Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

KAT2B (Q92831) - Overview - Molecular Target Synopsis

Protein


KAT2B, Histone acetyltransferase KAT2B
Enzyme Classification 2.3.1.48
UniProt Q92831

Also Known as KAT2B_HUMAN, KAT2B, PCAF

Functions as a histone acetyltransferase (HAT) to promote transcriptional activation. Has significant histone acetyltransferase activity with core histones (H3 and H4), and also with nucleosome core particles. Also acetylates non-histone proteins, such as ACLY, PLK4 and TBX5. Inhibits cell-cycle progression and counteracts the mitogenic activity of the adenoviral oncoprotein E1A. Acts as a circadian transcriptional coactivator which enhances the activity of the circadian transcriptional activators: NPAS2-ARNTL/BMAL1 and CLOCK-ARNTL/BMAL1 heterodimers. Involved in heart and limb development by mediating acetylation of TBX5, acetylation regulating nucleocytoplasmic shuttling of TBX5 (PubMed:29174768). Acts as a negative regulator of centrosome amplification by mediating acetylation of PLK4 (PubMed:27796307). Also acetylates spermidine (PubMed:27389534)., (Microbial infection) In case of HIV-1 infection, it is recruited by the viral protein Tat. Regulates Tat's transactivating activity and may help inducing chromatin remodeling of proviral genes. Interacts with SIRT1. Interacts (unsumoylated form) with NR2C1; the interaction promotes transactivation activity (By similarity). Interacts with EP300, CREBBP and DDX17. Interacts with NCOA1 and NCOA3. Component of a large chromatin remodeling complex, at least composed of MYSM1, KAT2B/PCAF, RBM10 and KIF11/TRIP5. Interacts with NR2C2 (hypophosphorylated and unsumoylated form); the interaction promotes the transactivation activity of NR2C2. Interacts with KLF1; the interaction does not acetylate KLF1 and there is no enhancement of its transactivational activity. Interacts with NFE4. Interacts with MECOM. Interacts with E2F1; the interaction acetylates E2F1 augmenting its DNA-binding and transcriptional activity. Interacts with NPAS2, ARNTL/BMAL1 and CLOCK. Interacts with BCAS3. Interacts with CEBPB (PubMed:17301242). Interacts with NR4A3 (By similarity). Interacts with NFATC2 (By similarity). Interacts with TBX5 (PubMed:29174768). Interacts with PLK4 (PubMed:27796307).

6J3O
CRYSTAL STRUCTURE OF THE HUMAN PCAF BROMODOMAIN IN COMPLEX WITH COMPOUND 12
RCSB/PDB
Inspect Structure
See all 3D Structures for KAT2B

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
832ENSG00000114166ENST00000263754ENSP00000263754Q92831-1

Sub-cellular localization


UniProt: KAT2B is active in the following subcellular-locations: centrosome, cytoplasm, cytoskeleton, microtubule organizing center, nucleus.
GO terms: KAT2B is active in the following subcellular-locations: A band, actomyosin, Ada2/Gcn5/Ada3 transcription activator complex, centrosome, I band, kinetochore, nucleoplasm, nucleus, PCAF complex, protein-containing complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project KAT2B has gain in 3 cell-lines, loss in 4 cell-lines and no signal in 998 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: M14, MDA_N, MDA_MB_435

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HT-144, MeWo, DEOC-1

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: NHLF, MCF-7, SK-N-SH

(see details)

3D Structures


For KAT2B there are:
25 structures (45 chains) solved
20 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


KAT2B has been screened with 484 compounds (624 bioactivities), 8 compounds have bioactivities that show binding affinity of <= 500nM (13 bioactivities). (see details)