|
| Status |
Public on Jan 22, 2020 |
| Title |
Selective Inhibition of the Second Bromodomain of BET Family Maintains Anti-Tumor Efficacy and Improves Tolerability |
| Organism |
Homo sapiens |
| Experiment type |
Genome binding/occupancy profiling by high throughput sequencing
|
| Summary |
Here we report the discovery of ABBV-744, a first in class, highly potent and selective inhibitor of BET family BD2 domains with drug like properties. ChIP-seq analysis revealed that ABBV-744 displaced BRD4 from AR-containing super enhancers and elicited potent inhibition of AR-dependent transcription without causing broad transcription alterations associated with exposure to pan BET inhibitors.
|
| |
|
| Overall design |
BRD4 ChIP-Seq under four different treatment conditions in two cell lines. H3K27Ac ChIP-Seq from two cell lines, vehicle treatment only. AR ChIP-Seq in one cell line (LNCaP) with three treatment conditions. BRD4 and AR ChIP-Seq were all spike-in controlled.
|
| |
|
| Contributor(s) |
Faivre E, Plotnik J |
| Citation(s) |
31969702 |
| |
| Submission date |
Aug 07, 2018 |
| Last update date |
Feb 19, 2020 |
| Contact name |
Josh Plotnik |
| E-mail(s) |
[email protected]
|
| Organization name |
AbbVie Inc.
|
| Street address |
1 North Waukegan Rd, AP10/210A
|
| City |
North Chicago |
| State/province |
IL |
| ZIP/Postal code |
60064 |
| Country |
USA |
| |
|
| Platforms (1) |
| GPL18573 |
Illumina NextSeq 500 (Homo sapiens) |
|
| Samples (14)
|
|
| Relations |
| BioProject |
PRJNA484953 |
| SRA |
SRP156578 |
Less...
More...