The DOI matches its Crossref record; 13 of the 13 references it cites were found in a registry or an index.
An androgen receptor N-terminal domain antagonist for treating prostate cancer
Open accessAbstract
Hormone therapies for advanced prostate cancer target the androgen receptor (AR) ligand-binding domain (LBD), but these ultimately fail and the disease progresses to lethal castration-resistant prostate cancer (CRPC). The mechanisms that drive CRPC are incompletely understood, but may involve constitutively active AR splice variants that lack the LBD. The AR N-terminal domain (NTD) is essential for AR activity, but targeting this domain with small-molecule inhibitors is complicated by its intrinsic disorder. Here we investigated EPI-001, a small-molecule antagonist of AR NTD that inhibits protein-protein interactions necessary for AR transcriptional activity. We found that EPI analogs covalently bound the NTD to block transcriptional activity of AR and its splice variants and reduced the growth of CRPC xenografts. These findings suggest that the development of small-molecule inhibitors that bind covalently to intrinsically disordered proteins is a promising strategy for development of specific and effective anticancer agents.
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Cites
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“Functional NTD is necessary for AR transcriptional activity (23–25).”
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Self-citationCREB-binding protein in androgen receptor-mediated signaling
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Cited by
Pathological Unfoldomics of Uncontrolled Chaos: Intrinsically Disordered Proteins and Human Diseases
Uversky, V. N., Davé, V., Iakoucheva, L. M., Malaney, P., Metallo, S. J., Pathak, R. R., & Joerger, A. C. (2014) · Chemical Reviews · doi:10.1021/cr400713r · Cited by 288
Han, X., Zhao, L., Xiang, W., Qin, C., Miao, B., McEachern, D., Wang, Y., Metwally, H., Wang, L., Matvekas, A., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00882 · Cited by 170
Intrinsically disordered proteins and biomolecular condensates as drug targets
Biesaga, M., Frigolé-Vivas, M., & Salvatella, X. (2021) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2021.02.009 · Cited by 115
Minireview: Dynamic Structures of Nuclear Hormone Receptors: New Promises and Challenges
Simons, S. S., Edwards, D. P., & Kumar, R. (2014) · Molecular Endocrinology · doi:10.1210/me.2013-1334 · Cited by 88
Rational optimization of a transcription factor activation domain inhibitor
Basu, S., Martínez-Cristóbal, P., Frigolé-Vivas, M., Pesarrodona, M., Lewis, M., Szulc, E., Bañuelos, C. A., Sánchez-Zarzalejo, C., Bielskutė, S., Zhu, J., et al. (2023) · Nature Structural & Molecular Biology · doi:10.1038/s41594-023-01159-5 · Cited by 83
“In addition, 3D HNCO and HNCA experiments were acquired for two 15N,13C double labeled AR AD (1-558) samples (25 μM and 100 μM) dissolved in NMR buffer.”
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Metadata
- Authors
- Myung, J.-K., Banuelos, C. A., Fernandez, J. G., Mawji, N. R., Wang, J., Tien, A. H., Yang, Y. C., Tavakoli, I., Haile, S., Watt, K., McEwan, I. J., Plymate, S., Andersen, R. J., & Sadar, M. D.
- Venue
- Journal of Clinical Investigation
- Published
- 2013-06-03
- Volume
- 123
- Issue
- 7
- Pages
- 2948-2960
- ISSN
- 0021-9738 (ISSN-L)
- OpenAlex
- W2017839954
- Cited by
- 305
- References
- 13
- FWCI
- 28.01
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Myung, J.-K., Banuelos, C. A., Fernandez, J. G., Mawji, N. R., Wang, J., Tien, A. H., Yang, Y. C., Tavakoli, I., Haile, S., Watt, K., McEwan, I. J., Plymate, S., Andersen, R. J., & Sadar, M. D. (2013). An androgen receptor N-terminal domain antagonist for treating prostate cancer. Journal of Clinical Investigation. https://doi.org/10.1172/jci66398
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