Coregulator control of androgen receptor action by a novel nuclear receptor-binding motif
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The androgen receptor (AR) is a ligand-activated transcription factor that is essential for prostate cancer development. It is activated by androgens through its ligand-binding domain (LBD), which consists predominantly of 11 α-helices. Upon ligand binding, the last helix is reorganized to an agonist conformation termed activator function-2 (AF-2) for coactivator binding. Several coactivators bind to the AF-2 pocket through conserved LXXLL or FXXLF sequences to enhance the activity of the receptor. Recently, a small compound-binding surface adjacent to AF-2 has been identified as an allosteric modulator of the AF-2 activity and is termed binding function-3 (BF-3). However, the role of BF-3 in vivo is currently unknown, and little is understood about what proteins can bind to it. Here we demonstrate that a duplicated GARRPR motif at the N terminus of the cochaperone Bag-1L functions through the BF-3 pocket. These findings are supported by the fact that a selective BF-3 inhibitor or mutations within the BF-3 pocket abolish the interaction between the GARRPR motif(s) and the BF-3. Conversely, amino acid exchanges in the two GARRPR motifs of Bag-1L can impair the interaction between Bag-1L and AR without altering the ability of Bag-1L to bind to chromatin. Furthermore, the mutant Bag-1L increases androgen-dependent activation of a subset of AR targets in a genome-wide transcriptome analysis, demonstrating a repressive function of the GARRPR/BF-3 interaction. We have therefore identified GARRPR as a novel BF-3 regulatory sequence important for fine-tuning the activity of the AR.
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Bag-1L regulates AR through the BF3 surface.
“Indeed, the long isoform of the cochaperone BCL2-associated athanogene (Bag-1L) was recently demonstrated to regulate AR through the BF3 surface and further studies are needed to understand how regulation by Bag-1L is related, if at all, to FKBP52/β-catenin co-regulation [31].”
From The FKBP52 Cochaperone Acts in Synergy with β-Catenin to Potentiate Androgen Receptor Signaling (2015) · cites this paper as [31]
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- Authors
- Jehle, K., Cato, L., Neeb, A., Muhle-Goll, C., Jung, N., Smith, E. W., Buzon, V., Carbó, L. R., Estébanez-Perpiñá, E., Schmitz, K., Fruk, L., Luy, B., Chen, Y., Cox, M. B., Bräse, S., Brown, M., & Cato, A. C. B.
- Affiliations
- Karlsruhe Institute of Technology (DE)
- Harvard University (US)
- University of South Florida (US)
- Institut de Biomedicina de la Universitat de Barcelona (ES)
- Technische Universität Darmstadt (DE)
- The University of Texas at El Paso (US)
- Corresponding author
- Cato, Andrew C.B.
- ORCID
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 2014-03
- Volume
- 289
- Issue
- 13
- Pages
- 8839-8851
- ISSN
- 0021-9258 (ISSN-L)
- PMC
- PMC3979403
- OpenAlex
- W2093418017
- Cited by
- 53
- References
- 75
- Citations by year
- 2026: 2 · 2025: 2 · 2024: 2 · 2023: 2 · 2022: 7 · 2021: 4 · 2019: 7 · 2018: 4 · 2017: 4 · 2016: 8 · 2015: 7 · 2014: 4
- FWCI
- 6.41
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- Journal of Biological Chemistry (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Dipòsit Digital de la Universitat de Barcelona (Universitat de Barcelona) (acceptedVersion)
- scholarworks - UTEP (The University of Texas at El Paso) (submittedVersion)
- RECERCAT (Consorci de Serveis Universitaris de Catalunya) (submittedVersion, public-domain)
- TUbilio (Technical University of Darmstadt) (submittedVersion)
- RECERCAT (Consorci de Serveis Universitaris de Catalunya) (submittedVersion)
- Funders
- National Institutes of Health (5 G12 RR008124, 8 G12 MD007592, 1P01CA163227–01A1, P50CA090381)
- Topics
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Prostate Cancer Treatment and Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chromatin Remodeling and Cancer
- Keywords
- androgen receptor, ligand-binding domain, coactivator binding, transcriptional co-regulation, allosteric modulation, prostate cancer, chromatin binding, transcriptional repression
- MeSH terms
- Allosteric Regulation, Amino Acid Sequence, Cell Line, DNA-Binding Proteins, Humans, Mutation, Oligopeptides, Protein Binding, Receptors, Androgen, Transcription Factors, Transcriptional Activation, Protein Structure, Tertiary, Repetitive Sequences, Amino Acid, Amino Acid Motifs
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