Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor.

PubWeight™: 3.38‹?› | Rank: Top 1%

🔗 View Article (PMC 2884008)

Published in Chem Biol on May 28, 2010

Authors

Erin M Bowers1, Gai Yan, Chandrani Mukherjee, Andrew Orry, Ling Wang, Marc A Holbert, Nicholas T Crump, Catherine A Hazzalin, Glen Liszczak, Hua Yuan, Cecilia Larocca, S Adrian Saldanha, Ruben Abagyan, Yan Sun, David J Meyers, Ronen Marmorstein, Louis C Mahadevan, Rhoda M Alani, Philip A Cole

Author Affiliations

1: Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, MD 21205, USA.

Articles citing this

(truncated to the top 100)

Epigenetic protein families: a new frontier for drug discovery. Nat Rev Drug Discov (2012) 6.70

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

Bromodomains as therapeutic targets. Expert Rev Mol Med (2011) 2.52

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

Developing therapeutic approaches to tau, selected kinases, and related neuronal protein targets. Cold Spring Harb Perspect Med (2011) 1.68

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

Glutamine Triggers Acetylation-Dependent Degradation of Glutamine Synthetase via the Thalidomide Receptor Cereblon. Mol Cell (2016) 1.55

CBP/p300 double null cells reveal effect of coactivator level and diversity on CREB transactivation. EMBO J (2010) 1.55

MacroH2A1.1 and PARP-1 cooperate to regulate transcription by promoting CBP-mediated H2B acetylation. Nat Struct Mol Biol (2014) 1.52

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

3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands. J Med Chem (2011) 1.48

CBP binding outside of promoters and enhancers in Drosophila melanogaster. Epigenetics Chromatin (2015) 1.41

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

A chemical probe toolbox for dissecting the cancer epigenome. Nat Rev Cancer (2017) 1.40

Regulation of RNA polymerase II activation by histone acetylation in single living cells. Nature (2014) 1.40

BET Bromodomain Inhibition Suppresses the Function of Hematopoietic Transcription Factors in Acute Myeloid Leukemia. Mol Cell (2015) 1.36

Docking and scoring with ICM: the benchmarking results and strategies for improvement. J Comput Aided Mol Des (2012) 1.34

p300/CBP histone acetyltransferase activity is required for newly acquired and reactivated fear memories in the lateral amygdala. Learn Mem (2013) 1.31

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

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

Therapeutic strategies to inhibit MYC. Cold Spring Harb Perspect Med (2014) 1.19

Histone acetyltransferases are crucial regulators in NF-κB mediated inflammation. Drug Discov Today (2011) 1.18

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

Structure of a ternary Naa50p (NAT5/SAN) N-terminal acetyltransferase complex reveals the molecular basis for substrate-specific acetylation. J Biol Chem (2011) 1.11

A biotin switch-based proteomics approach identifies 14-3-3ζ as a target of Sirt1 in the metabolic regulation of caspase-2. Mol Cell (2011) 1.09

Use of epigenetic drugs in disease: an overview. Genet Epigenet (2014) 1.08

Paradoxical enhancement of fear extinction memory and synaptic plasticity by inhibition of the histone acetyltransferase p300. J Neurosci (2011) 1.05

A dynamic H3K27ac signature identifies VEGFA-stimulated endothelial enhancers and requires EP300 activity. Genome Res (2013) 1.05

Breaking immune tolerance by targeting Foxp3(+) regulatory T cells mitigates Alzheimer's disease pathology. Nat Commun (2015) 1.04

A histone acetyltransferase p300 inhibitor C646 induces cell cycle arrest and apoptosis selectively in AML1-ETO-positive AML cells. PLoS One (2013) 1.02

Inhibition of p300 impairs Foxp3⁺ T regulatory cell function and promotes antitumor immunity. Nat Med (2013) 1.02

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

p53 and p16(INK4A) independent induction of senescence by chromatin-dependent alteration of S-phase progression. Nat Commun (2011) 1.00

Spermidine induces autophagy by inhibiting the acetyltransferase EP300. Cell Death Differ (2014) 1.00

Histone acetyltransferases: Rising ancient counterparts to protein kinases. Biopolymers (2013) 0.98

Selective inhibition of p300 HAT blocks cell cycle progression, induces cellular senescence, and inhibits the DNA damage response in melanoma cells. J Invest Dermatol (2013) 0.96

Epigenetic pathway targets for the treatment of disease: accelerating progress in the development of pharmacological tools: IUPHAR Review 11. Br J Pharmacol (2014) 0.94

Experimental validation of FINDSITE(comb) virtual ligand screening results for eight proteins yields novel nanomolar and micromolar binders. J Cheminform (2014) 0.94

A small molecule that binds and inhibits the ETV1 transcription factor oncoprotein. Mol Cancer Ther (2014) 0.94

Lysine acetyltransferases CBP and p300 as therapeutic targets in cognitive and neurodegenerative disorders. Curr Pharm Des (2013) 0.93

Ordered changes in histone modifications at the core of the Arabidopsis circadian clock. Proc Natl Acad Sci U S A (2012) 0.93

Changing the selectivity of p300 by acetyl-CoA modulation of histone acetylation. ACS Chem Biol (2014) 0.92

Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents. Mol Cancer Ther (2013) 0.92

Epigenetic (re)programming of caste-specific behavior in the ant Camponotus floridanus. Science (2016) 0.91

Control of Foxo1 gene expression by co-activator P300. J Biol Chem (2013) 0.90

Mapping of histone modifications in episomal HBV cccDNA uncovers an unusual chromatin organization amenable to epigenetic manipulation. Proc Natl Acad Sci U S A (2015) 0.90

Targeting the histone orthography of cancer: drugs for writers, erasers and readers. Br J Pharmacol (2014) 0.90

KATs in cancer: functions and therapies. Oncogene (2015) 0.89

The Role of Histone Acetyltransferases in Normal and Malignant Hematopoiesis. Front Oncol (2015) 0.89

Regulation of Myf5 Early Enhancer by Histone Acetyltransferase p300 during Stem Cell Differentiation. Mol Biol (2012) 0.89

Chromatin signatures at Notch-regulated enhancers reveal large-scale changes in H3K56ac upon activation. EMBO J (2015) 0.89

p300 exerts an epigenetic role in chronic neuropathic pain through its acetyltransferase activity in rats following chronic constriction injury (CCI). Mol Pain (2012) 0.88

Structural determinants of PERK inhibitor potency and selectivity. Chem Biol Drug Des (2010) 0.88

Deregulation of the Ras-Erk Signaling Axis Modulates the Enhancer Landscape. Cell Rep (2015) 0.87

Targeting of histone acetyltransferase p300 by cyclopentenone prostaglandin Δ(12)-PGJ(2) through covalent binding to Cys(1438). Chem Res Toxicol (2011) 0.86

MYC in pancreatic cancer: novel mechanistic insights and their translation into therapeutic strategies. Oncogene (2015) 0.86

Histone acetyltransferase inhibitor II induces apoptosis in glioma cell lines via the p53 signaling pathway. J Exp Clin Cancer Res (2014) 0.86

Chemoproteomic profiling of lysine acetyltransferases highlights an expanded landscape of catalytic acetylation. J Am Chem Soc (2014) 0.86

Small molecule inhibitors of histone acetyltransferase Tip60. Bioorg Chem (2010) 0.85

Live-cell studies of p300/CBP histone acetyltransferase activity and inhibition. Chembiochem (2012) 0.85

The epigenetic regulators CBP and p300 facilitate leukemogenesis and represent therapeutic targets in acute myeloid leukemia. Oncogene (2015) 0.85

Histone acetyltransferase inhibitors block neuroblastoma cell growth in vivo. Oncogenesis (2015) 0.84

P300-dependent STAT3 acetylation is necessary for angiotensin II-induced pro-fibrotic responses in renal tubular epithelial cells. Acta Pharmacol Sin (2014) 0.83

Lysine acetyltransfer supports platelet function. J Thromb Haemost (2015) 0.83

Altering cancer transcriptomes using epigenomic inhibitors. Epigenetics Chromatin (2015) 0.83

Three-dimensional collagen I promotes gemcitabine resistance in vitro in pancreatic cancer cells through HMGA2-dependent histone acetyltransferase expression. PLoS One (2013) 0.83

Epigenetics in the hematologic malignancies. Haematologica (2014) 0.83

Dynamics and function of distal regulatory elements during neurogenesis and neuroplasticity. Genome Res (2015) 0.83

The multifaceted role of lysine acetylation in cancer: prognostic biomarker and therapeutic target. Oncotarget (2016) 0.83

Acetylation and deacetylation--novel factors in muscle wasting. Metabolism (2012) 0.82

Dynamic acetylation of lysine-4-trimethylated histone H3 and H3 variant biology in a simple multicellular eukaryote. Nucleic Acids Res (2012) 0.81

Diverse small molecule inhibitors of human apurinic/apyrimidinic endonuclease APE1 identified from a screen of a large public collection. PLoS One (2012) 0.81

Epigenetic targets for novel therapies of lung diseases. Pharmacol Ther (2014) 0.81

Prostate cancer epigenetics and its clinical implications. Asian J Androl (2016) 0.80

H4K12ac is regulated by estrogen receptor-alpha and is associated with BRD4 function and inducible transcription. Oncotarget (2015) 0.80

Systems pharmacology of adiposity reveals inhibition of EP300 as a common therapeutic mechanism of caloric restriction and resveratrol for obesity. Front Pharmacol (2015) 0.80

Acetylation Reader Proteins: Linking Acetylation Signaling to Genome Maintenance and Cancer. PLoS Genet (2016) 0.79

Noradrenaline goes nuclear: epigenetic modifications during long-lasting synaptic potentiation triggered by activation of β-adrenergic receptors. J Physiol (2015) 0.78

Naphthoquinone-mediated inhibition of lysine acetyltransferase KAT3B/p300, basis for non-toxic inhibitor synthesis. J Biol Chem (2014) 0.78

Targeting HSF1 disrupts HSP90 chaperone function in chronic lymphocytic leukemia. Oncotarget (2015) 0.78

Structure of the p300 histone acetyltransferase bound to acetyl-coenzyme A and its analogues. Biochemistry (2014) 0.78

Histone deacetylase inhibition enhances antimicrobial peptide but not inflammatory cytokine expression upon bacterial challenge. Proc Natl Acad Sci U S A (2016) 0.78

A permissive chromatin structure is adopted prior to site-specific DNA demethylation of developmentally expressed genes involved in macronuclear differentiation. Epigenetics Chromatin (2013) 0.78

A small molecule inhibitor of fungal histone acetyltransferase Rtt109. Bioorg Med Chem Lett (2013) 0.78

Enzyme kinetics and inhibition of histone acetyltransferase KAT8. Eur J Med Chem (2015) 0.78

Metabolic alkene labeling and in vitro detection of histone acylation via the aqueous oxidative Heck reaction. Org Biomol Chem (2015) 0.78

EP300 Protects from Light-Induced Retinopathy in Zebrafish. Front Pharmacol (2016) 0.78

Inhibition of p300 lysine acetyltransferase activity by luteolin reduces tumor growth in head and neck squamous cell carcinoma (HNSCC) xenograft mouse model. Oncotarget (2015) 0.78

An epigenetic switch regulates de novo DNA methylation at a subset of pluripotency gene enhancers during embryonic stem cell differentiation. Nucleic Acids Res (2016) 0.77

Roles for Histone Acetylation in Regulation of Telomere Elongation and Two-cell State in Mouse ES Cells. J Cell Physiol (2015) 0.77

Defining the orphan functions of lysine acetyltransferases. ACS Chem Biol (2015) 0.77

A novel nuclear Src and p300 signaling axis controls migratory and invasive behavior in pancreatic cancer. Oncotarget (2016) 0.77

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

Chromatin Kinases Act on Transcription Factors and Histone Tails in Regulation of Inducible Transcription. Mol Cell (2016) 0.77

Effective Quenchers Are Required to Eliminate the Interference of Substrate: Cofactor Binding in the HAT Scintillation Proximity Assay. Assay Drug Dev Technol (2015) 0.77

TRIM33 switches off Ifnb1 gene transcription during the late phase of macrophage activation. Nat Commun (2015) 0.77

The histone acetyltransferase p300 inhibitor C646 reduces pro-inflammatory gene expression and inhibits histone deacetylases. Biochem Pharmacol (2015) 0.77

Inhibition of bromodomain and extra-terminal (BET) proteins increases NKG2D ligand MICA expression and sensitivity to NK cell-mediated cytotoxicity in multiple myeloma cells: role of cMYC-IRF4-miR-125b interplay. J Hematol Oncol (2016) 0.77

CBP/p300 acetyltransferases regulate the expression of NKG2D ligands on tumor cells. Oncogene (2016) 0.77

HAT trick: p300, small molecule, inhibitor. Chem Biol (2010) 0.77

Articles cited by this

NMRPipe: a multidimensional spectral processing system based on UNIX pipes. J Biomol NMR (1995) 93.94

Lysine acetylation targets protein complexes and co-regulates major cellular functions. Science (2009) 20.49

Activation of p53 sequence-specific DNA binding by acetylation of the p53 C-terminal domain. Cell (1997) 16.79

The CBP co-activator is a histone acetyltransferase. Nature (1997) 10.91

CBP/p300 in cell growth, transformation, and development. Genes Dev (2000) 10.76

The many roles of histone deacetylases in development and physiology: implications for disease and therapy. Nat Rev Genet (2009) 9.68

Potent and specific inhibition of mammalian histone deacetylase both in vivo and in vitro by trichostatin A. J Biol Chem (1990) 9.21

Nuclear receptor coactivator ACTR is a novel histone acetyltransferase and forms a multimeric activation complex with P/CAF and CBP/p300. Cell (1997) 8.72

Esters of methanesulfonic acid as irreversible inhibitors of acetylcholinesterase. J Biol Chem (1962) 7.31

Lysine acetylation: codified crosstalk with other posttranslational modifications. Mol Cell (2008) 6.93

Extraction, purification and analysis of histones. Nat Protoc (2007) 6.25

A fasting inducible switch modulates gluconeogenesis via activator/coactivator exchange. Nature (2008) 4.43

High-throughput assays for promiscuous inhibitors. Nat Chem Biol (2005) 4.32

Dynamic histone H3 methylation during gene induction: HYPB/Setd2 mediates all H3K36 trimethylation. EMBO J (2007) 3.81

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

The nucleosomal response associated with immediate-early gene induction is mediated via alternative MAP kinase cascades: MSK1 as a potential histone H3/HMG-14 kinase. EMBO J (1999) 3.58

Phosphoacetylation of histone H3 on c-fos- and c-jun-associated nucleosomes upon gene activation. EMBO J (2000) 3.35

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

Curcumin, a novel p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. J Biol Chem (2004) 3.13

Flexible protein-ligand docking by global energy optimization in internal coordinates. Proteins (1997) 3.02

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

Small molecule modulators of histone acetyltransferase p300. J Biol Chem (2003) 2.74

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

Global and site-specific quantitative phosphoproteomics: principles and applications. Annu Rev Pharmacol Toxicol (2009) 2.53

Specific inhibition of p300-HAT alters global gene expression and represses HIV replication. Chem Biol (2007) 2.15

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

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

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

Histone acetyl transferases as emerging drug targets. Drug Discov Today (2009) 1.64

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

Discovery of novel chemotypes to a G-protein-coupled receptor through ligand-steered homology modeling and structure-based virtual screening. J Med Chem (2008) 1.52

Chemistry of acetyl transfer by histone modifying enzymes: structure, mechanism and implications for effector design. Oncogene (2007) 1.50

Sas4 and Sas5 are required for the histone acetyltransferase activity of Sas2 in the SAS complex. J Biol Chem (2003) 1.48

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

Bisubstrate inhibition: Theory and application to N-acetyltransferases. Biochemistry (2006) 1.32

Isoform-selective histone deacetylase inhibitors. Curr Pharm Des (2008) 1.29

Modeling of the aryl hydrocarbon receptor (AhR) ligand binding domain and its utility in virtual ligand screening to predict new AhR ligands. J Med Chem (2009) 1.28

A continuous, nonradioactive assay for histone acetyltransferases. Anal Biochem (2000) 1.26

Structure of the GCN5 histone acetyltransferase bound to a bisubstrate inhibitor. Proc Natl Acad Sci U S A (2002) 1.22

Small molecules block the polymerization of Z alpha1-antitrypsin and increase the clearance of intracellular aggregates. J Med Chem (2007) 1.21

Recent advances in chemical approaches to the study of biological systems. Annu Rev Cell Dev Biol (2001) 1.17

Inhibition of lysine acetyltransferase KAT3B/p300 activity by a naturally occurring hydroxynaphthoquinone, plumbagin. J Biol Chem (2009) 1.17

Characterization of the yeast trimeric-SAS acetyltransferase complex. J Biol Chem (2005) 1.16

Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity. Mol Cancer Ther (2005) 1.15

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

p300 is required for orderly G1/S transition in human cancer cells. Oncogene (2006) 1.13

Mechanism of p300 specific histone acetyltransferase inhibition by small molecules. J Med Chem (2009) 1.11

The human monocytic leukemia zinc finger histone acetyltransferase domain contains DNA-binding activity implicated in chromatin targeting. J Biol Chem (2007) 1.05

Discovery of new Gram-negative antivirulence drugs: structure and properties of novel E. coli WaaC inhibitors. Bioorg Med Chem Lett (2008) 0.99

De novo discovery of serotonin N-acetyltransferase inhibitors. J Med Chem (2007) 0.86

Dantrolene analogues revisited: general synthesis and specific functions capable of discriminating two kinds of Ca2+ release from sarcoplasmic reticulum of mouse skeletal muscle. Bioorg Med Chem (2003) 0.85

Highly modular synthesis of C1-symmetric aminosulfoximines and their use as ligands in copper-catalyzed asymmetric Mukaiyama-aldol reactions. Chemistry (2005) 0.83

Fluorescent markers for hypoxic cells. A study of novel heterocyclic compounds that undergo bio-reductive binding. Biochem Pharmacol (1991) 0.82

General strategy for the synthesis of natural and unnatural dialkylmaleic anhydrides. J Org Chem (2008) 0.81

Articles by these authors

Efficacy and safety of sorafenib in patients in the Asia-Pacific region with advanced hepatocellular carcinoma: a phase III randomised, double-blind, placebo-controlled trial. Lancet Oncol (2008) 23.93

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

XCMS: processing mass spectrometry data for metabolite profiling using nonlinear peak alignment, matching, and identification. Anal Chem (2006) 15.00

Tet-mediated formation of 5-carboxylcytosine and its excision by TDG in mammalian DNA. Science (2011) 13.16

Gefitinib versus docetaxel in previously treated non-small-cell lung cancer (INTEREST): a randomised phase III trial. Lancet (2008) 10.74

Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists. Science (2010) 10.30

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

METLIN: a metabolite mass spectral database. Ther Drug Monit (2005) 10.15

Detection of circulating tumor DNA in early- and late-stage human malignancies. Sci Transl Med (2014) 8.36

Association of BRCA1 and BRCA2 mutations with survival, chemotherapy sensitivity, and gene mutator phenotype in patients with ovarian cancer. JAMA (2011) 6.81

Evaluation of the bacterial diversity in the feces of cattle using 16S rDNA bacterial tag-encoded FLX amplicon pyrosequencing (bTEFAP). BMC Microbiol (2008) 6.28

Ecological impacts of invasive alien plants: a meta-analysis of their effects on species, communities and ecosystems. Ecol Lett (2011) 5.95

Afatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a phase 2b/3 randomised trial. Lancet Oncol (2012) 5.82

Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease. Science (2007) 5.49

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

The kinase mTOR regulates the differentiation of helper T cells through the selective activation of signaling by mTORC1 and mTORC2. Nat Immunol (2011) 5.22

Treatment of anemia with darbepoetin alfa in systolic heart failure. N Engl J Med (2013) 4.67

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

A fasting inducible switch modulates gluconeogenesis via activator/coactivator exchange. Nature (2008) 4.43

Nitric oxide-induced mitochondrial fission is regulated by dynamin-related GTPases in neurons. EMBO J (2006) 4.43

Survey of bacterial diversity in chronic wounds using pyrosequencing, DGGE, and full ribosome shotgun sequencing. BMC Microbiol (2008) 4.30

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

Intercalated combination of chemotherapy and erlotinib for patients with advanced stage non-small-cell lung cancer (FASTACT-2): a randomised, double-blind trial. Lancet Oncol (2013) 4.20

Neuroprotective effects of brain-derived neurotrophic factor in rodent and primate models of Alzheimer's disease. Nat Med (2009) 4.11

Dynamic histone H3 methylation during gene induction: HYPB/Setd2 mediates all H3K36 trimethylation. EMBO J (2007) 3.81

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

Enhanced histone acetylation and transcription: a dynamic perspective. Mol Cell (2006) 3.59

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

Phase III study of letrozole versus tamoxifen as first-line therapy of advanced breast cancer in postmenopausal women: analysis of survival and update of efficacy from the International Letrozole Breast Cancer Group. J Clin Oncol (2003) 3.51

De novo gene mutations highlight patterns of genetic and neural complexity in schizophrenia. Nat Genet (2012) 3.49

Structure of the human histamine H1 receptor complex with doxepin. Nature (2011) 3.48

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

Vandetanib plus docetaxel versus docetaxel as second-line treatment for patients with advanced non-small-cell lung cancer (ZODIAC): a double-blind, randomised, phase 3 trial. Lancet Oncol (2010) 3.30

An effective PSO-based memetic algorithm for flow shop scheduling. IEEE Trans Syst Man Cybern B Cybern (2007) 3.30

Comparative study of several algorithms for flexible ligand docking. J Comput Aided Mol Des (2003) 3.29

MSK2 and MSK1 mediate the mitogen- and stress-induced phosphorylation of histone H3 and HMG-14. EMBO J (2003) 3.29

PKA-I holoenzyme structure reveals a mechanism for cAMP-dependent activation. Cell (2007) 3.19

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

EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformation. Cancer Cell (2013) 3.13

Distal airway stem cells yield alveoli in vitro and during lung regeneration following H1N1 influenza infection. Cell (2011) 3.00

Icotinib versus gefitinib in previously treated advanced non-small-cell lung cancer (ICOGEN): a randomised, double-blind phase 3 non-inferiority trial. Lancet Oncol (2013) 2.94

Rac function and regulation during Drosophila development. Nature (2002) 2.89

Polymicrobial nature of chronic diabetic foot ulcer biofilm infections determined using bacterial tag encoded FLX amplicon pyrosequencing (bTEFAP). PLoS One (2008) 2.87

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

Pocketome via comprehensive identification and classification of ligand binding envelopes. Mol Cell Proteomics (2005) 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

Comprehensive expression profiling of tumor cell lines identifies molecular signatures of melanoma progression. PLoS One (2007) 2.77

Severe fever with thrombocytopenia syndrome virus, Shandong Province, China. Emerg Infect Dis (2012) 2.77

Bacterial tag-encoded FLX amplicon pyrosequencing (bTEFAP) for microbiome studies: bacterial diversity in the ileum of newly weaned Salmonella-infected pigs. Foodborne Pathog Dis (2008) 2.77

Concurrent chemoradiotherapy plus adjuvant chemotherapy versus concurrent chemoradiotherapy alone in patients with locoregionally advanced nasopharyngeal carcinoma: a phase 3 multicentre randomised controlled trial. Lancet Oncol (2011) 2.75

A method to measure cardiac autophagic flux in vivo. Autophagy (2008) 2.72

Human embryonic stem cell-derived GABA neurons correct locomotion deficits in quinolinic acid-lesioned mice. Cell Stem Cell (2012) 2.62

Conserved binding mode of human beta2 adrenergic receptor inverse agonists and antagonist revealed by X-ray crystallography. J Am Chem Soc (2010) 2.62

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

Computational analysis of bacterial RNA-Seq data. Nucleic Acids Res (2013) 2.50

MAPK-regulated transcription: a continuously variable gene switch? Nat Rev Mol Cell Biol (2002) 2.46

Effects of glucosinolate-rich broccoli sprouts on urinary levels of aflatoxin-DNA adducts and phenanthrene tetraols in a randomized clinical trial in He Zuo township, Qidong, People's Republic of China. Cancer Epidemiol Biomarkers Prev (2005) 2.45

Randomized phase III placebo-controlled trial of letrozole plus oral temsirolimus as first-line endocrine therapy in postmenopausal women with locally advanced or metastatic breast cancer. J Clin Oncol (2012) 2.44

Randomized, multicenter, open-label study of oxaliplatin plus fluorouracil/leucovorin versus doxorubicin as palliative chemotherapy in patients with advanced hepatocellular carcinoma from Asia. J Clin Oncol (2013) 2.44

Early use of noninvasive positive pressure ventilation for acute lung injury: a multicenter randomized controlled trial. Crit Care Med (2012) 2.43

Differential effects of prostaglandin derived from omega-6 and omega-3 polyunsaturated fatty acids on COX-2 expression and IL-6 secretion. Proc Natl Acad Sci U S A (2003) 2.40

A network model to predict the risk of death in sickle cell disease. Blood (2007) 2.39

Flexible ligand docking to multiple receptor conformations: a practical alternative. Curr Opin Struct Biol (2008) 2.38

Id proteins in cell growth and tumorigenesis. Cancer Cell (2003) 2.38

Integrated analyses identify a master microRNA regulatory network for the mesenchymal subtype in serous ovarian cancer. Cancer Cell (2013) 2.34

Neratinib, an irreversible ErbB receptor tyrosine kinase inhibitor, in patients with advanced ErbB2-positive breast cancer. J Clin Oncol (2010) 2.34

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

A hybrid vector for ligand-directed tumor targeting and molecular imaging. Cell (2006) 2.20

Efficacy and safety of dexamethasone ointment on recurrent aphthous ulceration. Am J Med (2012) 2.19

Rac GTPases control axon growth, guidance and branching. Nature (2002) 2.14

Direct evidence for endothelial vascular endothelial growth factor receptor-1 function in nitric oxide-mediated angiogenesis. Circ Res (2006) 2.12

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

Status of GPCR modeling and docking as reflected by community-wide GPCR Dock 2010 assessment. Structure (2011) 2.11

Molecular basis for the recognition of phosphorylated and phosphoacetylated histone h3 by 14-3-3. Mol Cell (2005) 2.10

Nuclear hormone receptor targeted virtual screening. J Med Chem (2003) 2.05

Analysis of full and partial agonists binding to beta2-adrenergic receptor suggests a role of transmembrane helix V in agonist-specific conformational changes. J Mol Recognit (2009) 2.05

The BCL6 transcriptional program features repression of multiple oncogenes in primary B cells and is deregulated in DLBCL. Blood (2009) 2.04

Clinicopathological significance of microRNA-31, -143 and -145 expression in colorectal cancer. Dis Markers (2009) 2.02

Crop diversity for yield increase. PLoS One (2009) 2.02

Efficacy, safety, and immunogenicity of an enterovirus 71 vaccine in China. N Engl J Med (2014) 2.01

MicroRNA-1 regulates cardiomyocyte apoptosis by targeting Bcl-2. Int Heart J (2009) 2.01

Effect of otitis media with effusion and its clinical intervention on the development of mastoid in children. Acta Otolaryngol (2014) 1.98

S100A8/A9 activate key genes and pathways in colon tumor progression. Mol Cancer Res (2011) 1.98

Toward a molecular classification of melanoma. J Clin Oncol (2007) 1.95

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

Effect of different labor forces on fetal skull molding. Med Eng Phys (2011) 1.92

MAP kinase-mediated phosphoacetylation of histone H3 and inducible gene regulation. FEBS Lett (2003) 1.92

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