Structure of the GCN5 histone acetyltransferase bound to a bisubstrate inhibitor.

PubWeight™: 1.22‹?› | Rank: Top 10%

🔗 View Article (PMC 137837)

Published in Proc Natl Acad Sci U S A on October 21, 2002

Authors

Arienne N Poux1, Marek Cebrat, Cheol M Kim, Philip A Cole, Ronen Marmorstein

Author Affiliations

1: The Wistar Institute, and Department of Chemistry, University of Pennsylvania, Philadelphia, PA 19104, USA.

Articles citing this

Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. Chem Biol (2010) 3.38

Chemical probes for histone-modifying enzymes. Nat Chem Biol (2008) 3.30

Molecular basis for age-dependent microtubule acetylation by tubulin acetyltransferase. Cell (2014) 1.79

Histone acetyltransferase activity of p300 is required for transcriptional repression by the promyelocytic leukemia zinc finger protein. Mol Cell Biol (2005) 1.52

Sirtuin 1 (SIRT1) deacetylase activity is not required for mitochondrial biogenesis or peroxisome proliferator-activated receptor-gamma coactivator-1alpha (PGC-1alpha) deacetylation following endurance exercise. J Biol Chem (2011) 1.47

Writers and readers of histone acetylation: structure, mechanism, and inhibition. Cold Spring Harb Perspect Biol (2014) 1.12

Crystal structure of RimI from Salmonella typhimurium LT2, the GNAT responsible for N(alpha)-acetylation of ribosomal protein S18. Protein Sci (2008) 1.11

Protein lysine acetylation by p300/CBP. Chem Rev (2015) 1.02

Histone acetyltransferases and histone deacetylases in B- and T-cell development, physiology and malignancy. Genes Cancer (2015) 0.95

Mechanistic and structural analysis of human spermidine/spermine N1-acetyltransferase. Biochemistry (2007) 0.93

Characterization, localization, essentiality, and high-resolution crystal structure of glucosamine 6-phosphate N-acetyltransferase from Trypanosoma brucei. Eukaryot Cell (2011) 0.92

Structure and mechanism of non-histone protein acetyltransferase enzymes. FEBS J (2013) 0.90

A random sequential mechanism of aminoglycoside acetylation by Mycobacterium tuberculosis Eis protein. PLoS One (2014) 0.89

Structural basis for substrate specificity and catalysis of human histone acetyltransferase 1. Proc Natl Acad Sci U S A (2012) 0.88

Processing mechanism and substrate selectivity of the core NuA4 histone acetyltransferase complex. Biochemistry (2011) 0.86

Metabolic Regulation of Histone Acetyltransferases by Endogenous Acyl-CoA Cofactors. Chem Biol (2015) 0.80

Structure of the complex of Neisseria gonorrhoeae N-acetyl-L-glutamate synthase with a bound bisubstrate analog. Biochem Biophys Res Commun (2012) 0.80

Involvement of Hat1p (Kat1p) catalytic activity and subcellular localization in telomeric silencing. J Biol Chem (2008) 0.78

PCAF regulates the stability of the transcriptional regulator and cyclin-dependent kinase inhibitor p27 Kip1. Nucleic Acids Res (2012) 0.78

Structure and Functional Diversity of GCN5-Related N-Acetyltransferases (GNAT). Int J Mol Sci (2016) 0.77

Probing the reaction coordinate of the p300/CBP histone acetyltransferase with bisubstrate analogs. Bioorg Chem (2010) 0.77

Regulation of a Protein Acetyltransferase in Myxococcus xanthus by the Coenzyme NADP. J Bacteriol (2015) 0.75

Structural basis for acyl-group discrimination by human Gcn5L2. Acta Crystallogr D Struct Biol (2016) 0.75

Structural Basis of Eco1-Mediated Cohesin Acetylation. Sci Rep (2017) 0.75

Generating enzyme and radical-mediated bisubstrates as tools for investigating Gcn5-related N-acetyltransferases. FEBS Lett (2017) 0.75

Articles cited by this

Crystallography & NMR system: A new software suite for macromolecular structure determination. Acta Crystallogr D Biol Crystallogr (1998) 169.28

Improved methods for building protein models in electron density maps and the location of errors in these models. Acta Crystallogr A (1991) 119.63

The language of covalent histone modifications. Nature (2000) 44.92

Acetylation of histones and transcription-related factors. Microbiol Mol Biol Rev (2000) 9.36

Histone deacetylases and cancer: causes and therapies. Nat Rev Cancer (2001) 9.12

Implementation of molecular replacement in AMoRe. Acta Crystallogr D Biol Crystallogr (2001) 8.92

Histone modifications in transcriptional regulation. Curr Opin Genet Dev (2002) 8.10

Structures of a histone deacetylase homologue bound to the TSA and SAHA inhibitors. Nature (1999) 7.47

Epigenetic codes for heterochromatin formation and silencing: rounding up the usual suspects. Cell (2002) 6.25

Expanded lysine acetylation specificity of Gcn5 in native complexes. J Biol Chem (1999) 2.91

Critical residues for histone acetylation by Gcn5, functioning in Ada and SAGA complexes, are also required for transcriptional function in vivo. Genes Dev (1998) 2.76

HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol Cell (2000) 2.68

Structure of Tetrahymena GCN5 bound to coenzyme A and a histone H3 peptide. Nature (1999) 2.50

Role of the Ada2 and Ada3 transcriptional coactivators in histone acetylation. J Biol Chem (2001) 2.50

DNA damage-dependent acetylation of p73 dictates the selective activation of apoptotic target genes. Mol Cell (2002) 2.29

Catalytic mechanism and function of invariant glutamic acid 173 from the histone acetyltransferase GCN5 transcriptional coactivator. J Biol Chem (1999) 2.13

Histone acetylation and disease. Cell Mol Life Sci (2001) 2.11

Structure of the histone acetyltransferase Hat1: a paradigm for the GCN5-related N-acetyltransferase superfamily. Cell (1998) 1.96

Crystal structure of yeast Esa1 suggests a unified mechanism for catalysis and substrate binding by histone acetyltransferases. Mol Cell (2000) 1.80

Transcriptional coactivator protein p300. Kinetic characterization of its histone acetyltransferase activity. J Biol Chem (2001) 1.77

Kinetic mechanism of the histone acetyltransferase GCN5 from yeast. J Biol Chem (2000) 1.62

Crystal structure of the histone acetyltransferase domain of the human PCAF transcriptional regulator bound to coenzyme A. EMBO J (1999) 1.39

p300/CBP-associated factor histone acetyltransferase processing of a peptide substrate. Kinetic analysis of the catalytic mechanism. J Biol Chem (2000) 1.38

CBP/p300 and muscle differentiation: no HAT, no muscle. EMBO J (2001) 1.30

X-ray crystallographic studies of serotonin N-acetyltransferase catalysis and inhibition. J Mol Biol (2002) 1.09

Mechanism-based inhibition of the melatonin rhythm enzyme: pharmacologic exploitation of active site functional plasticity. Proc Natl Acad Sci U S A (1999) 0.92

Articles by these authors

Histone demethylation mediated by the nuclear amine oxidase homolog LSD1. Cell (2004) 21.30

An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor. Cell (2006) 10.28

Acetylation of the p53 DNA-binding domain regulates apoptosis induction. Mol Cell (2006) 5.40

Regulation of histone acetylation in the nucleus by sphingosine-1-phosphate. Science (2009) 4.45

Human Proteinpedia enables sharing of human protein data. Nat Biotechnol (2008) 4.21

Regulation of the p300 HAT domain via a novel activation loop. Nat Struct Mol Biol (2004) 3.70

Butyrate greatly enhances derivation of human induced pluripotent stem cells by promoting epigenetic remodeling and the expression of pluripotency-associated genes. Stem Cells (2010) 3.53

A Src-like inactive conformation in the abl tyrosine kinase domain. PLoS Biol (2006) 3.40

Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. Chem Biol (2010) 3.38

Acetylation of tau inhibits its degradation and contributes to tauopathy. Neuron (2010) 3.15

The structural basis of protein acetylation by the p300/CBP transcriptional coactivator. Nature (2008) 2.83

Mechanism of activation and inhibition of the HER4/ErbB4 kinase. Structure (2008) 2.79

Inhibition of the EGF receptor by binding of MIG6 to an activating kinase domain interface. Nature (2007) 2.78

The catalytic mechanism of the ESA1 histone acetyltransferase involves a self-acetylated intermediate. Nat Struct Biol (2002) 2.56

Phosphoproteomic analysis of Her2/neu signaling and inhibition. Proc Natl Acad Sci U S A (2006) 2.30

DNA damage-dependent acetylation of p73 dictates the selective activation of apoptotic target genes. Mol Cell (2002) 2.29

Glucose and weight control in mice with a designed ghrelin O-acyltransferase inhibitor. Science (2010) 2.12

Chemical rescue of a mutant enzyme in living cells. Science (2006) 1.95

Fungal Rtt109 histone acetyltransferase is an unexpected structural homolog of metazoan p300/CBP. Nat Struct Mol Biol (2008) 1.89

A tight junction-associated Merlin-angiomotin complex mediates Merlin's regulation of mitogenic signaling and tumor suppressive functions. Cancer Cell (2011) 1.86

Structural basis for nicotinamide inhibition and base exchange in Sir2 enzymes. Mol Cell (2007) 1.77

Structural basis for ubiquitin recognition by the Otu1 ovarian tumor domain protein. J Biol Chem (2008) 1.75

Structure and chemistry of the p300/CBP and Rtt109 histone acetyltransferases: implications for histone acetyltransferase evolution and function. Curr Opin Struct Biol (2008) 1.72

Chromatin "prepattern" and histone modifiers in a fate choice for liver and pancreas. Science (2011) 1.70

Crystal structure of the retinoblastoma tumor suppressor protein bound to E2F and the molecular basis of its regulation. Proc Natl Acad Sci U S A (2003) 1.68

Structural basis for the recognition of c-Src by its inactivator Csk. Cell (2008) 1.66

A role for cofactor-cofactor and cofactor-histone interactions in targeting p300, SWI/SNF and Mediator for transcription. EMBO J (2003) 1.65

Structure of the human Papillomavirus E7 oncoprotein and its mechanism for inactivation of the retinoblastoma tumor suppressor. J Biol Chem (2005) 1.61

Structure of the p53 core domain dimer bound to DNA. J Biol Chem (2006) 1.60

Construction of human activity-based phosphorylation networks. Mol Syst Biol (2013) 1.59

The chemical biology of protein phosphorylation. Annu Rev Biochem (2009) 1.59

Structure and autoregulation of the yeast Hst2 homolog of Sir2. Nat Struct Biol (2003) 1.59

Structural basis of histone demethylation by LSD1 revealed by suicide inactivation. Nat Struct Mol Biol (2007) 1.59

Structure of a human ASF1a-HIRA complex and insights into specificity of histone chaperone complex assembly. Nat Struct Mol Biol (2006) 1.58

Regulation of c-Src nonreceptor tyrosine kinase activity by bengamide A through inhibition of methionine aminopeptidases. Chem Biol (2007) 1.58

Oncogenesis by sequestration of CBP/p300 in transcriptionally inactive hyperacetylated chromatin domains. EMBO J (2010) 1.58

Structure of the yeast Hst2 protein deacetylase in ternary complex with 2'-O-acetyl ADP ribose and histone peptide. Structure (2003) 1.55

Structural basis for DNA recognition by FoxO1 and its regulation by posttranslational modification. Structure (2008) 1.55

Down-regulation of p300/CBP histone acetyltransferase activates a senescence checkpoint in human melanocytes. Cancer Res (2002) 1.53

Histone acetyltransferase activity of p300 is required for transcriptional repression by the promyelocytic leukemia zinc finger protein. Mol Cell Biol (2005) 1.52

LSD1 and the chemistry of histone demethylation. Curr Opin Chem Biol (2007) 1.52

Reading and function of a histone code involved in targeting corepressor complexes for repression. Mol Cell Biol (2005) 1.52

Maintenance of low histone ubiquitylation by Ubp10 correlates with telomere-proximal Sir2 association and gene silencing. Mol Cell (2005) 1.51

Structure of the retinoblastoma protein bound to adenovirus E1A reveals the molecular basis for viral oncoprotein inactivation of a tumor suppressor. Genes Dev (2007) 1.49

The leukemogenicity of AML1-ETO is dependent on site-specific lysine acetylation. Science (2011) 1.49

Structural basis for histone and phosphohistone binding by the GCN5 histone acetyltransferase. Mol Cell (2003) 1.47

Structural basis for nicotinamide cleavage and ADP-ribose transfer by NAD(+)-dependent Sir2 histone/protein deacetylases. Proc Natl Acad Sci U S A (2004) 1.45

Structure and function of the SWIRM domain, a conserved protein module found in chromatin regulatory complexes. Proc Natl Acad Sci U S A (2006) 1.44

Structural basis for the inhibition of the LSD1 histone demethylase by the antidepressant trans-2-phenylcyclopropylamine. Biochemistry (2007) 1.44

A mechanism-based inactivator for histone demethylase LSD1. J Am Chem Soc (2006) 1.43

Concurrent MEK2 mutation and BRAF amplification confer resistance to BRAF and MEK inhibitors in melanoma. Cell Rep (2013) 1.43

Acetylation of Tat defines a cyclinT1-independent step in HIV transactivation. Mol Cell (2003) 1.42

Acetylation of RNA polymerase II regulates growth-factor-induced gene transcription in mammalian cells. Mol Cell (2013) 1.40

Structure and mechanism of lysine-specific demethylase enzymes. J Biol Chem (2007) 1.40

Inhibition of the acetyltransferases p300 and CBP reveals a targetable function for p300 in the survival and invasion pathways of prostate cancer cell lines. Mol Cancer Ther (2011) 1.39

TRRAP and GCN5 are used by c-Myc to activate RNA polymerase III transcription. Proc Natl Acad Sci U S A (2007) 1.39

Electrophilic tuning of the chemoprotective natural product sulforaphane. Proc Natl Acad Sci U S A (2010) 1.37

Human immunodeficiency virus type 1 Tat protein inhibits the SIRT1 deacetylase and induces T cell hyperactivation. Cell Host Microbe (2008) 1.35

The role of C-terminal tyrosine phosphorylation in the regulation of SHP-1 explored via expressed protein ligation. J Biol Chem (2002) 1.34

Structure and substrate binding properties of cobB, a Sir2 homolog protein deacetylase from Escherichia coli. J Mol Biol (2004) 1.31

Csk, a critical link of g protein signals to actin cytoskeletal reorganization. Dev Cell (2002) 1.30

Dynamic acetylation of all lysine-4 trimethylated histone H3 is evolutionarily conserved and mediated by p300/CBP. Proc Natl Acad Sci U S A (2011) 1.30

Comparative analysis of small molecules and histone substrate analogues as LSD1 lysine demethylase inhibitors. J Am Chem Soc (2010) 1.29

MYST protein acetyltransferase activity requires active site lysine autoacetylation. EMBO J (2011) 1.29

Structure of Vps75 and implications for histone chaperone function. Proc Natl Acad Sci U S A (2008) 1.27

14-3-3 interaction with histone H3 involves a dual modification pattern of phosphoacetylation. Mol Cell Biol (2008) 1.27

Kinetic and mass spectrometric analysis of p300 histone acetyltransferase domain autoacetylation. J Biol Chem (2006) 1.26

Structural basis for sirtuin function: what we know and what we don't. Biochim Biophys Acta (2009) 1.26

p300/CBP-associated factor drives DEK into interchromatin granule clusters. J Biol Chem (2005) 1.24

Structure and activity of enzymes that remove histone modifications. Curr Opin Struct Biol (2005) 1.24

Development of small-molecule inhibitors of the group I p21-activated kinases, emerging therapeutic targets in cancer. Biochem Pharmacol (2010) 1.24

Regulation of CK2 by phosphorylation and O-GlcNAcylation revealed by semisynthesis. Nat Chem Biol (2012) 1.24

MicroRNA-224 is up-regulated in hepatocellular carcinoma through epigenetic mechanisms. FASEB J (2012) 1.24

Human UBN1 is an ortholog of yeast Hpc2p and has an essential role in the HIRA/ASF1a chromatin-remodeling pathway in senescent cells. Mol Cell Biol (2008) 1.23

Targeting large kinase active site with rigid, bulky octahedral ruthenium complexes. J Am Chem Soc (2008) 1.21

Mechanistic insights into the activation of oncogenic forms of EGF receptor. Nat Struct Mol Biol (2011) 1.21

Investigation of the roles of catalytic residues in serotonin N-acetyltransferase. J Biol Chem (2002) 1.20

Mechanistic analysis of a suicide inactivator of histone demethylase LSD1. Biochemistry (2007) 1.20

Cellular stability of serotonin N-acetyltransferase conferred by phosphonodifluoromethylene alanine (Pfa) substitution for Ser-205. J Biol Chem (2005) 1.17

Development of Neh2-luciferase reporter and its application for high throughput screening and real-time monitoring of Nrf2 activators. Chem Biol (2011) 1.16

Structural basis for dimerization in DNA recognition by Gal4. Structure (2008) 1.16

Molecular basis for N-terminal acetylation by the heterodimeric NatA complex. Nat Struct Mol Biol (2013) 1.16

In vitro enzymatic characterization of near full length EGFR in activated and inhibited states. Biochemistry (2009) 1.16

Site-specific introduction of an acetyl-lysine mimic into peptides and proteins by cysteine alkylation. J Am Chem Soc (2010) 1.15

Structure of a Sir2 substrate, Alba, reveals a mechanism for deacetylation-induced enhancement of DNA binding. J Biol Chem (2003) 1.14

Acetylation of nucleosomal histones by p300 facilitates transcription from tax-responsive human T-cell leukemia virus type 1 chromatin template. Mol Cell Biol (2002) 1.14

The role of the phospho-CDK2/cyclin A recruitment site in substrate recognition. J Biol Chem (2006) 1.14

Synthesis and evaluation of a potent and selective cell-permeable p300 histone acetyltransferase inhibitor. J Am Chem Soc (2005) 1.14

Biochemical analysis of MST1 kinase: elucidation of a C-terminal regulatory region. Biochemistry (2008) 1.14

Nuclear export modulates the cytoplasmic Sir2 homologue Hst2. EMBO Rep (2006) 1.12

Crystal structure and functional interpretation of the erythrocyte spectrin tetramerization domain complex. Blood (2010) 1.11