Histone acetyltransferases: challenges in targeting bi-substrate enzymes

Enzyme kinetics and inhibition of histone acetyltransferase KAT8

(2015) Hannah Wapenaar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A Novel Cell-Permeable, Selective, and Noncompetitive Inhibitor of KAT3 Histone Acetyltransferases from a Combined Molecular Pruning/Classical Isosterism Approach

(2015) Ciro Milite et al.   JOURNAL OF MEDICINAL CHEMISTRY

Garcinol, an Acetyltransferase Inhibitor, Suppresses Proliferation of Breast Cancer Cell Line MCF-7 Promoted by 17β-Estradiol

(2014) Xia Ye et al.   Asian Pacific Journal of Cancer Prevention

Crafting the Brain – Role of Histone Acetyltransferases in Neural Development and Disease

(2014) Bilal N. Sheikh   CELL AND TISSUE RESEARCH

Rational Design of Substrate-Based Multivalent Inhibitors of the Histone Acetyltransferase Tip60

(2014) Chao Yang et al.   ChemMedChem

The Histone Acetylase Activator Pentadecylidenemalonate 1b Rescues Proliferation and Differentiation in the Human Cardiac Mesenchymal Cells of Type 2 Diabetic Patients

(2014) Matteo Vecellio et al.   DIABETES

Histone Acetylation and Flagellin Are Essential for Legionella pneumophila-Induced Cytokine Expression

(2014) B. Schmeck et al.   JOURNAL OF IMMUNOLOGY

Garcinol suppresses inflammation-associated colon carcinogenesis in mice

(2014) Mei-Ling Tsai et al.   MOLECULAR NUTRITION & FOOD RESEARCH

The Chemistry of Curcumin: From Extraction to Therapeutic Agent

(2014) Kavirayani Priyadarsini   MOLECULES

C646, a selective small molecule inhibitor of histone acetyltransferase p300, radiosensitizes lung cancer cells by enhancing mitotic catastrophe

(2014) Takahiro Oike et al.   RADIOTHERAPY AND ONCOLOGY

Rational design and validation of a Tip60 histone acetyltransferase inhibitor

(2014) Chunxia Gao et al.   Scientific Reports

Lysine Acetyltransferase PCAF Is a Key Regulator of Arteriogenesis

(2013) Antonius J.N.M. Bastiaansen et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Activity and expression of histone acetylases and deacetylases in inflammatory phenotypes of asthma

(2013) L. P. Gunawardhana et al.   CLINICAL AND EXPERIMENTAL ALLERGY

Selective Inhibition of p300 HAT Blocks Cell Cycle Progression, Induces Cellular Senescence, and Inhibits the DNA Damage Response in Melanoma Cells

(2013) Gai Yan et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

A Novel Activator of CBP/p300 Acetyltransferases Promotes Neurogenesis and Extends Memory Duration in Adult Mice

(2013) S. Chatterjee et al.   JOURNAL OF NEUROSCIENCE

A Histone Acetyltransferase p300 Inhibitor C646 Induces Cell Cycle Arrest and Apoptosis Selectively in AML1-ETO-Positive AML Cells

(2013) Xiao-ning Gao et al.   PLoS One

Small organic molecules targeting PCAF bromodomain as potent inhibitors of HIV-1 replication

(2013) Qiang Wang et al.   MedChemComm

P300/CBP Associated Factor Regulates Nitroglycerin-Dependent Arterial Relaxation by N ε -Lysine Acetylation of Contractile Proteins

(2012) Claudia Colussi et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Garcinol, a Histone Acetyltransferase Inhibitor, Radiosensitizes Cancer Cells by Inhibiting Non-Homologous End Joining

(2012) Takahiro Oike et al.   INTERNATIONAL JOURNAL OF RADIATION ONCOLOGY BIOLOGY PHYSICS

p300/CBP-Associated Factor Selectively Regulates the Extinction of Conditioned Fear

(2012) W. Wei et al.   JOURNAL OF NEUROSCIENCE

Small Molecule Inhibitors of Histone Acetyltransferases as Epigenetic Tools and Drug Candidates

(2011) Silviya D. Furdas et al.   ARCHIV DER PHARMAZIE

A Small Molecule Binding to the Coactivator CREB-Binding Protein Blocks Apoptosis in Cardiomyocytes

(2011) Jagat C. Borah et al.   CHEMISTRY & BIOLOGY

Histone acetyltransferases are crucial regulators in NF-κB mediated inflammation

(2011) Massimo Ghizzoni et al.   DRUG DISCOVERY TODAY

MYST protein acetyltransferase activity requires active site lysine autoacetylation

(2011) Hua Yuan et al.   EMBO JOURNAL

Bromodomains as therapeutic targets

(2011) Susanne Muller et al.   EXPERT REVIEWS IN MOLECULAR MEDICINE

Lysine acetylation in obesity, diabetes and metabolic disease

(2011) Abishek Iyer et al.   IMMUNOLOGY AND CELL BIOLOGY

Rational Design of Cyclic Peptide Modulators of the Transcriptional Coactivator CBP: A New Class of p53 Inhibitors

(2011) Guillermo Gerona-Navarro et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Inhibition of the Acetyltransferases p300 and CBP Reveals a Targetable Function for p300 in the Survival and Invasion Pathways of Prostate Cancer Cell Lines

(2011) F. R. Santer et al.   MOLECULAR CANCER THERAPEUTICS

Isothiazolones; thiol-reactive inhibitors of cysteine protease cathepsin B and histone acetyltransferase PCAF

(2011) Rosalina Wisastra et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

N -lysine acetylation determines dissociation from GAP junctions and lateralization of connexin 43 in normal and dystrophic heart

(2011) C. Colussi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Global Histone Modification Patterns as Prognostic Markers to Classify Glioma Patients

(2010) B.-l. Liu et al.   CANCER EPIDEMIOLOGY BIOMARKERS & PREVENTION

Global Levels of Specific Histone Modifications and an Epigenetic Gene Signature Predict Prostate Cancer Progression and Development

(2010) T. Bianco-Miotto et al.   CANCER EPIDEMIOLOGY BIOMARKERS & PREVENTION

Virtual Ligand Screening of the p300/CBP Histone Acetyltransferase: Identification of a Selective Small Molecule Inhibitor

(2010) Erin M. Bowers et al.   CHEMISTRY & BIOLOGY

Role of histone acetylation in cell physiology and diseases: An update

(2010) Shahper N. Khan et al.   CLINICA CHIMICA ACTA

Inhibition of Wnt/ -catenin/CREB binding protein (CBP) signaling reverses pulmonary fibrosis

(2010) W. R. Henderson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Current Perspectives on Role of Chromatin Modifications and Deacetylases in Lung Inflammation in COPD

(2009) Saravanan Rajendrasozhan et al.   COPD-Journal of Chronic Obstructive Pulmonary Disease

Histone acetyl transferases as emerging drug targets

(2009) Frank J. Dekker et al.   DRUG DISCOVERY TODAY

Two Mammalian MOF Complexes Regulate Transcription Activation by Distinct Mechanisms

(2009) Xiangzhi Li et al.   MOLECULAR CELL

Lysine Acetylation Targets Protein Complexes and Co-Regulates Major Cellular Functions

(2009) C. Choudhary et al.   SCIENCE

Acetylation of Sirt2 by p300 attenuates its deacetylase activity

(2008) Younho Han et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs)

(2008) Stephen Gorsuch et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Inhibition of the PCAF histone acetyl transferase and cell proliferation by isothiazolones

(2008) Frank J. Dekker et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases

(2008) Gianluca Sbardella et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Human ATAC Is a GCN5/PCAF-containing Acetylase Complex with a Novel NC2-like Histone Fold Module That Interacts with the TATA-binding Protein

(2008) Yuan-Liang Wang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Mechanism of p300 Specific Histone Acetyltransferase Inhibition by Small Molecules

(2008) M. Arif et al.   JOURNAL OF MEDICINAL CHEMISTRY

The structural basis of protein acetylation by the p300/CBP transcriptional coactivator

(2008) Xin Liu et al.   NATURE