Property Summary

NCBI Gene PubMed Count 76
PubMed Score 258.21
PubTator Score 146.99

Knowledge Summary

Patent

No data available

TINX Plot

Expression

  Differential Expression (4)

Disease log2 FC p
oligodendroglioma 1.400 6.4e-03
psoriasis 1.100 6.8e-04
pancreatic ductal adenocarcinoma liver m... 1.244 8.3e-03
lung adenocarcinoma 1.600 1.7e-09

Protein-protein Interaction (4)

MLP Assay (3)

AID Type Active / Inconclusive / Inactive Description
504327 confirmatory 817 / 10134 / 376634 qHTS Assay for Inhibitors of GCN5L2
504398 summary 0 / 0 / 0 qHTS Assay for Inhibitors of GCN5L2: Summary
588347 confirmatory 96 / 49 / 0 qHTS Assay for Inhibitors of GCN5L2: Hit confirmation

Gene RIF (60)

PMID Text
27022023 Methionine was the only essential amino acid that rapidly induced PGC-1alpha acetylation through activating the GCN5 acetyltransferase.
27005833 Data uncover GCN5 as a negative regulator of C/EBPalpha and demonstrate the importance of C/EBPalpha acetylation in myeloid differentiation.
26637399 GCN5 plays a positive role in human colon cancer development, and its suppression holds a great therapeutic potential in antitumor therapy
26546801 Acetyltransferase p300 collaborates with chromodomain helicase DNA-binding protein 4 (CHD4) to facilitate DNA double-strand break repair
26468280 results thus demonstrate that the catalytic activity of GCN5 is stimulated by subunits of the ADA2a- or ADA2b-containing HAT modules and is further increased by incorporation of the distinct HAT modules in the ATAC or SAGA holo-complexes
26420353 these results may point to the GCN5-NF-kappaB pathway as a novel potential molecular target for stem cell mediated regenerative medicine and the treatment of metabolic bone diseases such as osteoporosis.
26378521 GCN5 Potentiates Glioma Proliferation and Invasion via STAT3 and AKT Signaling Pathways
26256950 Suggest lysine acetyltransfer as a potential regulator of platelet actin dynamics, and potential roles for lysine acetylation in the molecular coordination of platelet activation and function.
25770212 DDIT3 and KAT2A cooperatively up-regulate TNFRSF10A and TNFRSF10B.
25707573 The antifibrotic effects of SIRT1 in systemic sclerosis were due in part to decreased expression and function of the acetyltransferase p300.
25686500 HBXIP promotes the migration of breast cancer cells through modulating microtubule acetylation mediated by GCN5.
25426559 our results represent the first work demonstrating that GCN5 and PCAF exhibit different functions and antagonistically regulate the XBP-1S-mediated transcription.
25269644 Gcn5 and PCAF repress IFN-beta production in an enzymatic activity-independent and non-transcriptional manner: by inhibiting the innate immune signaling kinase TBK1 in the cytoplasm.
25111486 Genetic studies indicate that Gcn5 and USP22 have important roles during development, which may presage important functions for these proteins in human diseases. [review]
24705139 Purified GCN5 binds to an N-terminal sub-domain of MYC TAD.
24480624 P300 acetyltransferase is a molecular determinant of androge receptor degradation.
24302725 PR acetylation at Lys-183 by p300 potentiates PR activity through accelerated binding of its direct target genes without affecting PR tethering on other transcription factors.
23913178 These results demonstrate that GCN5, through its acetyltransferase activity, inhibits PGC1alpha-induced enhancement of hepatitis B virus transcription and replication both in vitro and in vivo.
23863879 The K19A, K41Q, and K51A mutations decrease HIV-1 Tat binding to hGCN5, whereas the K50Q and K50R mutations increase the binding
23826228 The K19A, K41Q, and K51A mutations decrease HIV-1 Tat binding to hGCN5, whereas the K50Q and K50R mutations increase the binding
23661605 Expression of PCAF was upregulated in PCa cells through suppression of miR-17. Phenethyl isothiocyanate treatment significantly decreased PCAF expression and promoted transcription of miR-17 in LNCaP cells.
23543735 GCN5 has a role in potentiating growth of non-small cell lung cancer by promoting E2F1, cyclin D1, and cyclin E1 expression
23437046 These data provide a first look at quantitating the specificity and selectivity of multiple lysines on a single substrate (histone H3) by Gcn5.
23033487 GCN5 takes part in transcription regulation of POLH gene through alterations in the chromatin structure by direct interaction with its 5'-flanking region, and protects vertebrate cells against UV-induced DNA damage via controlling POLH gene expression.
22623781 GCN5 as a new negative regulator of transactivation by E1A and suggest that its KAT activity is required for optimal virus replication.
22574209 acetylation mechanism by GCN5
22465951 H1.4K34 acetylation is mediated by GCN5 and is preferentially enriched at promoters of active genes, where it stimulates transcription by increasing H1 mobility and recruiting a general transcription factor.
22086303 Genetic variants in KAT2A does not contribute to the development of Lynch syndrome.
22055187 Human HAT complexes, sharing the same catalytic GCN5 or PCAF subunit are targeted to different genomic loci representing functionally distinct regulatory elements.
21725360 Data show that And-1 forms a complex with both histone H3 and Gcn5.
21367571 GCN5 differentially affects expression of multiple genes; ethanol-induced histone H3-lysine 9 acetylation is mediated via GCN5, and GCN5 is involved in ethanol-induced expression of the putative choline transporter SLC44A2.
21131905 Deletion of GCN5/PCAF in cells specifically and dramatically reduces acetylation on histone H3K9.
20937768 Data show that Pygo2 associates with MLL2 histone methyltransferase and STAGA histone acetyltransferase to facilitate their interaction with beta-catenin and Wnt1-induced, TCF/LEF-dependent transactivation in breast cancer cells.
20227660 The K19A, K41Q, and K51A mutations decrease HIV-1 Tat binding to hGCN5, whereas the K50Q and K50R mutations increase the binding
20226045 In this study the authors demonstrate that another cellular histone acetyltransferase, GCN5, acetylates HIV-1 integrase leading to enhanced 3'-end processing and strand transfer activities.
20226045 The K19A, K41Q, and K51A mutations decrease HIV-1 Tat binding to hGCN5, whereas the K50Q and K50R mutations increase the binding
20138641 The K19A, K41Q, and K51A mutations decrease HIV-1 Tat binding to hGCN5, whereas the K50Q and K50R mutations increase the binding
19716452 The K19A, K41Q, and K51A mutations decrease HIV-1 Tat binding to hGCN5, whereas the K50Q and K50R mutations increase the binding
19683498 Gcn5 regulates TRF1 levels through effects on Usp22 activity and SAGA integrity.
19491097 PGC-1beta is a substrate for general control of amino-acid synthesis (GCN5) and is acetylated on at least 10 lysine residues that are distributed along multiple domains of the protein.
19343071 GCN5 specifically acetylates CDC6 at three lysine residues flanking its cyclin-docking motif, and this modification is crucial for the subsequent phosphorylation of the protein by Cyclin A-CDKs at a specific residue close to the acetylation site.
19339690 GCN5, a histone acetyltransferase, associates with COMMD1 and other components of the ligase, promotes RelA ubiquitination, and represses kappaB-dependent transcription
19124466 Knockdown of p300 reduces acetylation of Atg5, Atg7, Atg8, and Atg12, although overexpressed p300 increases the acetylation of these same proteins.
18936164 ADA2a and ADA2b, two human homologues of yeast Ada2, each have the ability to form a heterotrimer with ADA3 and GCN5L but that only the ADA2b homologue is found in STAGA.
18842595 p300 acts as a critical coactivator of FXR induction of SHP by acetylating histones at the promoter and FXR itself
18838386 ATAC Is a GCN5/PCAF-containing acetylase complex with a novel NC2-like histone fold module that interacts with the TATA-binding protein
18418385 GCN5L acetyltransferase stably associates with Mediator together with the TRRAP polypeptide.
18250157 GCN5 regulates CDK9 function by specifically acetylating the catalytic core of the enzyme especially a Lys needed for ATP coordination & the phosphotransfer reaction.
18187620 The K19A, K41Q, and K51A mutations decrease HIV-1 Tat binding to hGCN5, whereas the K50Q and K50R mutations increase the binding
18187620 Knockdown of K(lysine) acetyltransferase 2A (KAT2A; GCN5L2) by siRNA inhibits HIV-1 replication in HeLa-derived TZM-bl cells
17967894 suggest a novel STAF65gamma-dependent function of STAGA-type complexes in cell proliferation and transcription activation by MYC postloading of TFIID and RNA polymerase II that involves direct recruitment of core Mediator
17301242 PCAF/GCN5-dependent acetylation of C/EBPbeta serves as an important molecular switch in determining the transcriptional regulatory potential of this transcription factor.
15715965 GCN5 preferentially controls cell cycle-related genes, as well as apoptosis-related genes
14767476 All human TACC family proteins can bind in vitro to GCN5L2.
14657027 The K19A, K41Q, and K51A mutations decrease HIV-1 Tat binding to hGCN5, whereas the K50Q and K50R mutations increase the binding
12660246 requirement in transcription activation via c-myc transformation domain
12391296 crystal structure of the GCN5 HAT bound to a peptide-CoA conjugate containing CoA covalently attached through an isopropionyl linker to Lys-14 of a 20-aa N-terminal fragment of histone H3
12154097 The K19A, K41Q, and K51A mutations decrease HIV-1 Tat binding to hGCN5, whereas the K50Q and K50R mutations increase the binding
11956210 The K19A, K41Q, and K51A mutations decrease HIV-1 Tat binding to hGCN5, whereas the K50Q and K50R mutations increase the binding
11384967 The K19A, K41Q, and K51A mutations decrease HIV-1 Tat binding to hGCN5, whereas the K50Q and K50R mutations increase the binding

AA Sequence

MAEPSQAPTPAPAAQPRPLQSPAPAPTPTPAPSPASAPIPTPTPAPAPAPAAAPAGSTGTGGPGVGSGGA      1 - 70
GSGGDPARPGLSQQQRASQRKAQVRGLPRAKKLEKLGVFSACKANETCKCNGWKNPKPPTAPRMDLQQPA     71 - 140
ANLSELCRSCEHPLADHVSHLENVSEDEINRLLGMVVDVENLFMSVHKEEDTDTKQVYFYLFKLLRKCIL    141 - 210
QMTRPVVEGSLGSPPFEKPNIEQGVLNFVQYKFSHLAPRERQTMFELSKMFLLCLNYWKLETPAQFRQRS    211 - 280
QAEDVATYKVNYTRWLCYCHVPQSCDSLPRYETTHVFGRSLLRSIFTVTRRQLLEKFRVEKDKLVPEKRT    281 - 350
LILTHFPKFLSMLEEEIYGANSPIWESGFTMPPSEGTQLVPRPASVSAAVVPSTPIFSPSMGGGSNSSLS    351 - 420
LDSAGAEPMPGEKRTLPENLTLEDAKRLRVMGDIPMELVNEVMLTITDPAAMLGPETSLLSANAARDETA    421 - 490
RLEERRGIIEFHVIGNSLTPKANRRVLLWLVGLQNVFSHQLPRMPKEYIARLVFDPKHKTLALIKDGRVI    491 - 560
GGICFRMFPTQGFTEIVFCAVTSNEQVKGYGTHLMNHLKEYHIKHNILYFLTYADEYAIGYFKKQGFSKD    561 - 630
IKVPKSRYLGYIKDYEGATLMECELNPRIPYTELSHIIKKQKEIIKKLIERKQAQIRKVYPGLSCFKEGV    631 - 700
RQIPVESVPGIRETGWKPLGKEKGKELKDPDQLYTTLKNLLAQIKSHPSAWPFMEPVKKSEAPDYYEVIR    701 - 770
FPIDLKTMTERLRSRYYVTRKLFVADLQRVIANCREYNPPDSEYCRCASALEKFFYFKLKEGGLIDK       771 - 837
//

Text Mined References (81)

PMID Year Title
27022023 2016 The Methionine Transamination Pathway Controls Hepatic Glucose Metabolism through Regulation of the GCN5 Acetyltransferase and the PGC-1? Transcriptional Coactivator.
27005833 2016 Acetylation of C/EBP? inhibits its granulopoietic function.
26637399 2015 The Histone Acetyltransferase GCN5 Expression Is Elevated and Regulated by c-Myc and E2F1 Transcription Factors in Human Colon Cancer.
26546801 2016 Acetyltransferase p300 collaborates with chromodomain helicase DNA-binding protein 4 (CHD4) to facilitate DNA double-strand break repair.
26468280 2015 Subunits of ADA-two-A-containing (ATAC) or Spt-Ada-Gcn5-acetyltrasferase (SAGA) Coactivator Complexes Enhance the Acetyltransferase Activity of GCN5.
26420353 2016 Histone Acetyltransferase GCN5 Regulates Osteogenic Differentiation of Mesenchymal Stem Cells by Inhibiting NF-?B.
26378521 2015 GCN5 Potentiates Glioma Proliferation and Invasion via STAT3 and AKT Signaling Pathways.
26256950 2015 Lysine acetyltransfer supports platelet function.
25770212 2015 DDIT3 and KAT2A Proteins Regulate TNFRSF10A and TNFRSF10B Expression in Endoplasmic Reticulum Stress-mediated Apoptosis in Human Lung Cancer Cells.
25707573 2015 The Histone Deacetylase Sirtuin 1 Is Reduced in Systemic Sclerosis and Abrogates Fibrotic Responses by Targeting Transforming Growth Factor ? Signaling.
25686500 2015 The oncoprotein HBXIP promotes migration of breast cancer cells via GCN5-mediated microtubule acetylation.
25426559 2015 GCN5 inhibits XBP-1S-mediated transcription by antagonizing PCAF action.
25269644 2014 Gcn5 and PCAF negatively regulate interferon-? production through HAT-independent inhibition of TBK1.
25111486 2014 Functions of SAGA in development and disease.
24912190 2014 Genome-wide RNAi screen identifies the Parkinson disease GWAS risk locus SREBF1 as a regulator of mitophagy.
24705139 2014 MYC interacts with the human STAGA coactivator complex via multivalent contacts with the GCN5 and TRRAP subunits.
24480624 2014 p300 acetyltransferase regulates androgen receptor degradation and PTEN-deficient prostate tumorigenesis.
24302725 2014 Acetylation at lysine 183 of progesterone receptor by p300 accelerates DNA binding kinetics and transactivation of direct target genes.
23913178 2013 GCN5 acetyltransferase inhibits PGC1?-induced hepatitis B virus biosynthesis.
23661605 2013 Phenethyl isothiocyanate inhibits androgen receptor-regulated transcriptional activity in prostate cancer cells through suppressing PCAF.
23543735 2013 Lysine acetyltransferase GCN5 potentiates the growth of non-small cell lung cancer via promotion of E2F1, cyclin D1, and cyclin E1 expression.
23437046 2013 Quantitating the specificity and selectivity of Gcn5-mediated acetylation of histone H3.
23033487 2012 GCN5 protects vertebrate cells against UV-irradiation via controlling gene expression of DNA polymerase ?.
22814378 2012 N-terminal acetylome analyses and functional insights of the N-terminal acetyltransferase NatB.
22664934 2012 Comparison of tear protein levels in breast cancer patients and healthy controls using a de novo proteomic approach.
22623781 2012 Cellular GCN5 is a novel regulator of human adenovirus E1A-conserved region 3 transactivation.
22574209 2012 Investigation of the acetylation mechanism by GCN5 histone acetyltransferase.
22465951 2012 A dual role of linker histone H1.4 Lys 34 acetylation in transcriptional activation.
22464331 2012 Histone recognition and large-scale structural analysis of the human bromodomain family.
22086303 2012 Mutation and association analyses of the candidate genes ESR1, ESR2, MAX, PCNA, and KAT2A in patients with unexplained MSH2-deficient tumors.
22055187 2011 SAGA and ATAC histone acetyl transferase complexes regulate distinct sets of genes and ATAC defines a class of p300-independent enhancers.
21725360 2012 And-1 is required for the stability of histone acetyltransferase Gcn5.
21367571 2011 Knock down of GCN5 histone acetyltransferase by siRNA decreases ethanol-induced histone acetylation and affects differential expression of genes in human hepatoma cells.
21131905 2011 Distinct roles of GCN5/PCAF-mediated H3K9ac and CBP/p300-mediated H3K18/27ac in nuclear receptor transactivation.
20937768 2010 Pygo2 associates with MLL2 histone methyltransferase and GCN5 histone acetyltransferase complexes to augment Wnt target gene expression and breast cancer stem-like cell expansion.
20562830 2010 The ATAC acetyl transferase complex controls mitotic progression by targeting non-histone substrates.
20226045 2010 GCN5-dependent acetylation of HIV-1 integrase enhances viral integration.
19683498 2009 Gcn5 and SAGA regulate shelterin protein turnover and telomere maintenance.
19491097 2009 GCN5-mediated transcriptional control of the metabolic coactivator PGC-1beta through lysine acetylation.
19343071 2009 Acetylation by GCN5 regulates CDC6 phosphorylation in the S phase of the cell cycle.
19339690 2009 GCN5 is a required cofactor for a ubiquitin ligase that targets NF-kappaB/RelA.
19124466 2009 Regulation of autophagy by the p300 acetyltransferase.
19103755 2009 The double-histone-acetyltransferase complex ATAC is essential for mammalian development.
18936164 2009 The STAGA subunit ADA2b is an important regulator of human GCN5 catalysis.
18842595 2008 The p300 acetylase is critical for ligand-activated farnesoid X receptor (FXR) induction of SHP.
18838386 2008 Human ATAC Is a GCN5/PCAF-containing acetylase complex with a novel NC2-like histone fold module that interacts with the TATA-binding protein.
18418385 2008 Cooperative activity of cdk8 and GCN5L within Mediator directs tandem phosphoacetylation of histone H3.
18250157 2008 Acetylation of conserved lysines in the catalytic core of cyclin-dependent kinase 9 inhibits kinase activity and regulates transcription.
18206972 2008 A TFTC/STAGA module mediates histone H2A and H2B deubiquitination, coactivates nuclear receptors, and counteracts heterochromatin silencing.
17967894 2008 STAGA recruits Mediator to the MYC oncoprotein to stimulate transcription and cell proliferation.
17664281 2007 Cyclic AMP-stimulated interaction between steroidogenic factor 1 and diacylglycerol kinase theta facilitates induction of CYP17.
17410582 2007 Crystal structure of a binary complex between human GCN5 histone acetyltransferase domain and acetyl coenzyme A.
17301242 2007 Glucocorticoid-stimulated preadipocyte differentiation is mediated through acetylation of C/EBPbeta by GCN5.
15715965 2005 GCN5: a supervisor in all-inclusive control of vertebrate cell cycle progression through transcription regulation of various cell cycle-related genes.
15592455 2005 Immunoaffinity profiling of tyrosine phosphorylation in cancer cells.
15489334 2004 The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).
14767476 2004 The transforming acidic coiled coil proteins interact with nuclear histone acetyltransferases.
14657027 2003 Regulation of HIV-1 gene expression by histone acetylation and factor recruitment at the LTR promoter.
12887892 2003 Sir2 regulates skeletal muscle differentiation as a potential sensor of the redox state.
12660246 2003 c-Myc transformation domain recruits the human STAGA complex and requires TRRAP and GCN5 acetylase activity for transcription activation.
12477932 2002 Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.
12391296 2002 Structure of the GCN5 histone acetyltransferase bound to a bisubstrate inhibitor.
12374802 2002 Acetylation of interferon regulatory factor-7 by p300/CREB-binding protein (CBP)-associated factor (PCAF) impairs its DNA binding.
12154097 2002 Tat-controlled protein acetylation.
11564863 2001 Human STAGA complex is a chromatin-acetylating transcription coactivator that interacts with pre-mRNA splicing and DNA damage-binding factors in vivo.
11438666 2001 The TFIID components human TAF(II)140 and Drosophila BIP2 (TAF(II)155) are novel metazoan homologues of yeast TAF(II)47 containing a histone fold and a PHD finger.
11406595 2001 UV-damaged DNA-binding protein in the TFTC complex links DNA damage recognition to nucleosome acetylation.
11384967 2001 The histone acetyltransferase, hGCN5, interacts with and acetylates the HIV transactivator, Tat.
11090279 2000 Solution structure and acetyl-lysine binding activity of the GCN5 bromodomain.
10747963 2000 Functional interaction between the mouse notch1 intracellular region and histone acetyltransferases PCAF and GCN5.
10611234 2000 The essential cofactor TRRAP recruits the histone acetyltransferase hGCN5 to c-Myc.
10373431 1999 Identification of TATA-binding protein-free TAFII-containing complex subunits suggests a role in nucleosome acetylation and signal transduction.
9742083 1998 Mammalian GCN5 and P/CAF acetyltransferases have homologous amino-terminal domains important for recognition of nucleosomal substrates.
9722949 1998 Identification and mapping of human histone acetylation modifier gene homologues.
9611240 1998 Cloning of Drosophila GCN5: conserved features among metazoan GCN5 family members.
9488450 1998 Repression of GCN5 histone acetyltransferase activity via bromodomain-mediated binding and phosphorylation by the Ku-DNA-dependent protein kinase complex.
9073520 1997 The human transcriptional adaptor genes TADA2L and GCN5L2 colocalize to chromosome 17q12-q21 and display a similar tissue expression pattern.
8972232 1997 Histone acetyltransferase activity is conserved between yeast and human GCN5 and is required for complementation of growth and transcriptional activation.
8684459 1996 A p300/CBP-associated factor that competes with the adenoviral oncoprotein E1A.
8552087 1996 Identification of human proteins functionally conserved with the yeast putative adaptors ADA2 and GCN5.
7670491 1995 Gene-based sequence-tagged-sites (STSs) as the basis for a human gene map.