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
KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative disease
Tamara Maes,Cristina Mascaró,Alberto Ortega,Serena Lunardi,Filippo Ciceri,Tim C. P. Somervaille,Carlos Buesa +6 more
TL;DR: A decade after the identification of KDM1A as a histone demethylase, the first selective inhibitors have now reached the clinic, offering additional opportunities for the development of novel therapeutic strategies in neurodegenerative disease.
Journal ArticleDOI
Discovery of [1,2,3]Triazolo[4,5-d]pyrimidine Derivatives as Novel LSD1 Inhibitors
Zhong-Hua Li,Xue-Qi Liu,Peng-Fei Geng,Feng-Zhi Suo,Jin-Lian Ma,Bin Yu,Tao-Qian Zhao,Zhao-Qing Zhou,Chen-Xi Huang,Yi-Chao Zheng,Hong-Min Liu +10 more
TL;DR: The [1,2,3]triazolo[4,5-d]pyrimidine scaffold can be used as the template for designing new LSD1 inhibitors and docking studies indicated that the hydrogen interaction between the nitrogen atom in the pyridine ring and Met332 could be responsible for the improved activity of 2-thiopyridine series.
Journal ArticleDOI
Development of the triazole-fused pyrimidine derivatives as highly potent and reversible inhibitors of histone lysine specific demethylase 1 (LSD1/KDM1A)
Zhong-Hua Li,Zhong-Hua Li,Lina Ding,Lina Ding,Zhong-Rui Li,Zhong-Rui Li,Zhi-Zheng Wang,Zhi-Zheng Wang,Feng-Zhi Suo,Feng-Zhi Suo,Dan-Dan Shen,Dan-Dan Shen,Tao-Qian Zhao,Tao-Qian Zhao,Xu-Dong Sun,Xu-Dong Sun,Jun-Wei Wang,Jun-Wei Wang,Ying Liu,Ying Liu,Li-Ying Ma,Li-Ying Ma,Bing Zhao,Bing Zhao,Peng-Fei Geng,Peng-Fei Geng,Bin Yu,Yi-Chao Zheng,Yi-Chao Zheng,Hong-Min Liu,Hong-Min Liu +30 more
TL;DR: The discovery of the hit compound 8a and further medicinal chemistry efforts, leading to the generation of compound 15u, which inhibited LSD1 reversibly and competitively with H3K4me2, and was selective to LSD1 over MAO-A/B, indicate that targeting LSD1 is a promising strategy for AML treatment and the triazole-fused pyrimidine derivatives are new scaffolds for the development of LSD1/KDM1A inhibitors.
Journal ArticleDOI
LSD1 cooperates with CTIP2 to promote HIV-1 transcriptional silencing
Valentin Le Douce,Laurence Colin,Laetitia Redel,Thomas Cherrier,Georges Herbein,Dominique Aunis,Olivier Rohr,Carine Van Lint,Christian Schwartz +8 more
TL;DR: It is reported that the histone demethylase LSD1 represses HIV-1 transcription and viral expression in a synergistic manner with CTIP2, and it is suggested that LSD1-induced H3K4 trimethylation is linked to hSET1 recruitment at the integrated provirus.
Journal ArticleDOI
Leaving a mark: the many footprints of the elongating RNA polymerase II.
TL;DR: The role for RNA polymerase II elongation in targeting chromatin modifications to include a histone methyl mark more commonly associated with gene silencing is expanded.
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.
Journal ArticleDOI
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.