What does CREB bind to?
CREB-TF (CREB, cAMP response element-binding protein) is a cellular transcription factor. It binds to certain DNA sequences called cAMP response elements (CRE), thereby increasing or decreasing the transcription of the genes.
What does CREB code for?
CREBBP (CREB binding protein or CBP) encodes for a large ubiquitously expressed protein of the same name that performs multiple roles in transcriptional coactivation, including the acetylation of histone and nonhistone targets.
What does a Bromodomain do?
Bromodomain proteins are involved in a diverse range of functions, such as acetylating histones, remodeling chromatin, and recruiting other factors necessary for transcription. These proteins thus play a critical role in the regulation of transcription.
Is CREB a DNA binding protein?
The cAMP-response element binding protein (CREB) is localized in the nucleus and acts as a transcription factor, which binds to the cAMP response element (CRE) of the promoters of its target genes, upon phosphorylation at Ser133 by different receptor-activated protein kinases, such as protein kinase A (PKA), calmodulin …
What is the molecular function of CREB?
CREB is a transcription factor that regulates diverse cellular responses, including proliferation, survival, and differentiation. CREB is induced by a variety of growth factors and inflammatory signals and subsequently mediates the transcription of genes containing a cAMP-responsive element.
What is CBP in DNA?
CREB-binding protein (CBP) and its homologue p300 are transcriptional co-activators of various sequence-specific transcription factors that are involved in a wide array of cellular activities, such as DNA repair, cell growth, differentiation and apoptosis.
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.
Is lysine acetylated?
Once a protein is properly localized, acetylation of key lysine residues can occur enzymatically or spontaneously to influence its intermolecular interactions, enzymatic functions, localization, and eventual degradation. Post-translational acetylation of lysine residues will be the primary focus of the current review.
Is CREB a co activator?
Recent studies indicate that CREB functions in concert with a family of latent cytoplasmic co-activators called cAMP-regulated transcriptional co-activators (CRTCs), which are activated through dephosphorylation.
What kind of protein is CREB binding protein?
CREB-binding protein, also known as CREBBP or CBP, is a protein that in humans is encoded by the CREBBP gene.
How are bromodomains related to other protein families?
Bromodomains (BRDs) are evolutionarily conserved protein–protein interaction modules. Structure-based alignments have clustered human BRDs into eight distinct families. BRD modules share a conserved bundle of 4 α-helices (αZ, αA, αB and αC) that are linked to each other by loop segments of variable length (ZA and BC loops).
Are there any small molecule inhibitors for bromodomain?
Small-molecule inhibitors that target the bromodomain and extraterminal domain (BET) family of BRDs are now being tested in clinical trials for the treatment of various types of cancers.
Which is small molecule inhibitor binds to CBP / p300?
A small molecule inhibitor (I-CBP112) binding to the bromodomain domain of CBP/p300 has been developed for leukemia therapy. CREB-binding protein has been shown to interact with: