Transcriptional activation and nuclear targeting signals of the human androgen receptor.

Simental, J A; Sar, M; Lane, M V; French, F S; Wilson, E M

doi:10.1016/s0021-9258(18)52466-2

Cited by 631Estrogen and related hormone effectsProstate Cancer Treatment and ResearchHormonal and reproductive studies

Transcriptional activation and nuclear targeting signals of the human androgen receptor.

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Simental, J A, Sar, M, Lane, M V, French, F S, Wilson, E M·1991·Journal of Biological Chemistry

DOI 10.1016/s0021-9258(18)52466-2

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Abstract

The androgen receptor (AR) is a signal-transducing protein required for sexual differentiation, development, and expression of the male phenotype. A series of human AR deletion mutants were created either by site-directed mutagenesis using restriction enzyme digestion, the polymerase chain reaction, or, for a series of unidirectional NH2-terminal deletions, exonuclease III digestion. Receptor mutants were expressed in monkey kidney COS cells as truncated AR proteins between 20 and 107 kDa as revealed on immunoblots, where wild type AR was a doublet of 114 and 108 kDa. Subcellular localization by immunocytochemical staining demonstrated androgen-dependent nuclear uptake of AR from a perinuclear region of the cytoplasm. A nuclear targeting signal similar in sequence and position to the glucocorticoid receptor and homologous to the SV40 large T antigen was required for androgen-induced nuclear uptake of wild type AR. AR mutants lacking the NH2-terminal and/or steroid binding domains were constitutively nuclear with reduced transcriptional activity. Transcriptional activation by wild type AR was androgen-dependent in cotransfection studies of CV1 cells using the chloramphenicol acetyltransferase reporter gene linked to the mouse mammary tumor virus promoter. Deletion mutagenesis revealed within the NH2-terminal region a domain required for full transcriptional activity and within the steroid binding domain, an inhibitory function, deletion of which yielded a constitutively active receptor. Inhibition of wild type AR by coexpression with an inactive NH2-terminal fragment suggested competition for nuclear factors required for transcriptional regulation. These studies demonstrate a concerted interplay among the domains of the AR protein in regulating gene transcription.

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Testosterone has been shown to induce its effects through binding to intracellular androgen receptors (ARs), which then regulate gene transcription.
“Testosterone has been shown to induce its effects through binding to intracellular androgen receptors (ARs) (34), which then regulate gene transcription (18, 81).”
From Sex-Based Differences in Skeletal Muscle Kinetics and Fiber-Type Composition (2015) · cites this paper as [81]

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Authors: Simental, J. A., Sar, M., Lane, M. V., French, F. S., & Wilson, E. M.
Affiliations: University of North Carolina at Chapel Hill (US)
ORCID: Lane, M V
Venue: Journal of Biological Chemistry
Publisher: Elsevier BV
Published: 1991-01
Volume: 266
Issue: 1
Pages: 510-518
ISSN: 0021-9258 (ISSN-L)
DOI: 10.1016/s0021-9258(18)52466-2
OpenAlex: W1495912963
Cited by: 631
References: 72
Citations by year: 2026: 2 · 2025: 10 · 2024: 7 · 2023: 9 · 2022: 8 · 2021: 8 · 2020: 13 · 2019: 7 · 2018: 12 · 2017: 17 · 2016: 17 · 2015: 14 · 2014: 8 · 2013: 16 · 2012: 16
FWCI: 16.90
Type: journal article
Language: en
Open access: hybrid
doi.org
Licence: cc-by
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
creativecommons.org/licenses/by/4.0/ (vor, 10876 d)
Locations: Journal of Biological Chemistry (publishedVersion, cc-by)
PubMed (publishedVersion)
Carolina Digital Repository (University of North Carolina at Chapel Hill) (submittedVersion)
UNC Libraries
Funders: National Institutes of Health (5p30hd018968-12, 5r01ns017479-11)
National Institute of Neurological Disorders and Stroke (NS-17479)
National Institute of Child Health and Human Development
Eunice Kennedy Shriver National Institute of Child Health and Human Development (P-30 HD18968, HD-16910)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Prostate Cancer Treatment and Research
Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Hormonal and reproductive studies
Keywords: androgen receptor, transcriptional activation, nuclear localization signal, nuclear translocation, steroid-binding domain, constitutively active receptor, transcriptional regulation
MeSH terms: Amino Acid Sequence, Animals, Cell Line, Cell Nucleus, Chromosome Deletion, Humans, Immunohistochemistry, Molecular Sequence Data, Plasmids, Receptors, Androgen, Transcription, Genetic, Transfection, Signal Transduction, Polymerase Chain Reaction, Mutagenesis, Site-Directed

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Transcriptional activation and nuclear targeting signals of the human androgen receptor.

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