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Androgen Receptor (AR) Coregulators: A Diversity of Functions Converging on and Regulating the AR Transcriptional Complex
Abstract
Androgens, acting through the androgen receptor (AR), are responsible for the development of the male phenotype during embryogenesis, the achievement of sexual maturation at puberty, and the maintenance of male reproductive function and behavior in adulthood. In addition, androgens affect a wide variety of nonreproductive tissues. Moreover, aberrant androgen action plays a critical role in multiple pathologies, including prostate cancer and androgen insensitivity syndromes. The formation of a productive AR transcriptional complex requires the functional and structural interaction of the AR with its coregulators. In the last decade, an overwhelming and ever increasing number of proteins have been proposed to possess AR coactivating or corepressing characteristics. Intriguingly, a vast diversity of functions has been ascribed to these proteins, indicating that a multitude of cellular functions and signals converge on the AR to regulate its function. The current review aims to provide an overview of the AR coregulator proteins identified to date and to propose a classification of these AR coregulator proteins according to the function(s) ascribed to them. Taken together, this approach will increase our understanding of the cellular pathways that converge on the AR to ensure an appropriate transcriptional response to androgens.
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“Androgen receptors can be modulated by specific proteins called coregulators [70–72] or mediated via the activation of membrane-bound protein receptors to initiate intracellular signalling pathways [73], which can occur even in the presence of low levels of androgens [74].”
From Integrating Transwomen and Female Athletes with Differences of Sex Development (DSD) into Elite Competition: The FIMS 2021 Consensus Statement (2021) · cites this paper as [71]
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Lin, W., Lu, K.-M., Chung, M.-H., Liu, S.-T., Chen, H.-H., Chang, Y., Wang, W.-M., & Huang, S.-M. (2010) · The International Journal of Biochemistry & Cell Biology · doi:10.1016/j.biocel.2010.09.024 · Cited by 10
Seleit, I., Bakry, O. A., Repey, H. S. E., & Ali, R. (2016) · Skin Pharmacology and Physiology · doi:10.1159/000446662 · Cited by 10
Myung, J., Wang, G., Chiu, H. H. L., Wang, J., Mawji, N. R., & Sadar, M. D. (2017) · PLoS ONE · doi:10.1371/journal.pone.0174134 · Cited by 10
Role of androgen and microRNA in triple-negative breast cancer
Al-Othman, N., Ahram, M. A., & Alqaraleh, M. (2019) · Breast Disease · doi:10.3233/bd-190416 · Cited by 10
Hormonal Therapy for Prostate Cancer
Vasilevskaya, I. A., Schiewer, M. J., & Knudsen, K. E. (2022) · doi:10.1093/med/9780198870197.003.0221 · Cited by 11
Tan, J.-A., Bai, S., Grossman, G., Titus, M. A., Ford, O. H., POP, E. A., Smith, G. J., Mohler, J. L., Wilson, E. M., & French, F. S. (2013) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2013.09.036 · Cited by 10
Jariwala, U., Cogan, J. P., Li, J., Frenkel, B., & Coetzee, G. A. (2008) · The Prostate · doi:10.1002/pros.20893 · Cited by 10
Zhang, J., Wu, D., He, Y., Li, L., Liu, S., Lu, J., Gui, H., Wang, Y., Tao, Y., Wang, H., et al. (2020) · Biochemistry and Biophysics Reports · doi:10.1016/j.bbrep.2020.100778 · Cited by 11
RETRACTED ARTICLE: ChIP-seq analysis of androgen receptor in LNCaP cell line
Tao, S., He, H., & Chen, Q. (2014) · Molecular Biology Reports · doi:10.1007/s11033-014-3511-0 · Cited by 9
RetractedThe Effects of Neuroactive Steroids on Myelin in Health and Disease
Kalakh, S., & Mouihate, A. (2024) · Medical Principles and Practice · doi:10.1159/000537794 · Cited by 8
Dobi, A., Sreenath, T., & Srivastava, S. K. (2013) · Springer eBooks · doi:10.1007/978-1-4614-6182-1_19 · Cited by 9
Immunolocalization of Androgen Receptor and Estrogen Receptors in Skin Tags
Bakry, O. A., Samaka, R. M., Shoeib, M. A., & Maher, A. (2014) · Ultrastructural Pathology · doi:10.3109/01913123.2014.911788 · Cited by 9
Metadata
- Authors
- Heemers, H. V., & Tindall, D. J.
- Affiliations
- Mayo Clinic (US)
- Corresponding author
- Tindall, Donald J.
- Venue
- Endocrine Reviews
- Publisher
- The Endocrine Society
- Published
- 2007-10-16
- Volume
- 28
- Issue
- 7
- Pages
- 778-808
- ISSN
- 0163-769X (ISSN-L)
- 1945-7189
- OpenAlex
- W2164092182
- Cited by
- 753
- References
- 375
- Citations by year
- 2026: 12 · 2025: 26 · 2024: 30 · 2023: 29 · 2022: 40 · 2021: 48 · 2020: 26 · 2019: 37 · 2018: 37 · 2017: 38 · 2016: 54 · 2015: 49 · 2014: 42 · 2013: 70 · 2012: 52
- FWCI
- 5.79
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Endocrine Reviews (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Cancer Institute (R01CA121277, CA125747, R01CA125747, CA 91956, CA121277, P50CA091956, CA 15083, P30CA015083)
- National Institute of Diabetes and Digestive and Kidney Diseases (R01DK065236, DK65236)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Prostate Cancer Treatment and Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Endocrinology › Estrogen and related hormone effects
- Health Sciences › Medicine › Reproductive Medicine › Sperm and Testicular Function
- Keywords
- androgen receptor, coregulators, transcriptional coactivator, corepressors, transcriptional complex, androgen signaling, male reproductive development, prostate cancer, androgen insensitivity syndrome
- MeSH terms
- Androgens, Gene Expression Regulation, Humans, Male, Receptors, Androgen, Transcription Factors
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