What does JQ1 do?

JQ1 is a bromodomain inhibitor, which selectively binds to the amino-terminal twin bromodomains of BET proteins10. JQ1 treatment displaces BRD4, inhibiting its ability to read acetylated lysine residues11.

Is JQ1 reversible?

JQ1 treatment produces a reversible contraceptive effect by targeting the activity of BRDT in mouse male germ cells, validating BRDT as a male contraceptive target.

How do BET inhibitors work?

BET inhibitors are a class of drugs that reversibly bind the bromodomains of Bromodomain and Extra-Terminal motif (BET) proteins BRD2, BRD3, BRD4, and BRDT, and prevent protein-protein interaction between BET proteins and acetylated histones and transcription factors.

What do bet proteins do?

BET proteins can recruit transcription factors in distant areas from the promoter of genes involved in different cellular processes. BET proteins, which are epigenetic regulators of gene transcription, are strongly implicated in the regulation of cell growth, differentiation, and inflammation (Figure 3).

Is BRD4 a transcription factor?

BRD4 plays an important role in transcription, both as a passive scaffold via its recruitment of vital transcription factors and as an active kinase that phosphorylates RNA polymerase II, directly and indirectly regulating transcription.

What is a Bromodomain protein BRD4?

Bromodomain-containing protein 4 (BRD4) is an epigenetic reader that recognizes histone proteins and acts as a transcriptional regulator to trigger tumor growth and the inflammatory response. The pan-bromodomain and extra-terminal domain (BET) inhibitor, (+)-JQ1 (1), was reported to inhibit angiogenesis.

What bet means?

Bet is a slang term of affirmation, agreement, or approval along the lines of “Cool!” or “I’m down!” It can also suggest doubt or disbelief: “Yeah, sure.”

Where is BRD4?

Gene expression profiles showed that BRD4 is expressed in a broad range of somatic cells. As well, ChIP seq data showed that BRD4 occupies many ENHs and promoters also in non-cancer cells and generally contributes to gene expression (Table 1) [6].

What does Sksksksks mean?

“Sksksksk” is a phrase that’s mostly typed, sort of like mashing your keyboard as an exclamation. It can stand in for laughter, or express awkwardness, or be the same as an “OMG.” It’s sort of like saying “I can’t even” if it were still 2013. As far as keyboard mashes go, it’s a good one.

Is BRD4 a protein?

Bromodomain-containing protein 4 is a protein that in humans is encoded by the BRD4 gene. BRD4, similar to other BET family members, contains two bromodomains that recognize acetylated lysine residues. …

What kind of protein is JQ1 an inhibitor of?

From Wikipedia, the free encyclopedia JQ1 is a thienotriazolodiazepine and a potent inhibitor of the BET family of bromodomain proteins which include BRD2, BRD3, BRD4, and the testis-specific protein BRDT in mammals.

How did the BET inhibitor JQ1 get its name?

It was developed by the James Bradner laboratory at Brigham and Women’s Hospital and named after chemist Jun Qi. The chemical structure was inspired by patent of similar BET inhibitors by Mitsubishi Tanabe Pharma [WO/2009/084693]. Structurally it is related to benzodiazepines.

Why is JQ1 not used in human clinical trials?

While widely used in laboratory applications, JQ1 is not itself being used in human clinical trials because it has a short half life. Interest in JQ1 as a cancer therapeutic stemmed from its ability to inhibit BRD4 and BRD3, both of which form fusion oncogenes that drive NUT midline carcinoma.

How is JQ1 related to benzodiazepines and BET?

The chemical structure was inspired by patent of similar BET inhibitors by Mitsubishi Tanabe Pharma [WO/2009/084693]. Structurally it is related to benzodiazepines. While widely used in laboratory applications, JQ1 is not itself being used in human clinical trials because it has a short half life.