Cited by 525Prostate Cancer Treatment and ResearchEstrogen and related hormone effectsHormonal and reproductive studies

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Domains of the Human Androgen Receptor Involved in Steroid Binding, Transcriptional Activation, and Subcellular Localization

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Jenster, Guido, van der Korput, Hetty A. G. M., van Vroonhoven, Cor, van der Kwast, Theo H., Trapman, Jan, Brinkmann, Albert O.·1991·Molecular Endocrinology

DOI 10.1210/mend-5-10-1396

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Abstract

A series of human androgen receptor (AR) deletion mutants was constructed to study the relationship between the structural domains and their different functions in the AR protein. Human AR mutants were expressed in COS-1 and HeLa cells to investigate hormone binding, transcriptional activation, and subcellular localization. The wild-type human AR (AR 1–910) was expressed as a 110- to 112-kDa doublet, as revealed on immunoblots. All mutant AR proteins also migrated as doublets, except for one. This AR has a deletion from amino acid residues 51–211 and migrated as a single protein band, possibly due to altered posttranslational modification. The AR steroid-binding domain is encoded by approximately 250 amino acid residues in the Cterminal end. Deletions in this domain as well as truncation of the last 12 C-terminal amino acid residues abolished hormone binding. Cotransfection studies in HeLa cells showed that transcriptional activation of an androgen-regulated reporter gene construct was induced by the wildtype human AR. Mutational analysis revealed two regions in the N-terminal part, encoded by amino acid residues 51–211 and 244–360, to be essential for this transcriptional activation. Deletion of the hormone-binding domain yielded a constitutively active AR protein, indicating that in the absence of hormone this domain displays an inhibitory function. In the presence of its ligand, the wild-type AR was located in the cell nucleus. In the absence of androgens the receptor was mainly nuclear, but cytoplasmic localization was observed as well. In contrast, an AR deletion mutant lacking part of the DNAbinding domain and part of the hinge region was exclusively cytoplasmic in the absence of hormone. This mutant AR lacks a region that is highly conserved among steroid receptors and homologous to the simian virus-40 large T-antigen- and nucleoplas-min-nuclear localization signals. Transformation by hormone directed this mutant to the nucleus, indicating the presence of a second, hormone-dependent nuclear targeting mechanism.

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Background
Non-Steroidal Androgen Receptor Antagonists and Prostate Cancer: A Survey on Chemical Structures Binding this Fast-Mutating Target
Ferroni, C., & Varchi, G. (2018) · Current Medicinal Chemistry · doi:10.2174/0929867325666180913095239 · Cited by 11
Cellular growth factors as prospective therapeutic targets for combination therapy in androgen independent prostate cancer (AIPC)
Jonnalagadda, B., Arockiasamy, S., & Krishnamoorthy, S. (2020) · Life Sciences · doi:10.1016/j.lfs.2020.118208 · Cited by 11
Rapid detection of a mutation hot‐spot in the human androgen receptor
Malmgren, H., Gustavsson, J., Tuvemo, T., & Dahl, N. (1996) · Clinical Genetics · doi:10.1111/j.1399-0004.1996.tb02626.x · Cited by 11
Testicular Androgen Receptor Protein: Distribution and Control of Expression
Saunders, P. T. K., Millar, M. R., Majdič, G., Bremner, W. J., McLaren, T. T., Grigor, K. M., & Sharpe, R. M. (1996) · Springer eBooks · doi:10.1007/978-1-4612-2374-0_14 · Cited by 11
Prostate Screening in Patients With 46,XY Disorders of Sex Development—Is it Necessary?
Salmasi, A., Wisniewski, A. B., Novak, T. E., Gearhart, J. P., Migeon, C. J., & Lakshmanan, Y. (2008) · The Journal of Urology · doi:10.1016/j.juro.2008.06.043 · Cited by 10
“The androgen receptor gene contains 8 exons with 3 main functional domains, that is the amino-terminal transactivation domain, the DNAbinding domain and the steroid-binding domain.(15) The amino-terminal transactivation domain is encoded by exon 1, the largest exon, and is critical for target gene transcriptional regu…”
Characterization of intracellular aggregates using fluorescently-tagged polyglutamine-expanded androgen receptor
Panet-Raymond, V., Gottlieb, B., Beitel, L. K., Schipper, H. M., Timiansky, M., Pinsky, L., & Trifiro, M. A. (2001) · Neurotoxicity Research · doi:10.1007/bf03033265 · Cited by 10
Mutations in the Androgen Receptor
Trapman, J., & Brinkmann, A. O. (1993) · Annals of the New York Academy of Sciences · doi:10.1111/j.1749-6632.1993.tb32273.x · Cited by 10
Self-citation
Structure-Based Study to Overcome Cross-Reactivity of Novel Androgen Receptor Inhibitors
Radaeva, M., Li, H., Leblanc, E., Dalal, K., Ban, F., Ciesielski, F., Chow, B., Morin, H., Awrey, S. J., Singh, K., et al. (2022) · Cells · doi:10.3390/cells11182785 · Cited by 10
“The AR has a modular structure composed of an N-terminal domain (NTD), a highly conserved DNA-binding domain (DBD) and a C-terminal ligand-binding domain (LBD) [1].”
Interaction between AR signalling and CRKL bypasses casodex inhibition in prostate cancer
Reebye, V., Bevan, C. L., Nohadani, M., Hajitou, A., Habib, N. A., & Mintz, P. J. (2010) · Cellular Signalling · doi:10.1016/j.cellsig.2010.07.015 · Cited by 9
Functional Analysis of Novel Androgen Receptor Mutations in a Unique Cohort of Indonesian Patients with a Disorder of Sex Development
Elfferich, P., Juniarto, A. Z., Dubbink, H. J., van Royen, M. E., Molier, M., Hoogerbrugge, J. W., Houtsmuller, A. B., Trapman, J., Santosa, A., de Jong, F. H., et al. (2009) · Sexual Development · doi:10.1159/000252814 · Cited by 9
Self-citation
Nonsteroidal Tissue‐Selective Androgen Receptor Modulators
Mohler, M. L., Bohl, C. E., Narayanan, R., He, Y., Hwang, D., Dalton, J. T., & Miller, D. D. (2008) · Methods and principles in medicinal chemistry · doi:10.1002/9783527623297.ch8 · Cited by 9
Dynamics of coregulator-induced conformational perturbations in androgen receptor ligand binding domain
Zakharov, M. N., Pillai, B. K., Bhasin, S., Ulloor, J., Istomin, A. Y., Guo, C., Godzik, A., Kumar, P., & Jasuja, R. (2011) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2011.03.003 · Cited by 8
“…hormone receptor superfamily which modulates diverse biological functions by ligand-induced alterations in gene expression (Quigley et al., 1995; Jenster et al., 1991, 1992, 1997; Brinkmann et al., 1989, 1992; Tan et al., 1988; Simental et al., 1991; Georget et al., 1999; Matias et al., 2000;…”
Background
An androgen receptor mutation in the direct vicinity of the proposed C-terminal α-helix of the ligand binding domain containing the AF-2 transcriptional activating function core is associated with complete androgen insensitivity
Peters, I., Weidemann, W. M., Romalo, G., Knorr, D., Schweikert, H. U., & Spindler, K. (1999) · Molecular and Cellular Endocrinology · doi:10.1016/s0303-7207(98)00237-8 · Cited by 8
Synergistic effect of estramustine and [3′-keto-Bmtl]-[Val2]-cyclosporine (PSC 833) on the inhibition of androgen receptor phosphorylation in LNCaP cells
Wang, L. G., Liu, X. M., Budman, D. R., & Kreis, W. (1999) · Biochemical Pharmacology · doi:10.1016/s0006-2952(99)00210-5 · Cited by 8
Stromal androgen signaling governs essential niches in supporting prostate development and tumorigenesis
Rhee, J., Adzavon, Y. M., & Sun, Z. (2024) · Oncogene · doi:10.1038/s41388-024-03175-1 · Cited by 7
“Activation of the AR through the ligand-receptor interaction is essential in early prostate development, morphogenesis, growth, and regeneration [21].”
Targeting of Androgen Receptor Expression by Andro-miRs as Novel Adjunctive Therapeutics in Prostate Cancer
Ebron, J. S., Weyman, C. M., & Shukla, G. C. (2013) · Journal of Cancer Therapy · doi:10.4236/jct.2013.44a006 · Cited by 7
“Molecular binding of DHT to the LBD stimulates the transcriptional activity of the AR, which then regulates the expression of numerous androgen-responsive genes with myriad of cellular functions.”
BackgroundInfluential
An Amyloidogenic Sequence at the N-Terminus of the Androgen Receptor Impacts Polyglutamine Aggregation
Oppong, E. K., Stier, G., Gaal, M., Seeger, R., Stoeck, M., Delsuc, M., Cato, A. C. B., & Kieffer, B. (2017) · Biomolecules · doi:10.3390/biom7020044 · Cited by 7
“Notwithstanding its lack of a defined fold, several features of the transcriptional activity of AR are attributed to the NTD where several short peptide motifs are involved in the modulation of full-length AR transcriptional activity [5,6].”
Background
Involvement of the MEN1 Gene in Hormone-Related Cancers: Clues from Molecular Studies, Mouse Models, and Patient Investigations
Ziki, R. A., Luo, Y., Vlaeminck‐Guillem, V., Romancer, M. L., & Zhang, C. X. (2020) · Endocrines · doi:10.3390/endocrines1020007 · Cited by 7
“Abbreviations ADT Androgen deprivation therapies AP-1 Activator protein 1 AR Androgen receptor AREs Androgen response elements ASK Activator of S-phase kinase BAX BCL2 Associated X BC Breast cancer BRCA1&2 Breast cancers 1 and 2 CDK Cyclin-dependent kinase CRPC Castration-resistant prostate cancer DBD DNA-binding doma…”
BackgroundInfluential
A Multifunctional LNA Oligonucleotide-Based Strategy Blocks AR Expression and Transactivation Activity in PCa Cells
Castanotto, D., Zhang, X., Rüger, J., Alluin, J. V., Sharma, R., Pirrotte, P., Joenson, L., Ioannou, S., Nelson, M. S., Vikeså, J., et al. (2020) · Molecular Therapy — Nucleic Acids · doi:10.1016/j.omtn.2020.10.032 · Cited by 7
Cheminformatics Driven Development of Novel Therapies for Drug Resistant Prostate Cancer
Ban, F., Dalal, K., Leblanc, E., Morin, H., Rennie, P. S., & Cherkasov, A. R. (2018) · Molecular Informatics · doi:10.1002/minf.201800043 · Cited by 7
Substitution of Cys-560 by Phe, Trp, Tyr, and Ser in the first zinc finger of human androgen receptor affects hormonal sensitivity and transcriptional activation.
Warriar, N., Yu, C., Pagé, N., & Govindan, M. V. (1994) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(19)62007-7 · Cited by 7
A naturally occurring mutation in the human androgen receptor of a subject with complete androgen insensitivity confers binding and transactivation by estradiol
Bonagura, T. W., Deng, M., & Brown, T. R. (2006) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2006.08.012 · Cited by 7
The Effect of Liver Disease on the Endocrine System
Kruszynska, Y. T., & Bouloux, P. M. (2007) · Wiley eBooks · doi:10.1002/9780470691861.ch21b · Cited by 7
Reproductive and Nonreproductive Actions of Testosterone
Bhasin, S., & Jasuja, R. (2018) · Elsevier eBooks · doi:10.1016/b978-0-12-801238-3.65412-0 · Cited by 7
Transcriptional and epigenetic reprogramming, lineage plasticity and therapy resistance in prostate cancer
Shuai, Y., & Huang, H. (2025) · Journal of the National Cancer Center · doi:10.1016/j.jncc.2025.06.001 · Cited by 6
Synthesis, biological evaluation and X-ray analysis of bicalutamide sulfoxide analogues for the potential treatment of prostate cancer
Kandil, S., Kariuki, B. M., McGuigan, C., & Westwell, A. D. (2021) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2021.127817 · Cited by 6
Challenges of Endocrine Disruption and Cardiac Development
Diamante, G., & Schlenk, D. (2018) · Springer eBooks · doi:10.1007/978-3-319-75935-7_13 · Cited by 6
Trihydrophobin 1 attenuates androgen signal transduction through promoting androgen receptor degradation
Yang, Y., Zou, W., Kong, X., Wang, H., Zong, H., Jiang, J., Wang, Y., Hong, Y., Chi, Y., Xie, J., et al. (2010) · Journal of Cellular Biochemistry · doi:10.1002/jcb.22484 · Cited by 6
“…which is involved in AR nuclear translocation, and a ligand-binding domain (LBD), which is responsible for ligand binding and transactivation [Jenster et al., 1991; MacLean et al., 1997]. anzhong Yang and Weiying Zou contributed equally to this work. dditional Supporting Information may be…”
Background
Androgen Receptor Phosphorylation
Kuiper, G. G. J. M., de Ruiter, P. E., & Brinkmann, A. O. (1993) · Annals of the New York Academy of Sciences · doi:10.1111/j.1749-6632.1993.tb32292.x · Cited by 6
Self-citation
Design, synthesis and anti-tumor evaluation of novel thiohydantoin congeners as androgen receptor antagonists with in vivo study
Mohamed, N. M., Rabeeb, S. I. E., Deeb, M. A. E., Mahfoz, A. M., & Abdulrahman, F. G. (2024) · Journal of Molecular Structure · doi:10.1016/j.molstruc.2024.138565 · Cited by 5
The Expression Signature of Androgen Receptor Splice Variants and Their Distinctive Transcriptional Activities in Castration-Resistant Prostate Cancer
Plymate, S. R., & Luo, J. (2013) · Springer eBooks · doi:10.1007/978-1-4614-6182-1_13 · Cited by 5
Differential Gene Expression Profiles between N-Terminal Domain and Ligand-Binding Domain Inhibitors of Androgen Receptor Reveal Ralaniten Induction of Metallothionein by a Mechanism Dependent on MTF1
Obst, J. K., Mawji, N. R., Teskey, S. J. L., Wang, J., & Sadar, M. D. (2022) · Cancers · doi:10.3390/cancers14020386 · Cited by 5
“Unlike the AR-LBD, the N-terminal domain (NTD) is essential for transcriptional activities of both full-length AR and ARVs [14,15].”
Background
Discovery of novel biphenyl derivatives as androgen receptor degraders for the treatment of enzalutamide-resistant prostate cancer
Zhang, W., Fan, Y., Zhang, Y., Feng, Y., Luo, Y., Zhou, X., Chen, Z., Wang, C., Lu, T., Tang, F., et al. (2024) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2024.107433 · Cited by 6
Retracted : Genotyping of Tunisian azoospermic men with Sertoli cell-only and maturation arrest
Hadj-Kacem, L., Hadj-Kacem, H., Salem, I. H., Bahloul, A., Fakhfakh, F., & Ayadi, H. (2011) · Andrologia · doi:10.1111/j.1439-0272.2010.01088.x · Cited by 5
“Exon 1 encodes the transactivation domain in the aminoterminal part of the protein (Jenster et al.,1991), which contains a polymorphic CAG repeat [(CAG)n] (Chang et al., 1988).”
Background
Retracted
The Biological Role of Androgen Receptor in Prostate Cancer Progression
Takayama, K. (2018) · IntechOpen eBooks · doi:10.5772/intechopen.76360 · Cited by 5
“Generally, nuclear receptors including AR have multiple domains called DNA binding domain, a ligand-binding domain (LBD), and an N-terminal domain (NTD), [2, 8, 9].”
Background
Orexins and Prostate Cancer: State of the Art and Potential Experimental and Therapeutic Perspectives
Costagliola, A., Lombardi, R., Liguori, G., Morrione, A., & Giordano, A. (2023) · Cancer Genomics & Proteomics · doi:10.21873/cgp.20412 · Cited by 5
“The PSMA is highly expressed in many PCas, especially in CRPC (46, 47).”
Background
Androgen Receptor
Sutinen, P., Malinen, M., & Palvimo, J. J. (2017) · Endocrinology · doi:10.1007/978-3-319-44441-3_12 · Cited by 5
Drug-Discovery Pipeline for Novel Inhibitors of the Androgen Receptor
Dalal, K., Munuganti, R. S. N., Morin, H., Lallous, N., Rennie, P. S., & Cherkasov, A. R. (2016) · Methods in molecular biology · doi:10.1007/978-1-4939-3724-0_4 · Cited by 5
Deletion of the p16INK4a tumor suppressor and expression of the androgen receptor induce sarcomatoid carcinomas with signet ring cells in the mouse prostate
Lee, D.-H., Yu, E., Aldahl, J., Yang, J., He, Y., Hooker, E., Le, V. L., Mi, J., Olson, A. W., Wu, H., et al. (2019) · PLoS ONE · doi:10.1371/journal.pone.0211153 · Cited by 6
“Upon binding to a ligand, the AR dissociates from the HSPs and translocates into the nucleus, where it binds to the androgen responsive element (ARE), recruits cofactors [22], and activates its targeted gene expression, which in turn controls prostate development and tumorigenesis.”
Background

Authors: Jenster, G., van der Korput, H. A. G. M., van Vroonhoven, C., van der Kwast, T. H., Trapman, J., & Brinkmann, A. O.
Affiliations: Erasmus University Rotterdam (NL)
ORCID: Jenster, Guido
Venue: Molecular Endocrinology
Publisher: The Endocrine Society
Published: 1991-10
Volume: 5
Issue: 10
Pages: 1396-1404
ISSN: 0888-8809 (ISSN-L)
1944-9917
DOI: 10.1210/mend-5-10-1396
OpenAlex: W2002791165
Cited by: 523
References: 52
Citations by year: 2026: 6 · 2025: 9 · 2024: 13 · 2023: 4 · 2022: 8 · 2021: 9 · 2020: 12 · 2019: 11 · 2018: 15 · 2017: 16 · 2016: 18 · 2015: 12 · 2014: 14 · 2013: 17 · 2012: 18
FWCI: 25.65
Type: journal article
Language: en
Open access: bronze
doi.org
Locations: Molecular Endocrinology (publishedVersion)
PubMed (publishedVersion)
Funders: Nederlandse Organisatie voor Wetenschappelijk Onderzoek
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 › Endocrinology, Diabetes and Metabolism › Hormonal and reproductive studies
Keywords: androgen receptor, steroid-binding domain, transcriptional activation, subcellular localization, nuclear localization signal, nuclear targeting, hormone binding, constitutively active receptor, deletion mutants, DNA-binding domain, hinge region, post-translational modification
MeSH terms: Animals, Binding Sites, Cell Line, Chromosome Deletion, DNA-Binding Proteins, Genetic Vectors, HeLa Cells, Humans, Immunohistochemistry, Plasmids, Receptors, Androgen, Recombinant Proteins, Transcription, Genetic, Transfection, Restriction Mapping, Chloramphenicol O-Acetyltransferase, Metribolone

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Domains of the Human Androgen Receptor Involved in Steroid Binding, Transcriptional Activation, and Subcellular Localization

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