Selective BET-domain inhibitors

What function do bromodomains have? 

• They are epigenetic erasers

• They are epigenetic writers

• They are epigenetic readers

• They are epigenetic scholars

Answer explanation

Bromodomains are approximately 110 amino acid protein domains recognized as readers of acetylated lysine residues.

Activation of the BD2 domain of the bromodomain family results in ?

• Anti-proliferation activity

• Transcriptional repression

• Recruitment of transcription factors

• Tumor suppression

Answer explanation

activation TURNs ON transcription.

by first recruitment of transcription factors so that RNA polymerase can transcribe the genes.

Which assays were utilized to help visualize the ABBV-744 compound and investigate DNA and protein interactions?

• Immunoblot and ChIP 

• ELISA and Western Blot 

• TR-FRET and SDS PAGE

• TR-FRET and ChIP 

Why is ABBV-744 a prefered inhibitor when compared to ABBV-075?

• higher gene expression changes  and lower impact on global transcription 

• lower gene expression changes  and lower impact on global transcription 

• higher gene expression changes  and higher impact on global transcription 

• lower gene expression changes  and higher impact on global transcription 

Answer explanation

highly selective for BD2 domain which led to it's lower change to off-target gene down regulations and over all lower effect on global transcription

Which one of the following methodology does the authors utilize for studying the efficacy and adverse effects of ABBV-744?

• Used human cell lines on mice xenograft model

• Used mice cell lines on mice xenograft model

• Used human cell lines on rat xenograft model

• Used human cell lines on rat xenograft model

Answer explanation

Efficacy was studied using Human cell lines on mice

Toxicity was studied using human cell lines on rats