Searching across hundreds of databases
The androgen receptor (AR) is critical for the progression of prostate cancer to a castration-resistant (CRPC) state. AR antagonists are ineffective due to their inability to repress the expression of AR or its splice variant, AR-V7. Here, we report that the tyrosine kinase ACK1 (TNK2) phosphorylates histone H4 at tyrosine 88 upstream of the AR transcription start site. The WDR5/MLL2 complex reads the H4-Y88-phosphorylation marks and deposits the transcriptionally activating H3K4-trimethyl marks promoting AR transcription. Reversal of the pY88-H4 epigenetic marks by the ACK1 inhibitor (R)-9bMS-sensitized naive and enzalutamide-resistant prostate cancer cells and reduced AR and AR-V7 levels to mitigate CRPC tumor growth. Thus, a feedforward ACK1/pY88-H4/WDR5/MLL2/AR epigenetic circuit drives CRPC and is necessary for maintenance of the malignant state.
Pubmed ID: 28609657 RIS Download
Publication data is provided by the National Library of Medicine ® and PubMed ®. Data is retrieved from PubMed ® on a weekly schedule. For terms and conditions see the National Library of Medicine Terms and Conditions.
Software package for interpreting gene expression data. Used for interpretation of a large-scale experiment by identifying pathways and processes.
View all literature mentionsThis polyclonal targets IgG (H+L)
View all literature mentionsThis monoclonal targets MLL2
View all literature mentionsThis monoclonal targets Anti-Androgen Receptor
View all literature mentionsThis monoclonal targets RNA pol II
View all literature mentionsThis polyclonal targets Histone H3K4me3
View all literature mentionsThis polyclonal targets WDR5
View all literature mentionsThis monoclonal targets FLAG
View all literature mentionsThis monoclonal targets HA-Tag
View all literature mentionsThis polyclonal secondary targets IgG (H+L)
View all literature mentionsThis polyclonal secondary targets IgG (H+L)
View all literature mentionsThis unknown targets Rabbit IgG
View all literature mentionsThis monoclonal targets Histone H4
View all literature mentionsThis monoclonal targets Histone H3
View all literature mentionsThis monoclonal targets Histone H2B
View all literature mentionsThis monoclonal targets Hist3h2a
View all literature mentionsThis polyclonal targets Human IgG antibody
View all literature mentionsThis unknown targets Histone H4
View all literature mentionsThis monoclonal targets slightly modified β-cytoplasmic actin N-terminal peptide, Ac-Asp-Asp-Asp-Ile-Ala-Ala-Leu-Val-Ile-Asp-Asn-Gly-Ser-Gly-Lys, conjugated to KLH
View all literature mentionsThis unknown targets Human ACK1, phospho (Tyr284)
View all literature mentionsThis monoclonal targets p-Tyr (PY20)
View all literature mentionsThis monoclonal targets ACK (A-11)
View all literature mentionsThis monoclonal targets Histone H3, dimethyl (Lys4)
View all literature mentionsThis monoclonal targets Androgen receptor variant 7
View all literature mentionsThis polyclonal targets Androgen Receptor
View all literature mentionsThis monoclonal targets Androgen Receptor (D6F11) XP Rabbit mAb
View all literature mentionsMus musculus with name Crl:NU-Foxn1nu from IMSR.
View all literature mentionsMus musculus with name CB17/Icr-Prkdcscid/IcrIcoCrl from IMSR.
View all literature mentionsCell line RWPE-1 is a Transformed cell line with a species of origin Homo sapiens
View all literature mentionsCell line DU145 is a Cancer cell line with a species of origin Homo sapiens (Human)
View all literature mentionsCell line PC-3 is a Cancer cell line with a species of origin Homo sapiens (Human)
View all literature mentionsCell line VCaP is a Cancer cell line with a species of origin Homo sapiens (Human)
View all literature mentionsCell line LNCaP clone FGC is a Cancer cell line with a species of origin Homo sapiens (Human)
View all literature mentionsSoftware for single-cell flow cytometry analysis. Its functions include management, display, manipulation, analysis and publication of the data stream produced by flow and mass cytometers.
View all literature mentionsThe SciCrunch Infrastructure was developed as a cooperative data platform to be used by diverse communities in making data more FAIR.
scicrunch.org
