., von Klot, C. A., Boegemann, M., & Bono, J. S. D. (2014) · European Urology · doi:10.1016/j.eururo.2014.07.028 · Cited by 120
Denmeade, S. R., & Isaacs, J. T. (2010) · The Prostate · doi:10.1002/pros.21196 · Cited by 116
CDK7 Inhibition Suppresses Castration-Resistant Prostate Cancer through MED1 Inactivation
Rasool, R. U., Natesan, R., Deng, Q., Aras, S., Lal, P., Effron, S. S., Mitchell-Velasquez, E., Posimo, J. M., Carskadon, S. L., Baca, S. C., et al. (2019) · Cancer Discovery · doi:10.1158/2159-8290.cd-19-0189 · Cited by 118
Revisiting the role of Wnt/β-catenin signaling in prostate cancer
Schneider, J. A., & Logan, S. K. (2017) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2017.02.008 · Cited by 115
Guerrero, J., Alfaro, I. E., Gómez, F. J., Protter, A. A., & Bernales, S. (2013) · The Prostate · doi:10.1002/pros.22674 · Cited by 120
Androgen receptor and its splice variants in prostate cancer
Haile, S., & Sadar, M. D. (2011) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-011-0766-7 · Cited by 118
Liu, Q., Tong, D., Liu, G., Xu, J., Do, K., Geary, K. R., Zhang, D., Zhang, J., Zhang, Y., Li, Y., et al. (2017) · Cell Death and Disease · doi:10.1038/cddis.2017.417 · Cited by 113
Wang, Y., Chen, J., Wu, Z., Ding, W., Gao, S., Gao, Y., & Xu, C. (2020) · British Journal of Pharmacology · doi:10.1111/bph.15300 · Cited by 117
Adeniji, A. O., Twenter, B. M., Byrns, M. C., Jin, Y., Chen, M., Winkler, J. D., & Penning, T. M. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm201547v · Cited by 113
Overcoming Drug Resistance and Treating Advanced Prostate Cancer
Semenas, J., Allegrucci, C., Boorjian, S. A., Mongan, N. P., & Persson, J. L. (2012) · Current Drug Targets · doi:10.2174/138945012802429615 · Cited by 115
Molina, A., & Belldegrun, A. (2011) · Journal of Urology · doi:10.1016/j.juro.2010.10.042 · Cited by 112
Therapeutic Approaches Targeting MYC-Driven Prostate Cancer
Rebello, R. J., Pearson, R. B., Hannan, R. D., & Furic, L. (2017) · Genes · doi:10.3390/genes8020071 · Cited by 110
The Role of Genetic Markers in the Management of Prostate Cancer
Choudhury, A. D., Eeles, R. A., Freedland, S. J., Isaacs, W. B., Pomerantz, M. M., Schalken, J. A., Tammela, T. L. J., & Visakorpi, T. (2012) · European Urology · doi:10.1016/j.eururo.2012.05.054 · Cited by 107
Benoist, G. E., Hendriks, R. J., Mulders, P., Gerritsen, W. R., Somford, D. M., Schalken, J. A., van Oort, I. M., Burger, D. M., & van Erp, N. P. (2016) · Clinical Pharmacokinetics · doi:10.1007/s40262-016-0403-6 · Cited by 107
Qu, F., Xie, W., Nakabayashi, M., Zhang, H., Jeong, S. H., Wang, X., Komura, K., Sweeney, C. J., Sartor, O. A., Lee, G. M., et al. (2016) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-16-1070 · Cited by 108
Neuwirt, H., Bouchal, J., Kharaishvili, G., Ploner, C., Jöhrer, K., Pitterl, F., Weber, A., Klocker, H., & Eder, I. E. (2020) · Cell Communication and Signaling · doi:10.1186/s12964-019-0505-5 · Cited by 106
Zhang, F., Biswas, M., Massah, S., Lee, J., Lingadahalli, S., Wong, S. T. S., Wells, C. A., Foo, J., Khan, N., Morin, H., et al. (2022) · Nucleic Acids Research · doi:10.1093/nar/gkac1158 · Cited by 108
Decker, K. F., Zheng, D., He, Y., Bowman, T. A., Edwards, J. R., & Li, J. (2012) · Nucleic Acids Research · doi:10.1093/nar/gks888 · Cited by 106
Purushottamachar, P., Godbole, A. M., Gediya, L. K., Martin, M. S., Vasaitis, T. S., Kwegyir‐Afful, A. K., Ramalingam, S., Ateş‐Alagöz, Z., & Njar, V. C. O. (2013) · Journal of Medicinal Chemistry · doi:10.1021/jm400048v · Cited by 105
Zhu, Y., Dalrymple, S. L., Coleman, I. M., Zheng, S. L., Xu, J., Hooper, J. E., Antonarakis, E. S., Marzo, A. M. D., Meeker, A. K., Nelson, P. S., et al. (2020) · Oncogene · doi:10.1038/s41388-020-01479-6 · Cited by 107
Kuruma, H., Matsumoto, H., Shiota, M., Bishop, J. L., Lamoureux, F., Thomas, C., Briere, D. M., Los, G., Gleave, M. E., Fanjul, A. N., et al. (2013) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-12-0798 · Cited by 105
Androgen receptor-mediated non-genomic regulation of prostate cancer cell proliferation.
Liao, R. S., Ma, S., Lu, M., Li, R., Yin, Y., & Raj, G. V. (2013) · PubMed Central · doi:10.3978/j.issn.2223-4683.2013.09.07 · Cited by 103
Inhibition of androgen receptor and β-catenin activity in prostate cancer
Lee, E., Madar, A., David, G., Garabedian, M. J., DasGupta, R., & Logan, S. K. (2013) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1218168110 · Cited by 103
The 2014 CUA-CUOG Guidelines for the Management of Castration Resistant Prostate Cancer (CRPC)
Fred Saad, C., Chi, K., Finelli, A., Hotte, S. J., Izawa, J. I., Kapoor, A., Kassouf, W., Loblaw, A., North, S. A., Rendon, R. A., et al. (2015) · Canadian Urological Association Journal · doi:10.5489/cuaj.2526 · Cited by 102
Abou, D. S., Ulmert, D., Doucet, M., Hobbs, R. F., Riddle, R. C., & Thorek, D. L. J. (2015) · JNCI Journal of the National Cancer Institute · doi:10.1093/jnci/djv380 · Cited by 102
Murga, J. D., Moorji, S. M., Han, A. Q., Magargal, W. W., DiPippo, V. A., & Olson, W. C. (2014) · The Prostate · doi:10.1002/pros.22910 · Cited by 102
Xie, N., Cheng, H., Lin, D., Liu, L., Ou, Y., Li, J., Fazli, L., Gleave, M. E., Wang, Y. Z., Rennie, P. S., et al. (2014) · International Journal of Cancer · doi:10.1002/ijc.29147 · Cited by 101
Nanoways to overcome docetaxel resistance in prostate cancer
Ganju, A., Yallapu, M. M., Khan, S., Behrman, S. W., Chauhan, S. C., & Jaggi, M. (2014) · Drug Resistance Updates · doi:10.1016/j.drup.2014.04.001 · Cited by 101
Targeting the Androgen Receptor in Breast Cancer
Chia, K., O’Brien, M., Brown, M. A., & Lim, E. (2015) · Current Oncology Reports · doi:10.1007/s11912-014-0427-8 · Cited by 103
Liu, C., Zhu, Y., Lou, W., Cui, Y., Evans, C. P., & Gao, A. C. (2013) · The Prostate · doi:10.1002/pros.22741 · Cited by 101
Jin, R., Yamashita, H., Yu, X., Wang, J., Franco, O. E., Wang, Y., Hayward, S. W., & Matusik, R. J. (2014) · Oncogene · doi:10.1038/onc.2014.302 · Cited by 104
Kallio, H. M. L., Hieta, R., Latonen, L., Brofeldt, A., Annala, M., Kivinummi, K. K., Tammela, T. L. J., Nykter, M., Isaacs, W. B., Lilja, H. G., et al. (2018) · British Journal of Cancer · doi:10.1038/s41416-018-0172-0 · Cited by 103
Enzalutamide: A Review in Castration-Resistant Prostate Cancer
Scott, L. J. (2018) · Drugs · doi:10.1007/s40265-018-1029-9 · Cited by 100
Mechanism of Androgen Receptor Antagonism by Bicalutamide in the Treatment of Prostate Cancer
Osguthorpe, D. J., & Hagler, A. T. (2011) · Biochemistry · doi:10.1021/bi102059z · Cited by 100
TOMBAL, B. F., Borre, M., Rathenborg, P., Werbrouck, P., Poppel, H. V., Heidenreich, A., Iversen, P., Braeckman, J., Heráček, J., Baskin-Bey, E. S., et al. (2014) · The Lancet Oncology · doi:10.1016/s1470-2045(14)70129-9 · Cited by 100
Resistance to Novel Antiandrogen Therapies in Metastatic Castration-Resistant Prostate Cancer
Antonarakis, E. S., & Boudadi, K. (2016) · Clinical Medicine Insights Oncology · doi:10.4137/cmo.s34534 · Cited by 101
Neoadjuvant hormonal therapy before radical prostatectomy in high-risk prostate cancer
Devos, G., Devlies, W., Meerleer, G. D., Baldewijns, M. M. L. L., Gevaert, T., Moris, L., Milonas, D., Poppel, H. V., Berghen, C., Everaerts, W., et al. (2021) · Nature Reviews Urology · doi:10.1038/s41585-021-00514-9 · Cited by 103
Axerio-Cilies, P., Lack, N. A., Nayana, M. R. S., Chan, K. H., Yeung, A., Leblanc, E., Guns, E. S. T., Rennie, P. S., & Cherkasov, A. (2011) · Journal of Medicinal Chemistry · doi:10.1021/jm200532b · Cited by 97
Role of the androgen receptor in triple-negative breast cancer.
Rampurwala, M. M., Wisinski, K. B., & O'Regan, R. M. (2016) · PubMed · Cited by 97
Androgen receptor signaling pathways as a target for breast cancer treatment
Pietri, E., Conteduca, V., Andreis, D., Massa, I., Melegari, E., Sarti, S., Cecconetto, L., Schirone, A., Bravaccini, S., Serra, P., et al. (2016) · Endocrine Related Cancer · doi:10.1530/erc-16-0190 · Cited by 101
Targeting Nuclear Receptors with PROTAC degraders
Flanagan, J. J., & Neklesa, T. K. (2019) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2019.110452 · Cited by 98
Development of Peptidomimetic Inhibitors of the ERG Gene Fusion Product in Prostate Cancer
Wang, X., Qiao, Y., Asangani, I. A., Ateeq, B., Poliakov, A., Cieslik, M. P., Pitchiaya, S., Chakravarthi, B. V. S. K., Cao, X., Jing, X., et al. (2017) · Cancer Cell · doi:10.1016/j.ccell.2017.02.017 · Cited by 96
Aldo-Keto Reductase (AKR) 1C3 inhibitors: a patent review
Penning, T. M. (2017) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2017.1379503 · Cited by 96
Inhibition of USP14 enhances the sensitivity of breast cancer to enzalutamide
Xia, X., Huang, C., Liao, Y., Liu, Y., He, J., Guo, Z., Jiang, L., Wang, X., Liu, J., & Huang, H. (2019) · Journal of Experimental & Clinical Cancer Research · doi:10.1186/s13046-019-1227-7 · Cited by 96
Armstrong, C. M., & Gao, A. C. (2015) · Europe PMC (PubMed Central) · Cited by 95
Ponnusamy, S., Coss, C. C., Thiyagarajan, T., Watts, K., Hwang, D., He, Y., Selth, L. A., McEwan, I. J., Duke, C. B., Pagadala, J., et al. (2017) · Cancer Research · doi:10.1158/0008-5472.can-17-0976 · Cited by 95
Consideration of breast cancer subtype in targeting the androgen receptor
Venema, C. M., Bense, R. D., Steenbruggen, T. G., Nienhuis, H. H., Qiu, S.-Q., van Kruchten, M., Brown, M. A., Tamimi, R. M., Hospers, G. A. P., Schroder, C. P., et al. (2019) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2019.05.005 · Cited by 94
Lai, K., Huang, C.-K., Chang, Y., Chung, C., Yamashita, S., Li, L., Lee, S. O., Yeh, S., & Chang, C. (2012) · American Journal Of Pathology · doi:10.1016/j.ajpath.2012.10.029 · Cited by 93
Mitsiades, N. (2013) · Cancer Research · doi:10.1158/0008-5472.can-12-4414 · Cited by 91
Li, F., Han, M., Dai, P., Xu, W., He, J., Tao, X., Wu, Y., Tong, X., Xia, X., Guo, W., et al. (2021) · Nature Communications · doi:10.1038/s41467-021-21171-x · Cited by 98
Self-citationAndrogen receptor gene mutation, rearrangement, polymorphism.
Eisermann, K., Wang, D., Jing, Y., Pascal, L. E., & Wang, Z. (2013) · Europe PMC (PubMed Central) · doi:10.3978/j.issn.2223-4683.2013.09.15 · Cited by 94
Mechanisms of Androgen Receptor Activation in Castration-Resistant Prostate Cancer
Sharifi, N. (2013) · Endocrinology · doi:10.1210/en.2013-1466 · Cited by 96
Agonist and antagonist switch DNA motifs recognized by human androgen receptor in prostate cancer
Chen, Z., Lan, X., Thomas‐Ahner, J. M., Wu, D., Liu, X., Ye, Z., Wang, L., Sunkel, B. D., Grenade, C., Chen, J., et al. (2014) · The EMBO Journal · doi:10.15252/embj.201490306 · Cited by 93
Yu, Z., Cai, C., Gao, S., Simon, N. I., Shen, H. C., & Balk, S. P. (2014) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-14-0292 · Cited by 90
Lee, S. O., Ma, Z., Yeh, C.-R., Luo, J., Lin, T., Lai, K.-P., Yamashita, S., Liang, L., Tian, J., Li, L., et al. (2012) · Journal of Molecular Cell Biology · doi:10.1093/jmcb/mjs042 · Cited by 90
Current Insights into Long Non-Coding RNAs (LncRNAs) in Prostate Cancer
Smolle, M. A., Bauernhofer, T., Pummer, K., Călin, G. A., & Pichler, M. (2017) · International Journal of Molecular Sciences · doi:10.3390/ijms18020473 · Cited by 90
Androgen receptor profiling predicts prostate cancer outcome
Stelloo, S., Nevedomskaya, E., van der Poel, H. G., de Jong, J., van Leenders, G. J. L. H., Jenster, G. W., Wessels, L. F. A., Bergman, A. M., & Zwart, W. T. (2015) · EMBO Molecular Medicine · doi:10.15252/emmm.201505424 · Cited by 93
The metabolism, analysis, and targeting of steroid hormones in breast and prostate cancer
Capper, C. P., Rae, J. M., & Auchus, R. J. (2016) · Hormones and Cancer · doi:10.1007/s12672-016-0259-0 · Cited by 89
Targeting the androgen receptor in prostate and breast cancer: several new agents in development
Proverbs-Singh, T. A., Feldman, J. L., Morris, M. J., Autio, K. A., & Traina, T. A. (2015) · Endocrine Related Cancer · doi:10.1530/erc-14-0543 · Cited by 90
Wnt/Beta-Catenin Signaling and Prostate Cancer Therapy Resistance
Yeh, Y. A., Guo, Q., Connelly, Z. M., Cheng, S., Yang, S., Prieto‐Domínguez, N., & Yu, X. (2019) · Advances in experimental medicine and biology · doi:10.1007/978-3-030-32656-2_16 · Cited by 94
Munuganti, R. S. N., Leblanc, E., Axerio-Cilies, P., Labrière, C., Frewin, K., Singh, K., Hassona, M. D. H., Lack, N. A., Li, H., Ban, F., et al. (2013) · Journal of Medicinal Chemistry · doi:10.1021/jm3015712 · Cited by 91
Advancing Precision Medicine for Prostate Cancer Through Genomics
Roychowdhury, S., & Chinnaiyan, A. M. (2013) · Journal of Clinical Oncology · doi:10.1200/jco.2012.45.3662 · Cited by 88
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Labrie, F. (2011) · Nature Reviews Urology · doi:10.1038/nrurol.2010.231 · Cited by 89
Intrinsic disorder in the androgen receptor: identification, characterisation and drugability
McEwan, I. J. (2011) · Molecular BioSystems · doi:10.1039/c1mb05249g · Cited by 93
Hamid, A. R. A. H., Pfeiffer, M. J., Verhaegh, G. W. C. T., Schaafsma, E., Brandt, A. M., Sweep, F. C. G. J., Sedelaar, J. P. M., & Schalken, J. A. (2012) · Molecular Medicine · doi:10.2119/molmed.2012.00296 · Cited by 87
Bioinformatics and variability in drug response: a protein structural perspective
Lahti, J. L., Tang, G. W., Capriotti, E., Liu, T., & Altman, R. B. (2012) · Journal of The Royal Society Interface · doi:10.1098/rsif.2011.0843 · Cited by 89
Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors
Richters, A., Doyle, S. K., Freeman, D. B., Lee, C., Leifer, B. S., Jagannathan, S., Kabinger, F., Koren, J. V., Struntz, N. B., Urgiles, J., et al. (2021) · Cell Chemical Biology · doi:10.1016/j.chembiol.2020.10.001 · Cited by 86
Effect of Ack1 tyrosine kinase inhibitor on ligand-independent androgen receptor activity.
Mahajan, K., Challa, S., Coppola, D., Lawrence, H., Luo, Y., Gevariya, H., Zhu, W., Chen, Y. A., Lawrence, N. J., & Mahajan, N. P. (2010) · The Prostate · doi:10.1002/pros.21163 · Cited by 86
Self-citationRevising the role of the androgen receptor in breast cancer
Fioretti, F. M., Sita-Lumsden, A. R., Bevan, C. L., & Brooke, G. N. (2014) · Journal of Molecular Endocrinology · doi:10.1530/jme-14-0030 · Cited by 89
Martin, S. K., Pu, H., Penticuff, J. C., Cao, Z., Horbinski, C., & Kyprianou, N. (2015) · Cancer Research · doi:10.1158/0008-5472.can-15-2078 · Cited by 87
Androgen receptor targeted therapies in castration‐resistant prostate cancer: Bench to clinic
Imamura, Y., & Sadar, M. D. (2016) · International Journal of Urology · doi:10.1111/iju.13137 · Cited by 88
Choi, E., Buie, J. D., Camacho, J., Sharma, P., & de Riese, W. T. W. (2022) · Research and Reports in Urology · doi:10.2147/rru.s303215 · Cited by 92
Rathkopf, D. E., Patel, M. R., Choudhury, A. D., Rasco, D. W., Lakhani, N. J., Hawley, J. E., Srinivas, S., Aparicio, A. M., Narayan, V., Runcie, K. D., et al. (2024) · Annals of Oncology · doi:10.1016/j.annonc.2024.09.005 · Cited by 89
Self-citationYamaoka, M., Hara, T., & Kusaka, M. (2010) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-10-0255 · Cited by 86
Sex hormones and prostate cancer
Auchus, R. J., & Sharifi, N. (2020) · Annual Review of Medicine · doi:10.1146/annurev-med-051418-060357 · Cited by 85
Meanwell, N. A. (2013) · Topics in medicinal chemistry · doi:10.1007/7355_2013_29 · Cited by 86
Moreira, R. B., Debiasi, M., Francini, E., Nuzzo, P. V., de Velasco, G., Maluf, F. C., Fay, A. P., Joaquim Bellmunt, B., Choueiri, T. K., & Schutz, F. A. B. (2017) · Oncotarget · doi:10.18632/oncotarget.20028 · Cited by 85
Cai, L., Tsai, Y., Wang, P., Wang, J., Li, D., Fan, H., Zhao, Y., Bareja, R., Lu, R., Wilson, E. M., et al. (2018) · Molecular Cell · doi:10.1016/j.molcel.2018.08.029 · Cited by 87
Crona, D. J., Milowsky, M., & Whang, Y. E. (2015) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt.256 · Cited by 84
Zhao, J., Ning, S., Lou, W., Yang, J. C., Armstrong, C. M., Lombard, A. P., D'Abronzo, L. S., Evans, C. P., Gao, A. C., & Liu, C. (2020) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-20-0015 · Cited by 85
Patient-derived xenografts as in vivo models for research in urological malignancies
Inoue, T., Terada, N., Kobayashi, T., & Ogawa, O. (2017) · Nature Reviews Urology · doi:10.1038/nrurol.2017.19 · Cited by 88
Metadata
- Authors
- Tran, C., Ouk, S., Clegg, N. J., Chen, Y., Watson, P. A., Arora, V., Wongvipat, J., Smith-Jones, P. M., Yoo, D., Kwon, A., Wasielewska, T., Welsbie, D., Chen, C. D., Higano, C. S., Beer, T. M., Hung, D. T., Scher, H. I., Jung, M. E., & Sawyers, C. L.
- Affiliations
- Memorial Sloan Kettering Cancer Center (US)
- University of California, Los Angeles (US)
- University of Washington (US)
- Oregon Health & Science University (US)
- Medivation, Inc. (United States) (US)
- Corresponding author
- Tran, Chris
- Ouk, Samedy
- Chen, Charlie Degui
- Jung, Michael E.
- Sawyers, Charles L.
- ORCID
- Venue
- Science
- Published
- 2009-05-08
- Volume
- 324
- Issue
- 5928
- Pages
- 787-790
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- PMC
- PMC2981508
- OpenAlex
- W2119504728
- Cited by
- 2,292
- References
- 21
- Citations by year
- 2026: 58 · 2025: 91 · 2024: 110 · 2023: 141 · 2022: 139 · 2021: 150 · 2020: 152 · 2019: 131 · 2018: 146 · 2017: 145 · 2016: 157 · 2015: 134 · 2014: 163 · 2013: 163 · 2012: 160
- FWCI
- 116.20
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Science (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Cancer Institute (P50CA092629)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Prostate Cancer Treatment and Research
- Physical Sciences › Chemistry › Organic Chemistry › Heterocyclic Compound Synthesis and Bioactivity
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Hormonal and reproductive studies
- Keywords
- castration-resistant prostate cancer, androgen receptor antagonists, enzalutamide, androgen receptor, bicalutamide, nonsteroidal antiandrogens, androgen receptor nuclear translocation, coactivator recruitment, prostate-specific antigen, oral anticancer drugs, drug development
- MeSH terms
- Androgen Antagonists, Anilides, Animals, Antineoplastic Agents, Benzamides, Biological Availability, Cell Nucleus, DNA, Drug Screening Assays, Antitumor, Humans, Male, Nitriles, Phenylthiohydantoin, Prostatic Neoplasms, Receptors, Androgen, Tosyl Compounds, Transcription, Genetic, Gene Expression Regulation, Neoplastic, Xenograft Model Antitumor Assays, Cell Line, Tumor, Cell Proliferation, Mice
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