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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]
In the citing paper
“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 401–500 of 1,000
Therapy escape mechanisms in the malignant prostate
Santer, F. R., Erb, H. H. H., & McNeill, R. V. (2015) · Seminars in Cancer Biology · doi:10.1016/j.semcancer.2015.08.005 · Cited by 67
Fred Saad, C., & Fizazi, K. S. (2015) · Urology · doi:10.1016/j.urology.2015.07.034 · Cited by 67
Beyond the Ligand-Binding Pocket: Targeting Alternate Sites in Nuclear Receptors
Caboni, L., & Lloyd, D. G. (2012) · Medicinal Research Reviews · doi:10.1002/med.21275 · Cited by 64
A Phase II Trial of Temsirolimus in Men With Castration-Resistant Metastatic Prostate Cancer
Armstrong, A. J., Shen, T., Halabi, S., Kemeny, G., Bitting, R. L., Kartcheske, P. A., Embree, E., Morris, K. K., Winters, C., Jaffe, T. A., et al. (2013) · Clinical Genitourinary Cancer · doi:10.1016/j.clgc.2013.05.007 · Cited by 66
Zhang, Y., Won, S., Jiang, C., Lee, H., Jeong, S., Lee, E., Zhang, J., Ye, M., Kim, S., & Lü, J. (2012) · Pharmaceutical Research · doi:10.1007/s11095-012-0670-3 · Cited by 64
Oh, S. J., Erb, H. H. H., Hobisch, A., Santer, F. R., & Čulig, Z. (2012) · Endocrine Related Cancer · doi:10.1530/erc-11-0298 · Cited by 64
Zhan, Y., Zhang, G., Wang, X., Qi, Y., Bai, S., Li, D., Ma, T., Sartor, O. A., Flemington, E. K., Zhang, H., et al. (2016) · Molecular Cancer Research · doi:10.1158/1541-7786.mcr-16-0236 · Cited by 66
Wang, H., Zhang, C., Rorick, A. M., Wu, D., Chiu, M., Thomas‐Ahner, J. M., Chen, Z., Chen, H., Clinton, S. K., Chan, K. K., et al. (2011) · Cancer Research · doi:10.1158/0008-5472.can-10-4576 · Cited by 64
Endo, S., Oguri, H., Segawa, J., Kawai, M., Hu, D., Xia, S., Okada, T., Irie, K., Fujii, S., Gouda, H., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00939 · Cited by 64
Fernandez, E. V., Reece, K. M., Ley, A. M., Troutman, S. M., Sissung, T. M., Price, D. K., Chau, C. H., & Figg, W. D. (2015) · Molecular Pharmacology · doi:10.1124/mol.114.097477 · Cited by 63
Schweizer, M. T., & Antonarakis, E. S. (2012) · Therapeutic Advances in Urology · doi:10.1177/1756287212452196 · Cited by 63
Targeting the androgen receptor in triple-negative breast cancer: current perspectives
Mina, A. A., Yoder, R., & Sharma, P. (2017) · OncoTargets and Therapy · doi:10.2147/ott.s126051 · Cited by 63
Xiong, W., Huang, C., Deng, H., Jian, C., Zen, C., Ye, K., Zhong, Z., Zhao, X., & Zhu, L. (2017) · The International Journal of Biochemistry & Cell Biology · doi:10.1016/j.biocel.2017.12.005 · Cited by 63
Ito, Y., & Sadar, M. D. (2018) · Research and Reports in Urology · doi:10.2147/rru.s157116 · Cited by 63
Hormone therapy for ovarian cancer: Emphasis on mechanisms and applications (Review)
Li, H., Liu, Y., Wang, Y., Zhao, X., & Qi, X. (2021) · Oncology Reports · doi:10.3892/or.2021.8174 · Cited by 68
Knuuttila, M., Yatkin, E., Kallio, J., Savolainen, S., Laajala, T. D., Aittokallio, T. A., Oksala, R., Häkkinen, M. R., Keski‐Rahkonen, P., Auriola, S. O. K., et al. (2014) · American Journal Of Pathology · doi:10.1016/j.ajpath.2014.04.010 · Cited by 65
Preclinical evaluation of the AR inhibitor enzalutamide in triple-negative breast cancer cells
Caiazza, F., Murray, A. M., Madden, S. F., Synnott, N. C., Ryan, E. J., O’Donovan, N., Crown, J. P., & Duffy, M. J. (2016) · Endocrine Related Cancer · doi:10.1530/erc-16-0068 · Cited by 63
Mechanisms of Prostate Cancer Initiation and Progression
Knudsen, B. S., & Vasioukhin, V. I. (2010) · Advances in cancer research · doi:10.1016/b978-0-12-380890-5.00001-6 · Cited by 71
Design and Synthesis of Novel Cereblon Binders for Use in Targeted Protein Degradation
Norris, S. H., Ba, X., Rhodes, J., Huang, D., Khambatta, G., Buenviaje, J., Nayak, S. K., Meiring, J., Reiss, S. M., Xu, S., et al. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c01848 · Cited by 61
Tamae, D., Mostaghel, E. A., Montgomery, B., Nelson, P. S., Balk, S. P., Kantoff, P. W., Taplin, M., & Penning, T. M. (2014) · Chemico-Biological Interactions · doi:10.1016/j.cbi.2014.12.012 · Cited by 61
Oncologic Imaging: A Guiding Hand of Personalized Cancer Care
Hricak, H. (2011) · Radiology · doi:10.1148/radiol.11110252 · Cited by 61
RhoA as a Mediator of Clinically Relevant Androgen Action in Prostate Cancer Cells
Schmidt, L. J., Duncan, K., Yadav, N., Regan, K. M., Verone, A. R., Lohse, C. M., POP, E. A., Attwood, K. M., Wilding, G. E., Mohler, J. L., et al. (2012) · Molecular Endocrinology · doi:10.1210/me.2011-1130 · Cited by 61
Molecular Pathways: Targeting Resistance in the Androgen Receptor for Therapeutic Benefit
Mostaghel, E. A., Plymate, S. R., & Montgomery, B. (2013) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-12-3601 · Cited by 63
Flaig, T. W., Potluri, R. C., Ng, Y., Todd, M. B., & Mehra, M. (2015) · Cancer Medicine · doi:10.1002/cam4.576 · Cited by 61
Banuelos, C. A., Tavakoli, I., Tien, A. H., Caley, D. P., Mawji, N. R., Li, Z., Wang, J., Yang, Y. C., Imamura, Y., Yan, L., et al. (2016) · Journal of Biological Chemistry · doi:10.1074/jbc.m116.734475 · Cited by 62
Rice, M. A., Hsu, E., Aslan, M., Ghoochani, A., Su, A., & Stoyanova, T. I. (2019) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-18-0804 · Cited by 60
Advances in Androgen Receptor Targeted Therapy for Prostate Cancer
Ahmed, A., Ali, S. S., & Sarkar, F. H. (2013) · Journal of Cellular Physiology · doi:10.1002/jcp.24456 · Cited by 60
Mounir, Z., Lin, F., Lin, V., Korn, J. M., Yu, Y., Valdez, R., Aina, O. H., Buchwalter, G., Jaffe, A. B., Korpal, M., et al. (2014) · Oncogene · doi:10.1038/onc.2014.308 · Cited by 60
Chen, Y., Cheng, F., Sun, L. G., Li, W., Liu, G., & Tang, Y. (2014) · Ecotoxicology and Environmental Safety · doi:10.1016/j.ecoenv.2014.08.026 · Cited by 61
Self-citationAbiraterone in Prostate Cancer: A New Angle to an Old Problem
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An update on enzalutamide in the treatment of prostate cancer
Merseburger, A. S., Haas, G. P., & von Klot, C. A. (2014) · Therapeutic Advances in Urology · doi:10.1177/1756287214555336 · Cited by 60
Ning, Y. M., Pierce, W. F., Maher, V. E., Karuri, S. W., Tang, S. W., Chiu, H.-J., Palmby, T. R., Zirkelbach, J. F., Marathe, D. D., Mehrotra, N., et al. (2013) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-13-1763 · Cited by 60
Naderi, A., Chia, K. M., & Liu, J. T. (2011) · Breast Cancer Research · doi:10.1186/bcr2858 · Cited by 60
Moving Beyond the Androgen Receptor (AR): Targeting AR-Interacting Proteins to Treat Prostate Cancer
Foley, C., & Mitsiades, N. (2016) · Hormones and Cancer · doi:10.1007/s12672-015-0239-9 · Cited by 62
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Luthold, C., Hallal, T., Labbé, D. P., & Bordeleau, F. (2022) · Cancers · doi:10.3390/cancers14122887 · Cited by 62
Emerging data on androgen receptor splice variants in prostate cancer
Cao, S., Zhan, Y., & Dong, Y. (2016) · Endocrine Related Cancer · doi:10.1530/erc-16-0298 · Cited by 62
Anti-androgen hormonal therapy for cancer and other diseases
Student, S., Hejmo, T., Poterała-Hejmo, A., Leśniak, A., & Bułdak, R. J. (2019) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2019.172783 · Cited by 63
Saber, S. H., Ali, H. E. A., Gaballa, R., Gaballah, M. S. A., Ali, H. I., Zerfaoui, M., & Elmageed, Z. Y. A. (2020) · Cells · doi:10.3390/cells9030564 · Cited by 63
Zarif, J. C., Lamb, L. E., Schulz, V. V., Nollet, E. A., & Miranti, C. K. (2015) · Oncotarget · doi:10.18632/oncotarget.3119 · Cited by 58
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Schiewer, M. J., Augello, M. A., & Knudsen, K. E. (2011) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2011.06.033 · Cited by 60
McGrath, M. J., Binge, L. C., Sriratana, A., Wang, H., Robinson, P. A., Pook, D. W., Fedele, C. G., Brown, S., Dyson, J. M., Cottle, D. L., et al. (2013) · Cancer Research · doi:10.1158/0008-5472.can-12-4520 · Cited by 58
New and emerging agents for the treatment of castration-resistant prostate cancer
Higano, C. S., & Crawford, E. D. (2011) · Urologic Oncology Seminars and Original Investigations · doi:10.1016/j.urolonc.2011.08.013 · Cited by 58
Self-citationLi, X., Liu, Z., Xu, X., Blair, C. A., Sun, Z., Xie, J., Lilly, M. B., & Zi, X. (2012) · PLoS ONE · doi:10.1371/journal.pone.0031213 · Cited by 58
Crnalic, S., Hörnberg, E., Wikström, P., Lerner, U. H., Tieva, Å., Svensson, O., Widmark, A., & Bergh, A. R. J. (2010) · Endocrine Related Cancer · doi:10.1677/erc-10-0059 · Cited by 58
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Karamouzis, M. V., Papavassiliou, K. A., Adamopoulos, C., & Papavassiliou, A. G. (2015) · Trends in cancer · doi:10.1016/j.trecan.2015.12.001 · Cited by 59
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Ferroni, C., Pepe, A., Kim, Y. S., Lee, S., Guerrini, A., Parenti, M. D., Tesei, A., Zamagni, A., Cortesi, M., Zaffaroni, N., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00105 · Cited by 58
Shaw, J., Leveridge, M., Norling, C., Karén, J., Molina, D. M., O’Neill, D. J., Dowling, J. E., Davey, P. R. J., Cowan, S., Dabrowski, M. A., et al. (2018) · Scientific Reports · doi:10.1038/s41598-017-18650-x · Cited by 58
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McKay, R. R., Feng, F. Y.-C., Wang, A. Y., Wallis, C. J. D., & Moses, K. A. (2020) · American Society of Clinical Oncology Educational Book · doi:10.1200/edbk_279459 · Cited by 60
Lv, S., Song, Q., Chen, G., Cheng, E., Chen, W., Cole, R. N., Wu, Z., Pascal, L. E., Wang, K., Wipf, P., et al. (2020) · Journal of Clinical Investigation · doi:10.1172/jci141335 · Cited by 58
Sridaran, D., Chouhan, S., Mahajan, K. N., Renganathan, A., Weimholt, C., Bhagwat, S., Reimers, M. A., Kim, E. H., Thakur, M. K., Saeed, M. A., et al. (2022) · Nature Communications · doi:10.1038/s41467-022-34724-5 · Cited by 59
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Knudsen, K. E., & Kelly, W. K. (2011) · Expert Review of Endocrinology & Metabolism · doi:10.1586/eem.11.33 · Cited by 60
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Asim, M., Massie, C. E., Orafidiya, F. A., Pértega‐Gomes, N., Warren, A. Y., Esmaeili, M., Selth, L. A., Zecchini, H. I., Luko, K., Qureshi, A., et al. (2015) · JNCI Journal of the National Cancer Institute · doi:10.1093/jnci/djv371 · Cited by 58
Sato, S., Katsushima, K., Shinjo, K., Hatanaka, A., Ohka, F., Suzuki, S., Naiki‐Ito, A., Soga, N., Takahashi, S., & Kondo, Y. (2016) · Cancer Research · doi:10.1158/0008-5472.can-15-3339 · Cited by 60
Wang, R., Lin, W., Lin, C.-Y., Li, L., Sun, Y., & Chang, C. (2016) · Cancer Letters · doi:10.1016/j.canlet.2016.05.018 · Cited by 57
Androgen receptor antagonism drives cytochrome P450 17A1 inhibitor efficacy in prostate cancer
Norris, J. D., Miner, S. J., Baker, J. G., Stagg, D. B., Wardell, S. E., Park, S. H., Alley, H. M., Baldi, R. M., Yllanes, A. P., Andreano, K. J., et al. (2017) · Journal of Clinical Investigation · doi:10.1172/jci87328 · Cited by 57
Liang, C., Wang, S., Qin, C., Bao, M., Cheng, G., Liu, B., Shao, P., Lv, Q., Song, N., Hua, L., et al. (2018) · Cell Death and Disease · doi:10.1038/s41419-017-0197-y · Cited by 59
Molecular determinants for enzalutamide-induced transcription in prostate cancer
Yuan, F., Hankey, W., Wu, D., Wang, H., Somarelli, J. A., Armstrong, A. J., Huang, J., Chen, Z., & Wang, Q. (2019) · Nucleic Acids Research · doi:10.1093/nar/gkz790 · Cited by 60
Morris, M. J., Heller, G., Hillman, D. W., Bobek, O. J., Ryan, C. J., Antonarakis, E. S., Bryce, A. H., Hahn, O. M., Beltran, H., Armstrong, A. J., et al. (2023) · Journal of Clinical Oncology · doi:10.1200/jco.22.02394 · Cited by 56
Zhang, J., Wei, J., Sun, R., Sheng, H., Yin, K., Pan, Y., Jiménez, R. E., Chen, S., Cui, X., Zou, Z., et al. (2023) · Molecular Cell · doi:10.1016/j.molcel.2023.06.024 · Cited by 58
Li, X., Wang, Y., Deng, S., Zhu, G., Wang, C., Johnson, N. A., Zhang, Z., Tirado, C. R., Xu, Y., Metang, L. A., et al. (2023) · Cancer Cell · doi:10.1016/j.ccell.2023.06.010 · Cited by 61
Targeting the interleukin‐11 receptor α in metastatic prostate cancer: A first‐in‐man study
Pasqualini, R., Millikan, R. E., Christianson, D. R., Cardó‐Vila, M., Driessen, W. H. P., Giordano, R. J., Hajitou, A., Hoang, A. G., Wen, S., Barnhart, K. F., et al. (2015) · Cancer · doi:10.1002/cncr.29344 · Cited by 56
Caboni, L., Kinsella, G. K., Blanco, F., Fayne, D., Jagoe, W. N., Carr, M. J., Williams, D. C., Meegan, M. J., & Lloyd, D. G. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm201438f · Cited by 56
Roell, D., & Baniahmad, A. (2010) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2010.09.013 · Cited by 56
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Dudek, H., Wong, D. H., Arvan, R., Shah, A., Wortham, K. A., Ying, B., Diwanji, R., Zhou, W. L., Holmes, B. R., Yang, H., et al. (2013) · Molecular Therapy · doi:10.1038/mt.2013.233 · Cited by 56
Fred Saad, C. (2013) · Therapeutic Advances in Urology · doi:10.1177/1756287213490054 · Cited by 56
Ban, F., Leblanc, E., Li, H., Munuganti, R. S. N., Frewin, K., Rennie, P. S., & Cherkasov, A. R. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm500684r · Cited by 56
Hoefer, J., Akbor, M., Handle, F., Ofer, P., Puhr, M., Parson, W., Čulig, Z., Klocker, H., & Heidegger, I. M. (2016) · Oncotarget · doi:10.18632/oncotarget.10926 · Cited by 57
Duan, M., Liu, N., Zhou, W., Li, D., Yang, M., & Hou, T. (2016) · Journal of Chemical Theory and Computation · doi:10.1021/acs.jctc.6b00424 · Cited by 56
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Snow, O., Lallous, N., Singh, K., Lack, N. A., Rennie, P. S., & Cherkasov, A. R. (2019) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2019.05.001 · Cited by 56
Human Steroid Biosynthesis for the Oncologist
Auchus, M., & Auchus, R. J. (2012) · Journal of Investigative Medicine · doi:10.2310/jim.0b013e3182408567 · Cited by 57
Westbrook, T. C., Guan, X., Rodansky, E. S., Flores, D. L., Liu, C.-J., Udager, A. M., Patel, R. A., Haffner, M. C., Hu, Y., Sun, D., et al. (2022) · Nature Communications · doi:10.1038/s41467-022-32701-6 · Cited by 57
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Friedlander, T. W., & Ryan, C. J. (2012) · Urologic Clinics of North America · doi:10.1016/j.ucl.2012.07.003 · Cited by 55
Xu, X. Y., Xu, X., Liu, P., Zhu, Z.-Y., Chen, J., Fu, H., Chen, L., Hu, L., & Shen, X. (2015) · Journal of Biological Chemistry · doi:10.1074/jbc.m114.630475 · Cited by 55
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Zarif, J. C., & Miranti, C. K. (2016) · Cellular Signalling · doi:10.1016/j.cellsig.2016.01.013 · Cited by 59
Schwartzberg, L. S., Yardley, D. A., ELIAS, A. D., Patel, M. R., LoRusso, P. M., Burris, H. A., Gucalp, A., Peterson, A., Blaney, M. E., Steinberg, J., et al. (2017) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-16-2339 · Cited by 55
Pal, S. K., Moreira, D., Won, H., White, S. V., Duttagupta, P., Lúcia, M., Jones, J. O., Hsu, J., & Kortylewski, M. (2019) · International Journal of Molecular Sciences · doi:10.3390/ijms20081831 · Cited by 55
Modulating protein–protein interaction networks in protein homeostasis
Zhong, M., Lee, G., Sijbesma, E., Ottmann, C., & Arkin, M. R. (2019) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2019.02.012 · Cited by 57
Penning, T. M. (2015) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2015.05.010 · Cited by 56
Molecular alterations and emerging targets in castration resistant prostate cancer
Lorente, D., & Bono, J. S. D. (2014) · European Journal of Cancer · doi:10.1016/j.ejca.2013.12.004 · Cited by 55
Opposing Effects of Androgen Deprivation and Targeted Therapy on Prostate Cancer Prevention
Jia, S., Gao, X., Lee, S., Maira, S.-M., Wu, X., Stack, E. C., Signoretti, S., Loda, M. F., Zhao, J. J., & Roberts, T. M. (2012) · Cancer Discovery · doi:10.1158/2159-8290.cd-12-0262 · Cited by 54
Wen, S., He, Y., Wang, L., Zhang, J., Quan, C., Niu, Y., & Huang, H. (2020) · Oncogene · doi:10.1038/s41388-020-01456-z · Cited by 55
Cherian, M. T., Lin, W., Wu, J., & Chen, T. (2015) · Molecular Pharmacology · doi:10.1124/mol.115.097782 · Cited by 54
Targeting persistent androgen receptor signaling in castration-resistant prostate cancer
Graham, L. S., & Schweizer, M. T. (2016) · Medical Oncology · doi:10.1007/s12032-016-0759-3 · Cited by 54
He, L., Fang, H., Chen, C., Wu, Y., Wang, Y., Ge, H., Wang, L., Wan, Y., & He, H. (2020) · Medicine · doi:10.1097/md.0000000000019760 · Cited by 55
Self-citationEighty Years of Targeting Androgen Receptor Activity in Prostate Cancer: The Fight Goes on
Estébanez‐Perpiñá, E., Bevan, C. L., & McEwan, I. J. (2021) · Cancers · doi:10.3390/cancers13030509 · Cited by 54
Zhang, Z., Chng, K. R., Lingadahalli, S., Chen, Z., Liu, M. H., Do, H. H., Cai, S., Rinaldi, N. J., Poh, H. M., Li, G., et al. (2019) · Genome Research · doi:10.1101/gr.230243.117 · Cited by 54
Khirallah, S. M., Ramadan, H. M. M., Shawky, A. M., Qahl, S. H., Baty, R. S., Alqadri, N., Alsuhaibani, A. M., Jaremko, M., Emwas, A.-H. M., & Saied, E. M. (2022) · Molecules · doi:10.3390/molecules27196271 · Cited by 54
Burris, T. P., de Vera, I. M. S., Côté, I., Flaveny, C. A., Wanninayake, U. S., Chatterjee, A., Walker, J. K., Steinauer, N., Zhang, J., Coons, L. A., et al. (2023) · Pharmacological Reviews · doi:10.1124/pharmrev.121.000436 · Cited by 54
Treatment strategies for high-risk locally advanced prostate cancer
Rosenthal, S. A., & Sandler, H. M. (2010) · Nature Reviews Urology · doi:10.1038/nrurol.2009.237 · Cited by 53
Higano, C. S., Beer, T. M., Taplin, M., Efstathiou, E., Hirmand, M., Forer, D., & Scher, H. I. (2015) · European Urology · doi:10.1016/j.eururo.2015.01.026 · Cited by 53
Self-citationAttard, G., & Bono, J. S. D. (2011) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-11-0943 · Cited by 53
Loriot, Y., Fizazi, K. S., Bono, J. S. D., Forer, D., Hirmand, M., & Scher, H. I. (2016) · Cancer · doi:10.1002/cncr.30336 · Cited by 53
Self-citationNiu, Y., Guo, C., Wen, S., Tian, J., Luo, J., Wang, K., Tian, H., Yeh, S., & Chang, C. (2018) · Cancer Letters · doi:10.1016/j.canlet.2018.09.020 · Cited by 53
Ji, C., Guha, M., Zhu, X., Whritenour, J., Hemkens, M. D., Tse, S., Walker, G. S., Evans, E., Khan, N., Finkelstein, M. B., et al. (2019) · Chemical Research in Toxicology · doi:10.1021/acs.chemrestox.9b00247 · Cited by 53
Serritella, A. V., Shevrin, D., Heath, E. I., Wade, J. L., Martinez, E., Anderson, A. K. L., Schonhoft, J. D., Chu, Y.-L., Karrison, T., Stadler, W. M., et al. (2022) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-21-4049 · Cited by 56
Christenson, J. L., O’Neill, K. I., Williams, M. M., Spoelstra, N. S., Jones, K. L., Trahan, G. D., Reese, J. M., Patten, E. T. V., ELIAS, A. D., Eisner, J. R., et al. (2021) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-20-0807 · Cited by 52
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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