ArticleCellular and molecular life sciences : CMLS2010
A 629RKLKK633 motif in the hinge region controls the androgen receptor at multiple levels.
Article in Cellular and molecular life sciences : CMLS, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 49 citations in OpenAlex.
- Targeting androgen receptor stability and degradation: approaches for developing a therapy for spinal and bulbar muscular atrophy.Cell communication and signaling : CCS · 2025Review
- RNA fine-tunes estrogen receptor-alpha binding on low-affinity DNA motifs for transcriptional regulation.The EMBO journal · 2024Article
- Study of novel androgen receptor V770 variant in androgen insensitivity syndrome patients reveals the transitional state of the androgen receptor ligand binding domain homodimer.Protein science : a publication of the Protein Society · 2023Article
- The T850D Phosphomimetic Mutation in the Androgen Receptor Ligand Binding Domain Enhances Recruitment at Activation Function 2.International journal of molecular sciences · 2022Article
- Molecular Mechanisms and Therapeutics for SBMA/Kennedy's Disease.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2019Review
- Comparing the rules of engagement of androgen and glucocorticoid receptors.Cellular and molecular life sciences : CMLS · 2017Review
- Polyglutamine androgen receptor-mediated neuromuscular disease.Cellular and molecular life sciences : CMLS · 2016Review
- Intracellular kinetics of the androgen receptor shown by multimodal Image Correlation Spectroscopy (mICS).Scientific reports · 2016Article
- Insights into Chemoresistance of Prostate Cancer.International journal of biological sciences · 2015Review
- Emerging mechanisms of enzalutamide resistance in prostate cancer.Nature reviews. Urology · 2014Article
- N-terminal targeting of androgen receptor variant enhances response of castration resistant prostate cancer to taxane chemotherapy.Molecular oncology · 2014Article
- Minireview: The versatile roles of lysine deacetylases in steroid receptor signaling.Molecular endocrinology (Baltimore, Md.) · 2014Review
- Androgen receptor splice variants determine taxane sensitivity in prostate cancer.Cancer research · 2014Article
- Androgen receptor as a driver of therapeutic resistance in advanced prostate cancer.International journal of biological sciences · 2014Article
- Constitutive activity of the androgen receptor.Advances in pharmacology (San Diego, Calif.) · 2014Review
- Allosteric conversation in the androgen receptor ligand-binding domain surfaces.Molecular endocrinology (Baltimore, Md.) · 2012Article
- Androgen receptor splice variants activate androgen receptor target genes and support aberrant prostate cancer cell growth independent of canonical androgen receptor nuclear localization signal.The Journal of biological chemistry · 2012Article
- Allosteric modulators of steroid hormone receptors: structural dynamics and gene regulation.Endocrine reviews · 2012Review
- Structural and functional analysis of domains of the progesterone receptor.Molecular and cellular endocrinology · 2012Review
- General molecular biology and architecture of nuclear receptors.Current topics in medicinal chemistry · 2012Review
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Authors and funding
11 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The androgen receptor protein has specific domains involved in DNA binding, ligand binding, and transactivation, whose activities need to be integrated during transcription activation. The hinge region, more particular a (629)RKLKK(633) motif, seems to play a crucial role in this process. Indeed, although the motif is not part of the DNA-binding domain, its positive residues are involved in optimal DNA binding and nuclear translocation as shown by mutation analysis. When the mutated ARs are forced into the nucleus, however, the residues seem to play different roles in transactivation. Moreover, we show by FRAP analysis that during activation, the AR is distributed in the nucleus in a mobile and two immobile fractions, and that mutations in the (629)RKLKK(633) motif affect the distribution of the AR over these three intranuclear fractions. Taken together, the (629)RKLKK(633) motif is a multifunctional motif that integrates nuclear localization, receptor stability, DNA binding, transactivation potential and intranuclear mobility.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.