GEO Logo
   NCBI > GEO > Accession DisplayHelp Not logged in | LoginHelp
GEO help: Mouse over screen elements for information.
Series GSE96084 Query DataSets for GSE96084
Status Public on Feb 16, 2018
Title Bypassing drug-resistance mechanisms of prostate cancer with small-molecules that target androgen receptor chromatin interactions
Organism Homo sapiens
Experiment type Genome binding/occupancy profiling by high throughput sequencing
Summary Human androgen receptor (AR) is a hormone-activated transcription factor that is an important drug-target in the treatment of prostate cancer. Current small molecule AR-antagonists (such as Enzalutamide) compete with male hormones that bind to the steroid binding pocket of the AR ligand binding domain (LBD). In castration-resistant prostate cancer (CRPC), drug-resistance can manifest through AR-LBD mutations that convert AR-antagonists into agonists, or by expression of AR-variants lacking the LBD. Such treatment resistance underscores the importance of novel ways of targeting the AR. In this study, we tested whether VPC14449, a small molecule inhibitor that was rationally designed to selectively target the AR DNA binding domain (DBD), could directly interfere with AR-DNA interactions. Using ChIP-seq in cell line models expressing AR or AR variants, we found that genome-wide chromatin binding of AR was dramatically impacted by VPC14449 (although with lesser effect on AR variants).
Overall design AR and AR variant ChIP-seq in R1-AD1 and R1-D567 prostate cancer cells with VPC14449 treatment
Contributor(s) Yang R, Che M, Dehm SM
Citation(s) 28775145
Submission date Mar 10, 2017
Last update date May 15, 2019
Contact name Scott M Dehm
Organization name University of Minnesota
Department Masonic Cancer center
Lab Dr Dehm M. Scott
Street address 8806 420 Delaware
City Minneapolis
State/province MN
ZIP/Postal code 55414
Country USA
Platforms (1)
GPL11154 Illumina HiSeq 2000 (Homo sapiens)
Samples (7)
GSM2532933 R1-AD1 ChIP-Seq_AR_VPCDHT
BioProject PRJNA378776
SRA SRP101727

Download family Format
SOFT formatted family file(s) SOFTHelp
MINiML formatted family file(s) MINiMLHelp
Series Matrix File(s) TXTHelp

Supplementary file Size Download File type/resource
GSE96084_RAW.tar 110.0 Kb (http)(custom) TAR (of NARROWPEAK)
SRA Run SelectorHelp
Raw data are available in SRA
Processed data provided as supplementary file

| NLM | NIH | GEO Help | Disclaimer | Accessibility |
NCBI Home NCBI Search NCBI SiteMap