Published in Biochemistry on March 17, 2007
Epigenetic protein families: a new frontier for drug discovery. Nat Rev Drug Discov (2012) 6.70
The lysine demethylase LSD1 (KDM1) is required for maintenance of global DNA methylation. Nat Genet (2008) 4.40
Chemical probes for histone-modifying enzymes. Nat Chem Biol (2008) 3.30
Inhibition of the histone demethylase LSD1 blocks alpha-herpesvirus lytic replication and reactivation from latency. Nat Med (2009) 2.51
A novel mammalian flavin-dependent histone demethylase. J Biol Chem (2009) 2.25
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Comparative analysis of small molecules and histone substrate analogues as LSD1 lysine demethylase inhibitors. J Am Chem Soc (2010) 1.29
FAD-dependent lysine-specific demethylase-1 regulates cellular energy expenditure. Nat Commun (2012) 1.21
Mechanistic analysis of a suicide inactivator of histone demethylase LSD1. Biochemistry (2007) 1.20
Inhibition of LSD1 sensitizes glioblastoma cells to histone deacetylase inhibitors. Neuro Oncol (2011) 1.16
A novel selective LSD1/KDM1A inhibitor epigenetically blocks herpes simplex virus lytic replication and reactivation from latency. MBio (2013) 1.15
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Recent advances in the development of polyamine analogues as antitumor agents. J Med Chem (2009) 1.06
Histone demethylases and cancer. Adv Cancer Res (2009) 1.05
Brain-penetrant LSD1 inhibitors can block memory consolidation. ACS Chem Neurosci (2011) 1.04
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Inhibition of LSD1 reduces herpesvirus infection, shedding, and recurrence by promoting epigenetic suppression of viral genomes. Sci Transl Med (2014) 1.00
Use of pH and kinetic isotope effects to establish chemistry as rate-limiting in oxidation of a peptide substrate by LSD1. Biochemistry (2009) 0.99
Targeting protein lysine methylation and demethylation in cancers. Acta Biochim Biophys Sin (Shanghai) (2012) 0.98
Facile synthesis of substituted trans-2-arylcyclopropylamine inhibitors of the human histone demethylase LSD1 and monoamine oxidases A and B. Bioorg Med Chem Lett (2008) 0.96
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Low molecular weight amidoximes that act as potent inhibitors of lysine-specific demethylase 1. J Med Chem (2012) 0.92
Lysine-specific histone demethylase 1 inhibitors control breast cancer proliferation in ERα-dependent and -independent manners. ACS Chem Biol (2012) 0.89
Polyamine-based small molecule epigenetic modulators. Medchemcomm (2011) 0.87
Histone lysine-specific methyltransferases and demethylases in carcinogenesis: new targets for cancer therapy and prevention. Curr Cancer Drug Targets (2013) 0.87
Structures and Mechanism of the Monoamine Oxidase Family. Biomol Concepts (2011) 0.86
Thermodynamic characterization of the binding interaction between the histone demethylase LSD1/KDM1 and CoREST. Biochemistry (2010) 0.86
Analysis of the levels of lysine-specific demethylase 1 (LSD1) mRNA in human ovarian tumors and the effects of chemical LSD1 inhibitors in ovarian cancer cell lines. J Ovarian Res (2013) 0.85
Helicobacter pylori regulates iNOS promoter by histone modifications in human gastric epithelial cells. Med Microbiol Immunol (2012) 0.85
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KDM1 class flavin-dependent protein lysine demethylases. Biopolymers (2015) 0.84
Azalysine analogues as probes for protein lysine deacetylation and demethylation. J Am Chem Soc (2012) 0.84
Lysine-specific demethylase 1-mediated demethylation of histone H3 lysine 9 contributes to interleukin 1β-induced microsomal prostaglandin E synthase 1 expression in human osteoarthritic chondrocytes. Arthritis Res Ther (2014) 0.83
Suppression of gluconeogenic gene expression by LSD1-mediated histone demethylation. PLoS One (2013) 0.82
Computational methods for de novo protein design and its applications to the human immunodeficiency virus 1, purine nucleoside phosphorylase, ubiquitin specific protease 7, and histone demethylases. Curr Drug Targets (2010) 0.81
Flavin-dependent enzymes in cancer prevention. Int J Mol Sci (2012) 0.81
Tranylcypromine reduces herpes simplex virus 1 infection in mice. Antimicrob Agents Chemother (2014) 0.79
Structure-activity study for (bis)ureidopropyl- and (bis)thioureidopropyldiamine LSD1 inhibitors with 3-5-3 and 3-6-3 carbon backbone architectures. Bioorg Med Chem (2015) 0.79
Chromatin-modifying agents for epigenetic reprogramming and endogenous neural stem cell-mediated repair in stroke. Transl Stroke Res (2011) 0.78
Expanding the druggable space of the LSD1/CoREST epigenetic target: new potential binding regions for drug-like molecules, peptides, protein partners, and chromatin. PLoS Comput Biol (2013) 0.78
Therapeutic opportunities in Ewing sarcoma: EWS-FLI inhibition via LSD1 targeting. Oncotarget (2016) 0.78
Effects of the monoamine oxidase inhibitors pargyline and tranylcypromine on cellular proliferation in human prostate cancer cells. Oncol Rep (2013) 0.77
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Fluorinated phenylcyclopropylamines. Part 5: Effects of electron-withdrawing or -donating aryl substituents on the inhibition of monoamine oxidases A and B by 2-aryl-2-fluoro-cyclopropylamines. Bioorg Med Chem (2008) 0.77
Inhibitors of Protein Methyltransferases and Demethylases. Chem Rev (2017) 0.76
A rationally-designed chimeric KDM1A/KDM1B histone demethylase tower domain deletion mutant retaining enzymatic activity. FEBS Lett (2015) 0.76
Key Targets for Multi-Target Ligands Designed to Combat Neurodegeneration. Front Neurosci (2016) 0.76
Exogenous application of histone demethylase inhibitor trans-2-phenylcyclopropylamine mimics FLD loss-of-function phenotype in terms of systemic acquired resistance in Arabidopsis thaliana. Plant Signal Behav (2014) 0.76
Measurement of lysine-specific demethylase-1 activity in the nuclear extracts by flow-injection based time-of-flight mass spectrometry. J Clin Biochem Nutr (2015) 0.76
Concerted hydrogen atom and electron transfer mechanism for catalysis by lysine-specific demethylase. J Phys Chem B (2013) 0.76
Synthesis, LSD1 Inhibitory Activity, and LSD1 Binding Model of Optically Pure Lysine-PCPA Conjugates. Comput Struct Biotechnol J (2014) 0.76
LSD1: biologic roles and therapeutic targeting. Epigenomics (2016) 0.76
LSD1 Histone Demethylase Assays and Inhibition. Methods Enzymol (2016) 0.76
Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies. ACS Med Chem Lett (2014) 0.76
Structure and function of dioxygenases in histone demethylation and DNA/RNA demethylation. IUCrJ (2014) 0.75
Lysine-Specific Demethylase 1A (KDM1A/LSD1): Product Recognition and Kinetic Analysis of Full-Length Histones. Biochemistry (2016) 0.75
Discovery of [1,2,3]Triazolo[4,5-d]pyrimidine Derivatives as Novel LSD1 Inhibitors. ACS Med Chem Lett (2017) 0.75
Towards the development of activity-based probes for detection of lysine-specific demethylase-1 activity. Bioorg Med Chem (2016) 0.75
Small Molecule Lysyl Oxidase-like 2 (LOXL2) Inhibitors: The Identification of an Inhibitor Selective for LOXL2 over LOX. ACS Med Chem Lett (2017) 0.75
The winding path of protein methylation research: milestones and new frontiers. Nat Rev Mol Cell Biol (2017) 0.75
Histone H3 lysine 4 demethylation is a target of nonselective antidepressive medications. Chem Biol (2006) 3.15
Reassessing the role of the secreted protease CPAF in Chlamydia trachomatis infection through genetic approaches. Pathog Dis (2014) 2.50
Crystal structure of Streptococcus pyogenes sortase A: implications for sortase mechanism. J Biol Chem (2009) 1.52
Critical role of NOD2 in regulating the immune response to Staphylococcus aureus. Infect Immun (2009) 1.49
Analysis of the substrate specificity of the Staphylococcus aureus sortase transpeptidase SrtA. Biochemistry (2004) 1.34
Sortase transpeptidases: insights into mechanism, substrate specificity, and inhibition. Biopolymers (2010) 1.26
The Chlamydia protease CPAF regulates host and bacterial proteins to maintain pathogen vacuole integrity and promote virulence. Cell Host Microbe (2011) 1.21
Facile synthesis of site-specifically acetylated and methylated histone proteins: reagents for evaluation of the histone code hypothesis. Proc Natl Acad Sci U S A (2003) 1.20
Staphylococcus aureus sortase transpeptidase SrtA: insight into the kinetic mechanism and evidence for a reverse protonation catalytic mechanism. Biochemistry (2005) 1.19
Development of a high-performance liquid chromatography assay and revision of kinetic parameters for the Staphylococcus aureus sortase transpeptidase SrtA. Anal Biochem (2004) 1.17
Mutagenesis studies of substrate recognition and catalysis in the sortase A transpeptidase from Staphylococcus aureus. J Biol Chem (2008) 1.07
Mutational analysis of active site residues in the Staphylococcus aureus transpeptidase SrtA. Biochemistry (2007) 1.07
Phosphorus-based SAHA analogues as histone deacetylase inhibitors. Org Lett (2003) 1.04
Engineering the substrate specificity of Staphylococcus aureus Sortase A. The beta6/beta7 loop from SrtB confers NPQTN recognition to SrtA. J Biol Chem (2007) 1.03
Vinyl sulfones: inhibitors of SrtA, a transpeptidase required for cell wall protein anchoring and virulence in Staphylococcus aureus. J Am Chem Soc (2004) 1.00
Use of pH and kinetic isotope effects to establish chemistry as rate-limiting in oxidation of a peptide substrate by LSD1. Biochemistry (2009) 0.99
Complexation of peptidoglycan intermediates by the lipoglycodepsipeptide antibiotic ramoplanin: minimal structural requirements for intermolecular complexation and fibril formation. Proc Natl Acad Sci U S A (2002) 0.98
Autocatalytic intramolecular isopeptide bond formation in gram-positive bacterial pili: a QM/MM simulation. J Am Chem Soc (2010) 0.97
Facile synthesis of substituted trans-2-arylcyclopropylamine inhibitors of the human histone demethylase LSD1 and monoamine oxidases A and B. Bioorg Med Chem Lett (2008) 0.96
Light-induced helix formation. J Am Chem Soc (2002) 0.93
Inhibition of the Staphylococcus aureus sortase transpeptidase SrtA by phosphinic peptidomimetics. Bioorg Med Chem (2004) 0.89
Lysine-specific histone demethylase 1 inhibitors control breast cancer proliferation in ERα-dependent and -independent manners. ACS Chem Biol (2012) 0.89
Techniques used to study transcription on chromatin templates. Methods Enzymol (2004) 0.87
Functional analysis of the lipoglycodepsipeptide antibiotic ramoplanin. Chem Biol (2002) 0.87
Thermodynamic characterization of the binding interaction between the histone demethylase LSD1/KDM1 and CoREST. Biochemistry (2010) 0.86
A crystal structure of a dimer of the antibiotic ramoplanin illustrates membrane positioning and a potential Lipid II docking interface. Proc Natl Acad Sci U S A (2009) 0.85
Chlamydia protease-like activity factor (CPAF): characterization of proteolysis activity in vitro and development of a nanomolar affinity CPAF zymogen-derived inhibitor. Biochemistry (2011) 0.84
Generation of ramoplanin-resistant Staphylococcus aureus. FEMS Microbiol Lett (2010) 0.82
Probing of the cis-5-phenyl proline scaffold as a platform for the synthesis of mechanism-based inhibitors of the Staphylococcus aureus sortase SrtA isoform. Bioorg Med Chem (2009) 0.81
Studies on the biosynthesis of the lipodepsipeptide antibiotic Ramoplanin A2. Bioorg Med Chem (2011) 0.80
Monitoring β-secretase activity in living cells with a membrane-anchored FRET probe. Angew Chem Int Ed Engl (2012) 0.78
Staphylococcus aureus sortase A contributes to the Trojan horse mechanism of immune defense evasion with its intrinsic resistance to Cys184 oxidation. Biochemistry (2011) 0.78
An economical and preparative orthogonal solid phase synthesis of fluorescein and rhodamine derivatized peptides: FRET substrates for the Staphylococcus aureus sortase SrtA transpeptidase reaction. Chem Commun (Camb) (2002) 0.78
Sortase-catalyzed initiator attachment enables high yield growth of a stealth polymer from the C terminus of a protein. Macromol Rapid Commun (2013) 0.77
Solvent dependence of intramolecular electron transfer in a helical oligoproline assembly. J Am Chem Soc (2004) 0.76
Profiling natural product biosynthesis. Chem Biol (2004) 0.75
Found in translation: applications of protein and peptide molecular diversity. Curr Opin Chem Biol (2011) 0.75