PatentDOI
Histone demethylation mediated by the nuclear amine oxidase homolog lsd1
Yang Shi,Yujiang Shi +1 more
TLDR
In this paper, the authors identify a histone demethylase conserved from S. pombe to human and reveal dynamic regulation of histone methylation by both histonemethylases and demethylases.About:
This article is published in Cell.The article was published on 2005-12-16. It has received 3281 citations till now. The article focuses on the topics: Histone lysine demethylation & Histone demethylation.read more
Citations
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Journal ArticleDOI
Cross-talk between Histone Modifications in Response to Histone Deacetylase Inhibitors MLL4 LINKS HISTONE H3 ACETYLATION AND HISTONE H3K4 METHYLATION
Karl P. Nightingale,Susanne Gendreizig,Darren A. White,Charlotte Bradbury,Florian Hollfelder,Bryan M. Turner +5 more
TL;DR: Using histone modification-specific antibodies to demonstrate that two histone modifications involved in gene activation, histone H3 acetylation and H3 lysine 4 methylation, are functionally linked, shows that the abundance of H3K4 methylation is regulated by the activities of two opposing enzyme activities.
Journal ArticleDOI
Structural basis of histone demethylation by LSD1 revealed by suicide inactivation
Maojun Yang,Jeffrey C. Culhane,Lawrence M. Szewczuk,Christian B. Gocke,Chad A. Brautigam,Diana R. Tomchick,Mischa Machius,Philip A. Cole,Hongtao Yu +8 more
TL;DR: The crystal structure of human LSD1 with a propargylamine-derivatized H3 peptide covalently tethered to FAD is reported and the unusual backbone conformation of LSD1-bound H3 suggests a strategy for designing potent LSD1 inhibitors with therapeutic potential.
Journal ArticleDOI
ORY-1001, a Potent and Selective Covalent KDM1A Inhibitor, for the Treatment of Acute Leukemia
Tamara Maes,Cristina Mascaró,Iñigo Tirapu,Angels Estiarte,Filippo Ciceri,Serena Lunardi,Nathalie Guibourt,Alvaro Perdones,Michele M.P. Lufino,Tim C. P. Somervaille,Daniel H. Wiseman,Cihangir Duy,Ari Melnick,Christophe Willekens,Alberto Ortega,Marc Martinell,Nuria Valls,Guido Kurz,Matthew Colin Thor Fyfe,Julio Cesar Castro-Palomino,Carlos Buesa +20 more
TL;DR: ORY-1001 exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of an AML xenograft model, and extends survival in a mouse PDX model of T cell acute leukemia.
REVIEW The Dynamic Epigenome and its Implications in Toxicology
TL;DR: In this article, it is proposed that exposure to different environmental agents could lead to interindividual phenotypic diversity as well as differential susceptibility to disease and behavioral pathologies, and interindividual differences in the epigenetic state could also affect susceptibility to xenobiotics.
Journal ArticleDOI
The Dynamic Epigenome and its Implications in Toxicology
TL;DR: It is proposed that exposures to different environmental agents could lead to interindividual phenotypic diversity as well as differential susceptibility to disease and behavioral pathologies.
References
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Journal ArticleDOI
Translating the Histone Code
Thomas Jenuwein,C. David Allis +1 more
TL;DR: It is proposed that this epigenetic marking system represents a fundamental regulatory mechanism that has an impact on most, if not all, chromatin-templated processes, with far-reaching consequences for cell fate decisions and both normal and pathological development.
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Role of Histone H3 Lysine 27 Methylation in Polycomb-Group Silencing
Ru Cao,Liangjun Wang,Hengbin Wang,Li Xia,Hediye Erdjument-Bromage,Paul Tempst,Richard S. Jones,Yi Zhang +7 more
TL;DR: The purification and characterization of an EED-EZH2 complex, the human counterpart of the Drosophila ESC-E(Z) complex, is reported, and it is demonstrated that the complex specifically methylates nucleosomal histone H3 at lysine 27 (H3-K27).
Journal ArticleDOI
Methylation of histone H3 lysine 9 creates a binding site for HP1 proteins.
TL;DR: It is shown that mammalian methyltransferases that selectively methylate histone H3 on lysine 9 (Suv39h HMTases) generate a binding site for HP1 proteins—a family of heterochromatic adaptor molecules implicated in both gene silencing and supra-nucleosomal chromatin structure.
Journal ArticleDOI
Selective recognition of methylated lysine 9 on histone H3 by the HP1 chromo domain.
Andrew J. Bannister,Philip Zegerman,Janet F. Partridge,Eric A. Miska,Jean O. Thomas,Robin C. Allshire,Tony Kouzarides +6 more
TL;DR: A stepwise model for the formation of a transcriptionally silent heterochromatin is provided: SUV39H1 places a ‘methyl marker’ on histone H3, which is then recognized by HP1 through its chromo domain, which may also explain the stable inheritance of theheterochromatic state.
Journal ArticleDOI
Regulation of chromatin structure by site-specific histone H3 methyltransferases
Stephen Rea,Frank Eisenhaber,Dónal O'Carroll,Brian D. Strahl,Zu-Wen Sun,Manfred Schmid,Susanne Opravil,Karl Mechtler,Chris P. Ponting,C D Allis,Thomas Jenuwein +10 more
TL;DR: A functional interdependence of site-specific H3 tail modifications is revealed and a dynamic mechanism for the regulation of higher-order chromatin is suggested.