Perspectives on the Discovery of Small-Molecule Modulators for Epigenetic Processes
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Deepak Bandyopadhyay | Alan P. Graves | Simon F. Semus | Quinn Lu | Deepak Bandyopadhyay | S. Semus | S. Thrall | A. P. Graves | A. Pope | Andrew J. Pope | Quinn Lu | Amy M. Quinn | Mehul P. Patel | Sara H. Thrall
[1] Stephan Beck,et al. The methylome: approaches for global DNA methylation profiling. , 2008, Trends in genetics : TIG.
[2] John Kuriyan,et al. The origin of protein interactions and allostery in colocalization , 2007, Nature.
[3] Dinshaw J. Patel,et al. Multivalent engagement of chromatin modifications by linked binding modules , 2007, Nature Reviews Molecular Cell Biology.
[4] Baoguang Zhao,et al. Design, synthesis and selection of DNA-encoded small-molecule libraries. , 2009, Nature chemical biology.
[5] M. Begemann,et al. Concise Review: Roles of Polycomb Group Proteins in Development and Disease: A Stem Cell Perspective , 2007, Stem cells.
[6] Jacqueline Cherfils,et al. Structure-based discovery of an inhibitor of Arf activation by Sec7 domains through targeting of protein–protein complexes , 2007, Proceedings of the National Academy of Sciences.
[7] T. Heightman,et al. Inhibition of Histone Demethylases by 4‐Carboxy‐2,2′‐Bipyridyl Compounds , 2011, ChemMedChem.
[8] T. Kundu,et al. Polyisoprenylated Benzophenone, Garcinol, a Natural Histone Acetyltransferase Inhibitor, Represses Chromatin Transcription and Alters Global Gene Expression* , 2004, Journal of Biological Chemistry.
[9] Burkhard Rost,et al. Protein–Protein Interaction Hotspots Carved into Sequences , 2007, PLoS Comput. Biol..
[10] C. Allis,et al. Chromatin remodeling and cancer, Part I: Covalent histone modifications. , 2007, Trends in molecular medicine.
[11] K. Kish,et al. Structural basis for CARM1 inhibition by indole and pyrazole inhibitors. , 2011, The Biochemical journal.
[12] Ruben Abagyan,et al. Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. , 2010, Chemistry & biology.
[13] R. Eglen,et al. Screening for Compounds That Modulate Epigenetic Regulation of the Transcriptome , 2011, Journal of biomolecular screening.
[14] S. Pang,et al. Pyrazole inhibitors of coactivator associated arginine methyltransferase 1 (CARM1). , 2008, Bioorganic & medicinal chemistry letters.
[15] Jonathan C. Fuller,et al. Predicting druggable binding sites at the protein-protein interface. , 2009, Drug discovery today.
[16] Nobuyoshi Sugaya,et al. Assessing the druggability of protein-protein interactions by a supervised machine-learning method , 2009, BMC Bioinformatics.
[17] A. Mills. Throwing the cancer switch: reciprocal roles of polycomb and trithorax proteins , 2010, Nature Reviews Cancer.
[18] G. Petsko,et al. Multiple solvent crystal structures: probing binding sites, plasticity and hydration. , 2006, Journal of molecular biology.
[19] D. Swinney,et al. How were new medicines discovered? , 2011, Nature Reviews Drug Discovery.
[20] D. Patel,et al. Histone H3 recognition and presentation by the WDR5 module of the MLL1 complex , 2006, Nature Structural &Molecular Biology.
[21] M. Duvic,et al. Selective induction of apoptosis by histone deacetylase inhibitor SAHA in cutaneous T-cell lymphoma cells: relevance to mechanism of therapeutic action. , 2005, The Journal of investigative dermatology.
[22] Chao Xu,et al. Binding of different histone marks differentially regulates the activity and specificity of polycomb repressive complex 2 (PRC2) , 2010, Proceedings of the National Academy of Sciences.
[23] D. Baker,et al. A simple physical model for binding energy hot spots in protein–protein complexes , 2002, Proceedings of the National Academy of Sciences of the United States of America.
[24] J. García,et al. Functional and quantitative proteomics using SILAC in cancer research , 2008 .
[25] Min Gyu Lee,et al. Histone H3 lysine 4 demethylation is a target of nonselective antidepressive medications. , 2006, Chemistry & biology.
[26] C. Arrowsmith,et al. Fluorescence-Based Methods for Screening Writers and Readers of Histone Methyl Marks , 2012, Journal of biomolecular screening.
[27] F. Sams-Dodd,et al. Drug discovery: selecting the optimal approach. , 2006, Drug discovery today.
[28] F. Pammolli,et al. The productivity crisis in pharmaceutical R&D , 2011, Nature Reviews Drug Discovery.
[29] P. Hajduk,et al. Druggability indices for protein targets derived from NMR-based screening data. , 2005, Journal of medicinal chemistry.
[30] A. Simeonov,et al. Methods for Activity Analysis of the Proteins that Regulate Histone Methylation , 2011, Current chemical genomics.
[31] M. Cosgrove,et al. Structure of WDR5 Bound to Mixed Lineage Leukemia Protein-1 Peptide* , 2008, Journal of Biological Chemistry.
[32] J. Snyder,et al. Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294 , 2009, Nature Structural &Molecular Biology.
[33] S. Lanouette,et al. Structural and biochemical insights into MLL1 core complex assembly. , 2011, Structure.
[34] R. Roeder,et al. HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. , 2000, Molecular cell.
[35] T. Berg. Small-molecule inhibitors of protein-protein interactions. , 2008, Current opinion in drug discovery & development.
[36] Ming-Ming Zhou,et al. A small molecule binding to the coactivator CREB-binding protein blocks apoptosis in cardiomyocytes. , 2011, Chemistry & biology.
[37] E. Li,et al. Epigenetics and Disease , 2011 .
[38] S. Knapp,et al. Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery. , 2011, Molecular bioSystems.
[39] D. Reinberg,et al. Role of the polycomb protein EED in the propagation of repressive histone marks , 2009, Nature.
[40] M. Bunnage. Getting pharmaceutical R&D back on target. , 2011, Nature chemical biology.
[41] Karl Mechtler,et al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. , 2007, Molecular cell.
[42] C. Allis,et al. Chromatin remodeling and cancer, Part II: ATP-dependent chromatin remodeling. , 2007, Trends in molecular medicine.
[43] R. Jaenisch,et al. Toxicity of 5-aza-2'-deoxycytidine to mammalian cells is mediated primarily by covalent trapping of DNA methyltransferase rather than DNA demethylation. , 1994, Proceedings of the National Academy of Sciences of the United States of America.
[44] C. Chung,et al. Progress in the Discovery of Small-Molecule Inhibitors of Bromodomain–Histone Interactions , 2011, Journal of biomolecular screening.
[45] William B. Smith,et al. Selective inhibition of BET bromodomains , 2010, Nature.
[46] Philip J. Hajduk,et al. Fragment-based lead discovery: challenges and opportunities , 2011, J. Comput. Aided Mol. Des..
[47] K. Parnell,et al. Epigenetic Drug Discovery , 2012, Journal of biomolecular screening.
[48] S. Schreiber,et al. A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases. , 2011, Journal of the American Chemical Society.
[49] S. Baylin,et al. Novel Oligoamine Analogues Inhibit Lysine-Specific Demethylase 1 and Induce Reexpression of Epigenetically Silenced Genes , 2009, Clinical Cancer Research.
[50] W. Sippl,et al. Computer- and structure-based lead design for epigenetic targets. , 2011, Bioorganic & medicinal chemistry.
[51] Ozlem Keskin,et al. HotSprint: database of computational hot spots in protein interfaces , 2007, Nucleic Acids Res..
[52] Paul A Clemons,et al. Complex phenotypic assays in high-throughput screening. , 2004, Current opinion in chemical biology.
[53] J. J. Jehring. The productivity crisis , 1967 .
[54] David C Fry,et al. Protein-protein interactions as targets for small molecule drug discovery. , 2006, Biopolymers.
[55] R. Jirtle,et al. Environmental epigenomics and disease susceptibility , 2007, Nature Reviews Genetics.
[56] Y. Dragan,et al. What do we need to know prior to thinking about incorporating an epigenetic evaluation into safety assessments? , 2010, Toxicological sciences : an official journal of the Society of Toxicology.
[57] P. Bamborough,et al. Discovery and characterization of small molecule inhibitors of the BET family bromodomains. , 2011, Journal of medicinal chemistry.
[58] J. Medina-Franco,et al. Advances in the computational development of DNA methyltransferase inhibitors. , 2011, Drug discovery today.
[59] Zhengwei Peng,et al. Druggability assessment of protein-protein interfaces. , 2011, Future medicinal chemistry.
[60] M. Mann,et al. A SILAC-based DNA protein interaction screen that identifies candidate binding proteins to functional DNA elements. , 2009, Genome research.
[61] R. Schneider-Stock,et al. Histone deacetylase inhibitors: signalling towards p21cip1/waf1. , 2007, The international journal of biochemistry & cell biology.
[62] P. Trojer,et al. Target-based approach to inhibitors of histone arginine methyltransferases. , 2007, Journal of medicinal chemistry.
[63] L. Vassilev,et al. In Vivo Activation of the p53 Pathway by Small-Molecule Antagonists of MDM2 , 2004, Science.
[64] Yong Chen,et al. Crystal structure of human histone lysine-specific demethylase 1 (LSD1) , 2006, Proceedings of the National Academy of Sciences.
[65] Richard M. Jackson,et al. Q-SiteFinder: an energy-based method for the prediction of protein-ligand binding sites , 2005, Bioinform..
[66] Anton V. Bieliauskas,et al. Isoform-Selective Histone Deacetylase Inhibitors , 2008 .
[67] Roberto Sanchez,et al. The role of human bromodomains in chromatin biology and gene transcription. , 2009, Current opinion in drug discovery & development.
[68] A. Wettstein. Fortschritte der Arzneimittelforschung , 1960, Experientia.
[69] Sean D. Taverna,et al. How chromatin-binding modules interpret histone modifications: lessons from professional pocket pickers , 2007, Nature Structural &Molecular Biology.
[70] N. Avvakumov,et al. The MYST family of histone acetyltransferases and their intimate links to cancer , 2007, Oncogene.
[71] Herbert Edelsbrunner,et al. Interface surfaces for protein-protein complexes , 2004, RECOMB.
[72] Peter A. Jones,et al. Targeting DNA methylation for epigenetic therapy. , 2010, Trends in pharmacological sciences.
[73] Jun Wang,et al. Small-Molecule Inhibition of TNF-α , 2005, Science.
[74] N. Keen,et al. Structural basis of substrate methylation and inhibition of SMYD2. , 2011, Structure.
[75] R. Higgs,et al. Small-molecule affinity chromatography coupled mass spectrometry for drug target deconvolution , 2009, Expert opinion on drug discovery.
[76] Hengbin Wang,et al. Role of Histone H3 Lysine 27 Methylation in Polycomb-Group Silencing , 2002, Science.
[77] S. Lampel,et al. The druggable genome: an update. , 2005, Drug discovery today.
[78] Makoto Hasegawa,et al. Identification of cell-active lysine specific demethylase 1-selective inhibitors. , 2009, Journal of the American Chemical Society.
[79] S. Pang,et al. Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)--Hit to Lead studies. , 2009, Bioorganic & medicinal chemistry letters.
[80] J. Buggy,et al. Isoform-specific histone deacetylase inhibitors: the next step? , 2009, Cancer letters.
[81] Huidong Shi,et al. Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor panobinostat against human AML cells. , 2009, Blood.
[82] E. Whitelaw,et al. Transgenerational epigenetic inheritance in health and disease. , 2008, Current opinion in genetics & development.
[83] Makoto Hasegawa,et al. Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors. , 2010, Journal of medicinal chemistry.
[84] Matthieu Schapira,et al. Structural genomics of histone tail recognition , 2010, Bioinform..
[85] Edwin Smith,et al. The Language of Histone Crosstalk , 2010, Cell.
[86] F. J. Luque,et al. Binding site detection and druggability index from first principles. , 2009, Journal of medicinal chemistry.
[87] P. Marks,et al. A class of hybrid polar inducers of transformed cell differentiation inhibits histone deacetylases. , 1998, Proceedings of the National Academy of Sciences of the United States of America.
[88] Albert J R Heck,et al. Revealing promiscuous drug-target interactions by chemical proteomics. , 2009, Drug discovery today.
[89] M. Szyf. Epigenetics, DNA methylation, and chromatin modifying drugs. , 2009, Annual review of pharmacology and toxicology.
[90] A. Jeltsch,et al. C5‐DNA Methyltransferase Inhibitors: From Screening to Effects on Zebrafish Embryo Development , 2011, Chembiochem : a European journal of chemical biology.
[91] J. Manfredi,et al. Target structure-based discovery of small molecules that block human p53 and CREB binding protein association. , 2006, Chemistry & biology.
[92] C. Rice,et al. Suppression of inflammation by a synthetic histone mimic , 2010, Nature.
[93] R A Rifkind,et al. Second generation hybrid polar compounds are potent inducers of transformed cell differentiation. , 1996, Proceedings of the National Academy of Sciences of the United States of America.
[94] Steven A Carr,et al. Identifying the proteins to which small-molecule probes and drugs bind in cells , 2009, Proceedings of the National Academy of Sciences.
[95] M. Schapira,et al. Finding Inspiration in the Protein Data Bank to Chemically Antagonize Readers of the Histone Code , 2010, Molecular informatics.
[96] Peter A. Jones,et al. Cellular differentiation, cytidine analogs and DNA methylation , 1980, Cell.
[97] S. Knapp,et al. 3,5-Dimethylisoxazoles Act As Acetyl-lysine-mimetic Bromodomain Ligands , 2011, Journal of medicinal chemistry.
[98] Sandor Vajda,et al. Identification of hot spots within druggable binding regions by computational solvent mapping of proteins. , 2007, Journal of medicinal chemistry.
[99] G. Perez,et al. Role of thioredoxin in the response of normal and transformed cells to histone deacetylase inhibitors. , 2005, Proceedings of the National Academy of Sciences of the United States of America.
[100] Tatjana Buklijas,et al. Epigenetic mechanisms that underpin metabolic and cardiovascular diseases , 2009, Nature Reviews Endocrinology.
[101] W. Sippl,et al. Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1. , 2011, Bioorganic & medicinal chemistry.
[102] Min Gyu Lee,et al. An essential role for CoREST in nucleosomal histone 3 lysine 4 demethylation , 2005, Nature.
[103] A. Hopkins,et al. The druggable genome , 2002, Nature Reviews Drug Discovery.
[104] S. Baylin,et al. Inhibition of lysine-specific demethylase 1 by polyamine analogues results in reexpression of aberrantly silenced genes , 2007, Proceedings of the National Academy of Sciences.
[105] P. Workman,et al. A duplexed phenotypic screen for the simultaneous detection of inhibitors of the molecular chaperone heat shock protein 90 and modulators of cellular acetylation , 2007, Molecular Cancer Therapeutics.
[106] John L Rinn,et al. RNA traffic control of chromatin complexes. , 2010, Current opinion in genetics & development.
[107] N. Reich,et al. DNA cytosine C5 methyltransferase Dnmt1: catalysis-dependent release of allosteric inhibition. , 2005, Biochemistry.
[108] F. Forneris,et al. Human Histone Demethylase LSD1 Reads the Histone Code* , 2005, Journal of Biological Chemistry.
[109] K. Morris,et al. Transcriptional gene silencing through epigenetic changes mediated by non-coding RNAs. , 2010, Current opinion in molecular therapeutics.
[110] D. Santi,et al. Covalent bond formation between a DNA-cytosine methyltransferase and DNA containing 5-azacytosine. , 1984, Proceedings of the National Academy of Sciences of the United States of America.
[111] Antoine H. F. M. Peters,et al. LSD1 demethylates repressive histone marks to promote androgen-receptor-dependent transcription , 2005, Nature.
[112] Ming-Ming Zhou,et al. Selective small molecules blocking HIV-1 Tat and coactivator PCAF association. , 2005, Journal of the American Chemical Society.
[113] R. Kingston,et al. WDR5 Interacts with Mixed Lineage Leukemia (MLL) Protein via the Histone H3-binding Pocket* , 2008, Journal of Biological Chemistry.
[114] Anton Simeonov,et al. Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a. , 2009, Journal of medicinal chemistry.
[115] Tim J. Wigle,et al. Screening for Inhibitors of Low-Affinity Epigenetic Peptide-Protein Interactions: An AlphaScreen™-Based Assay for Antagonists of Methyl-Lysine Binding Proteins , 2010, Journal of biomolecular screening.
[116] K. Helin,et al. Histone methyltransferases in cancer. , 2010, Seminars in cell & developmental biology.
[117] T. Ahrens,et al. Efficient Hit-Finding Approaches for Histone Methyltransferases , 2012, Journal of biomolecular screening.
[118] Bing Li,et al. Readers of histone modifications , 2011, Cell Research.
[119] A. Jadhav,et al. Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors , 2010, PloS one.
[120] R. Schneider,et al. Chatting histone modifications in mammals. , 2010, Briefings in functional genomics.
[121] Shiv k. Sharma,et al. (Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators. , 2010, Journal of medicinal chemistry.
[122] Ming-Ming Zhou,et al. Mechanism and Regulation of Acetylated Histone Binding by the Tandem PHD Finger of DPF3b , 2010, Nature.
[123] P. Grandi,et al. Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes , 2011, Nature Biotechnology.
[124] Yonghong Xiao,et al. Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor. , 2011, Cancer cell.
[125] J. Beutler,et al. Identification of Four Potential Epigenetic Modulators from the NCI Structural Diversity Library Using a Cell-Based Assay , 2010, Journal of biomedicine & biotechnology.
[126] N. Goodey,et al. Allosteric regulation and catalysis emerge via a common route. , 2008, Nature chemical biology.
[127] B. Strahl,et al. Influence of Combinatorial Histone Modifications on Antibody and Effector Protein Recognition , 2011, Current Biology.
[128] Jon R. Wilson,et al. Characterization of a Novel WDR5-binding Site That Recruits RbBP5 through a Conserved Motif to Enhance Methylation of Histone H3 Lysine 4 by Mixed Lineage Leukemia Protein-1* , 2010, The Journal of Biological Chemistry.
[129] Peter A. Jones,et al. Epigenetic Modifications as Therapeutic Targets , 2010, Nature Biotechnology.
[130] H. Haisma,et al. Histone acetyltransferases are crucial regulators in NF-κB mediated inflammation. , 2011, Drug discovery today.
[131] S. Frye,et al. Epigenetics: Tools and Technologies. , 2010, Drug discovery today. Technologies.
[132] S. Schreiber,et al. Identification of a Class of Small Molecule Inhibitors of the Sirtuin Family of NAD-dependent Deacetylases by Phenotypic Screening* , 2001, The Journal of Biological Chemistry.
[133] Akinori Sarai,et al. ProTherm and ProNIT: thermodynamic databases for proteins and protein–nucleic acid interactions , 2005, Nucleic Acids Res..
[134] W-S Xu,et al. Histone deacetylase inhibitors: Potential in cancer therapy , 2009, Journal of cellular biochemistry.
[135] Ramars Amanchy,et al. Phosphoproteome analysis of HeLa cells using stable isotope labeling with amino acids in cell culture (SILAC). , 2005, Journal of proteome research.
[136] T. Umehara,et al. Real-time imaging of histone H4K12-specific acetylation determines the modes of action of histone deacetylase and bromodomain inhibitors. , 2011, Chemistry & biology.
[137] Anton Simeonov,et al. Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. , 2010, Journal of medicinal chemistry.
[138] U. Oppermann,et al. Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. , 2008, Journal of medicinal chemistry.
[139] Craig W Lindsley,et al. Allosteric modulation of kinases and GPCRs: design principles and structural diversity. , 2008, Current opinion in chemical biology.
[140] Sydney L. Stoops,et al. Identification and optimization of small molecules that restore E-cadherin expression and reduce invasion in colorectal carcinoma cells. , 2011, ACS chemical biology.
[141] Takayoshi Suzuki,et al. Lysine demethylases inhibitors. , 2011, Journal of medicinal chemistry.
[142] M. Mann,et al. Identifying and quantifying in vivo methylation sites by heavy methyl SILAC , 2004, Nature Methods.
[143] C. Bronner,et al. The "Epigenetic Code Replication Machinery", ECREM: a promising drugable target of the epigenetic cell memory. , 2007, Current medicinal chemistry.
[144] Jian Jin,et al. Small-molecule ligands of methyl-lysine binding proteins. , 2011, Journal of medicinal chemistry.
[145] J. Chai,et al. Structural basis of EZH2 recognition by EED. , 2007, Structure.
[146] G. Terstappen,et al. Target deconvolution strategies in drug discovery , 2007, Nature Reviews Drug Discovery.
[147] Randall W King,et al. Small Molecule Regulators of Protein Arginine Methyltransferases* , 2004, Journal of Biological Chemistry.
[148] Daniel Cressey,et al. Traditional drug-discovery model ripe for reform , 2011, Nature.
[149] Andrew J. Bannister,et al. Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity , 2005, Molecular Cancer Therapeutics.