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https://www.readbyqxmd.com/read/27882807/jarid1-kdm5-demethylases-as-cancer-targets
#1
Joyce Taylor-Papadimitriou, Joy Burchell
No abstract text is available yet for this article.
November 24, 2016: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/27548260/kdmb-a-jumonji-histone-h3-demethylase-regulates-genome-wide-h3k4-trimethylation-and-is-required-for-normal-induction-of-secondary-metabolism-in-aspergillus-nidulans
#2
Agnieszka Gacek-Matthews, Harald Berger, Takahiko Sasaki, Kathrin Wittstein, Clemens Gruber, Zachary A Lewis, Joseph Strauss
Histone posttranslational modifications (HPTMs) are involved in chromatin-based regulation of fungal secondary metabolite biosynthesis (SMB) in which the corresponding genes-usually physically linked in co-regulated clusters-are silenced under optimal physiological conditions (nutrient-rich) but are activated when nutrients are limiting. The exact molecular mechanisms by which HPTMs influence silencing and activation, however, are still to be better understood. Here we show by a combined approach of quantitative mass spectrometry (LC-MS/MS), genome-wide chromatin immunoprecipitation (ChIP-seq) and transcriptional network analysis (RNA-seq) that the core regions of silent A...
August 2016: PLoS Genetics
https://www.readbyqxmd.com/read/27427228/structural-basis-for-kdm5a-histone-lysine-demethylase-inhibition-by-diverse-compounds
#3
John R Horton, Xu Liu, Molly Gale, Lizhen Wu, John R Shanks, Xing Zhang, Philip J Webber, Joshua S K Bell, Stephen C Kales, Bryan T Mott, Ganesha Rai, Daniel J Jansen, Mark J Henderson, Daniel J Urban, Matthew D Hall, Anton Simeonov, David J Maloney, Margaret A Johns, Haian Fu, Ajit Jadhav, Paula M Vertino, Qin Yan, Xiaodong Cheng
The KDM5/JARID1 family of Fe(II)- and α-ketoglutarate-dependent demethylases removes methyl groups from methylated lysine 4 of histone H3. Accumulating evidence supports a role for KDM5 family members as oncogenic drivers. We compare the in vitro inhibitory properties and binding affinity of ten diverse compounds with all four family members, and present the crystal structures of the KDM5A-linked Jumonji domain in complex with eight of these inhibitors in the presence of Mn(II). All eight inhibitors structurally examined occupy the binding site of α-ketoglutarate, but differ in their specific binding interactions, including the number of ligands involved in metal coordination...
July 21, 2016: Cell Chemical Biology
https://www.readbyqxmd.com/read/27214403/structural-analysis-of-human-kdm5b-guides-histone-demethylase-inhibitor-development
#4
Catrine Johansson, Srikannathasan Velupillai, Anthony Tumber, Aleksandra Szykowska, Edward S Hookway, Radoslaw P Nowak, Claire Strain-Damerell, Carina Gileadi, Martin Philpott, Nicola Burgess-Brown, Na Wu, Jola Kopec, Andrea Nuzzi, Holger Steuber, Ursula Egner, Volker Badock, Shonagh Munro, Nicholas B LaThangue, Sue Westaway, Jack Brown, Nick Athanasou, Rab Prinjha, Paul E Brennan, Udo Oppermann
Members of the KDM5 (also known as JARID1) family are 2-oxoglutarate- and Fe(2+)-dependent oxygenases that act as histone H3K4 demethylases, thereby regulating cell proliferation and stem cell self-renewal and differentiation. Here we report crystal structures of the catalytic core of the human KDM5B enzyme in complex with three inhibitor chemotypes. These scaffolds exploit several aspects of the KDM5 active site, and their selectivity profiles reflect their hybrid features with respect to the KDM4 and KDM6 families...
July 2016: Nature Chemical Biology
https://www.readbyqxmd.com/read/26741168/8-substituted-pyrido-3-4-d-pyrimidin-4-3h-one-derivatives-as-potent-cell-permeable-kdm4-jmjd2-and-kdm5-jarid1-histone-lysine-demethylase-inhibitors
#5
Vassilios Bavetsias, Rachel M Lanigan, Gian Filippo Ruda, Butrus Atrash, Mark G McLaughlin, Anthony Tumber, N Yi Mok, Yann-Vaï Le Bihan, Sally Dempster, Katherine J Boxall, Fiona Jeganathan, Stephanie B Hatch, Pavel Savitsky, Srikannathasan Velupillai, Tobias Krojer, Katherine S England, Jimmy Sejberg, Ching Thai, Adam Donovan, Akos Pal, Giuseppe Scozzafava, James M Bennett, Akane Kawamura, Catrine Johansson, Aleksandra Szykowska, Carina Gileadi, Nicola A Burgess-Brown, Frank von Delft, Udo Oppermann, Zoe Walters, Janet Shipley, Florence I Raynaud, Susan M Westaway, Rab K Prinjha, Oleg Fedorov, Rosemary Burke, Christopher J Schofield, Isaac M Westwood, Chas Bountra, Susanne Müller, Rob L M van Montfort, Paul E Brennan, Julian Blagg
We report the discovery of N-substituted 4-(pyridin-2-yl)thiazole-2-amine derivatives and their subsequent optimization, guided by structure-based design, to give 8-(1H-pyrazol-3-yl)pyrido[3,4-d]pyrimidin-4(3H)-ones, a series of potent JmjC histone N-methyl lysine demethylase (KDM) inhibitors which bind to Fe(II) in the active site. Substitution from C4 of the pyrazole moiety allows access to the histone peptide substrate binding site; incorporation of a conformationally constrained 4-phenylpiperidine linker gives derivatives such as 54j and 54k which demonstrate equipotent activity versus the KDM4 (JMJD2) and KDM5 (JARID1) subfamily demethylases, selectivity over representative exemplars of the KDM2, KDM3, and KDM6 subfamilies, cellular permeability in the Caco-2 assay, and, for 54k, inhibition of H3K9Me3 and H3K4Me3 demethylation in a cell-based assay...
February 25, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/26645689/characterization-of-a-linked-jumonji-domain-of-the-kdm5-jarid1-family-of-histone-h3-lysine-4-demethylases
#6
John R Horton, Amanda Engstrom, Elizabeth L Zoeller, Xu Liu, John R Shanks, Xing Zhang, Margaret A Johns, Paula M Vertino, Haian Fu, Xiaodong Cheng
The KDM5/JARID1 family of Fe(II)- and α-ketoglutarate-dependent demethylases remove methyl groups from tri- and dimethylated lysine 4 of histone H3. Accumulating evidence from primary tumors and model systems supports a role for KDM5A (JARID1A/RBP2) and KDM5B (JARID1B/PLU1) as oncogenic drivers. The KDM5 family is unique among the Jumonji domain-containing histone demethylases in that there is an atypical insertion of a DNA-binding ARID domain and a histone-binding PHD domain into the Jumonji domain, which separates the catalytic domain into two fragments (JmjN and JmjC)...
February 5, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/25537453/dynamic-epigenetic-regulation-by-menin-during-pancreatic-islet-tumor-formation
#7
Wenchu Lin, Hideo Watanabe, Shouyong Peng, Joshua M Francis, Nathan Kaplan, Chandra Sekhar Pedamallu, Aruna Ramachandran, Agoston Agoston, Adam J Bass, Matthew Meyerson
UNLABELLED: The tumor suppressor gene MEN1 is frequently mutated in sporadic pancreatic neuroendocrine tumors (PanNET) and is responsible for the familial multiple endocrine neoplasia type 1 (MEN-1) cancer syndrome. Menin, the protein product of MEN1, associates with the histone methyltransferases (HMT) MLL1 (KMT2A) and MLL4 (KMT2B) to form menin-HMT complexes in both human and mouse model systems. To elucidate the role of methylation of histone H3 at lysine 4 (H3K4) mediated by menin-HMT complexes during PanNET formation, genome-wide histone H3 lysine 4 trimethylation (H3K4me3) signals were mapped in pancreatic islets using unbiased chromatin immunoprecipitation coupled with next-generation sequencing (ChIP-seq)...
April 2015: Molecular Cancer Research: MCR
https://www.readbyqxmd.com/read/25248920/yeast-histone-h3-lysine-4-demethylase-jhd2-regulates-mitotic-rdna-condensation
#8
Hong-Yeoul Ryu, Seong Ahn
BACKGROUND: Nucleolar rDNA is tightly associated with silent heterochromatin, which is important for rDNA stability, nucleolar integration, and cellular senescence. Two pathways have been described that lead to rDNA silencing in yeast: 1) the RENT (regulator of nucleolar silencing and telophase exit) complex, which is composed of Net1, Sir2, and Cdc14 and is required for Sir2-dependent rDNA silencing; and 2) the Sir2-independent silencing mechanism, which involves the Tof2 and Tof2-copurified complex, made up of Lrs4 and Csm1...
2014: BMC Biology
https://www.readbyqxmd.com/read/23872847/targeting-h3k4-trimethylation-in-huntington-disease
#9
Malini Vashishtha, Christopher W Ng, Ferah Yildirim, Theresa A Gipson, Ian H Kratter, Laszlo Bodai, Wan Song, Alice Lau, Adam Labadorf, Annie Vogel-Ciernia, Juan Troncosco, Christopher A Ross, Gillian P Bates, Dimitri Krainc, Ghazaleh Sadri-Vakili, Steven Finkbeiner, J Lawrence Marsh, David E Housman, Ernest Fraenkel, Leslie M Thompson
Transcriptional dysregulation is an early feature of Huntington disease (HD). We observed gene-specific changes in histone H3 lysine 4 trimethylation (H3K4me3) at transcriptionally repressed promoters in R6/2 mouse and human HD brain. Genome-wide analysis showed a chromatin signature for this mark. Reducing the levels of the H3K4 demethylase SMCX/Jarid1c in primary neurons reversed down-regulation of key neuronal genes caused by mutant Huntingtin expression. Finally, reduction of SMCX/Jarid1c in primary neurons from BACHD mice or the single Jarid1 in a Drosophila HD model was protective...
August 6, 2013: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/23408432/identification-of-small-molecule-inhibitors-of-jumonji-at-rich-interactive-domain-1b-jarid1b-histone-demethylase-by-a-sensitive-high-throughput-screen
#10
Joyce Sayegh, Jian Cao, Mike Ran Zou, Alfonso Morales, Lauren P Blair, Michael Norcia, Denton Hoyer, Alan J Tackett, Jane S Merkel, Qin Yan
JARID1B (also known as KDM5B or PLU1) is a member of the JARID1 family of histone lysine demethylases responsible for the demethylation of trimethylated lysine 27 in histone H3 (H3K4me3), a mark for actively transcribed genes. JARID1B is overexpressed in several cancers, including breast cancer, prostate cancer, and lung cancer. In addition, JARID1B is required for mammary tumor formation in syngeneic or xenograft mouse models. JARID1B-expressing melanoma cells are associated with increased self-renewal character...
March 29, 2013: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/23123093/timing-of-transcriptional-quiescence-during-gametogenesis-is-controlled-by-global-histone-h3k4-demethylation
#11
Mengshu Xu, Maria Soloveychik, Mathieu Ranger, Michael Schertzberg, Zarna Shah, Ryan Raisner, Shivkumar Venkatasubrahmanyan, Kyle Tsui, Marinella Gebbia, Tim Hughes, Harm van Bakel, Corey Nislow, Hiten D Madhani, Marc D Meneghini
Gametes are among the most highly specialized cells produced during development. Although gametogenesis culminates in transcriptional quiescence in plants and animals, regulatory mechanisms controlling this are unknown. Here, we confirm that gamete differentiation in the single-celled yeast Saccharomyces cerevisiae is accompanied by global transcriptional shutoff following the completion of meiosis. We show that Jhd2, a highly conserved JARID1-family histone H3K4 demethylase, activates protein-coding gene transcription in opposition to this programmed transcriptional shutoff, sustaining the period of productive transcription during spore differentiation...
November 13, 2012: Developmental Cell
https://www.readbyqxmd.com/read/22555401/overexpression-of-a-histone-h3k4-demethylase-jmj15-accelerates-flowering-time-in-arabidopsis
#12
Hongchun Yang, Huixian Mo, Di Fan, Ying Cao, Sujuan Cui, Ligeng Ma
UNLABELLED: The methylation of histone 3 lysine 4 (H3K4) is essential for gene activation. Flowering Locus C (FLC), an important flowering repressor, quantitatively regulates flowering time in Arabidopsis and its expression level is coincident with H3K4 trimethylation (H3K4me3) dynamics. The methylation state of FLC chromatin is determined by the balance between methylation and demethylation, which is mediated by histone methyltransferases and demethylases, respectively. However, little is known about the role of histone demethylase(s) in FLC regulation...
July 2012: Plant Cell Reports
https://www.readbyqxmd.com/read/22468166/effects-of-histone-deacetylase-inhibitors-on-modulating-h3k4-methylation-marks-a-novel-cross-talk-mechanism-between-histone-modifying-enzymes
#13
Po-Hsien Huang, Christoph Plass, Ching-Shih Chen
A recent study reports that histone deacetylase (HDAC) inhibitors, AR42 and MS- 275, upregulated H3K4 methylation marks in prostate cancer cells, leading to transcriptional activation of genes including those associated with roles in tumor suppression and cell differentiation (1). Evidence suggests that the crosstalk between histone deacetylation and histone H3K4 methylation is attributable to the ability of these HDAC inhibitors to repress the JARID1 family of histone H3 lysine 4 demethylases (H3K4DMs), including RBP2, PLU-1, SMCX, and LSD1, through the downregulation of Sp1 expression...
2011: Molecular and Cellular Pharmacology
https://www.readbyqxmd.com/read/21544224/epigenetic-regulation-by-lysine-demethylase-5-kdm5-enzymes-in-cancer
#14
Lauren P Blair, Jian Cao, Mike Ran Zou, Joyce Sayegh, Qin Yan
Similar to genetic alterations, epigenetic aberrations contribute significantly to tumor initiation and progression. In many cases, these changes are caused by activation or inactivation of the regulators that maintain epigenetic states. Here we review our current knowledge on the KDM5/JARID1 family of histone demethylases. This family of enzymes contains a JmjC domain and is capable of removing tri- and di- methyl marks from lysine 4 on histone H3. Among these proteins, RBP2 mediates drug resistance while JARID1B is required for melanoma maintenance...
March 1, 2011: Cancers
https://www.readbyqxmd.com/read/21369698/plu-1-jarid1b-kdm5b-is-required-for-embryonic-survival-and-contributes-to-cell-proliferation-in-the-mammary-gland-and-in-er-breast-cancer-cells
#15
Steven Catchpole, Bradley Spencer-Dene, Debbie Hall, Samantha Santangelo, Ian Rosewell, Mounia Guenatri, Richard Beatson, Angelo G Scibetta, Joy M Burchell, Joyce Taylor-Papadimitriou
The four members of the JARID1/KDM5 family of proteins, a sub-group of the larger ARID (AT rich DNA binding domain) family, have been shown to demethylate trimethylated lysine 4 on histone 3 (H3K4me3), a chromatin mark associated with actively transcribed genes. In some lower organisms a single homologue of JARID1 is found, and functions of the four proteins found in mice and humans may be specific or overlapping. To investigate the function of the Jarid1B protein we examined the effects of deletion of the gene in mice...
May 2011: International Journal of Oncology
https://www.readbyqxmd.com/read/20959362/histone-deacetylase-inhibitors-stimulate-histone-h3-lysine-4-methylation-in-part-via-transcriptional-repression-of-histone-h3-lysine-4-demethylases
#16
COMPARATIVE STUDY
Po-Hsien Huang, Chun-Han Chen, Chih-Chien Chou, Aaron M Sargeant, Samuel K Kulp, Che-Ming Teng, John C Byrd, Ching-Shih Chen
This study investigates the mechanism by which histone deacetylase (HDAC) inhibitors up-regulate histone H3 lysine 4 (H3K4) methylation. Exposure of LNCaP prostate cancer cells and the prostate tissue of transgenic adenocarcinoma of the mouse prostate mice to the pan- and class I HDAC inhibitors (S)-(+)-N-hydroxy-4-(3-methyl-2-phenyl-butyrylamino)-benzamide (AR42), N-(2-aminophenyl)-4-[N-(pyridine-3-yl-methoxycarbonyl)-aminomethyl]-benzamide (MS-275), and vorinostat led to differential increases in H3K4 methylation...
January 2011: Molecular Pharmacology
https://www.readbyqxmd.com/read/20858896/activity-of-a-c-terminal-plant-homeodomain-phd-of-msc1-is-essential-for-function
#17
Xinxing Qiu, Barbara E Dul, Nancy C Walworth
Msc1, a member of the Jarid1 family of putative histone demethylases, is required for chromosome stability in fission yeast. Msc1 associates with the Swr1 complex that facilitates deposition of histone H2A.Z into chromatin. To assess the function of Msc1 in the Swr1 complex, domains of Msc1 necessary for interaction with Swr1 were identified. The C-terminal plant homeodomain (PHD) 2 and PHD3 of Msc1 are sufficient to confer association with Swr1 and allow Msc1 to function in the context of kinetochore mutants...
November 19, 2010: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/19911051/the-schizosaccharomyces-pombe-jmjc-protein-msc1-prevents-h2a-z-localization-in-centromeric-and-subtelomeric-chromatin-domains
#18
Luke Buchanan, Mickaël Durand-Dubief, Assen Roguev, Cagri Sakalar, Brian Wilhelm, Annelie Strålfors, Anna Shevchenko, Rein Aasland, Andrej Shevchenko, Karl Ekwall, A Francis Stewart
Eukaryotic genomes are repetitively packaged into chromatin by nucleosomes, however they are regulated by the differences between nucleosomes, which establish various chromatin states. Local chromatin cues direct the inheritance and propagation of chromatin status via self-reinforcing epigenetic mechanisms. Replication-independent histone exchange could potentially perturb chromatin status if histone exchange chaperones, such as Swr1C, loaded histone variants into wrong sites. Here we show that in Schizosaccharomyces pombe, like Saccharomyces cerevisiae, Swr1C is required for loading H2A...
November 2009: PLoS Genetics
https://www.readbyqxmd.com/read/19346402/polyubiquitination-of-the-demethylase-jhd2-controls-histone-methylation-and-gene-expression
#19
Douglas P Mersman, Hai-Ning Du, Ian M Fingerman, Paul F South, Scott D Briggs
The identification of histone methyltransferases and demethylases has uncovered a dynamic methylation system needed to modulate appropriate levels of gene expression. Gene expression levels of various histone demethylases, such as the JARID1 family, show distinct patterns of embryonic and adult expression and respond to different environmental cues, suggesting that histone demethylase protein levels must be tightly regulated for proper development. In our study, we show that the protein level of the yeast histone H3 Lys 4 (H3 K4) demethylase Jhd2/Kdm5 is modulated through polyubiquitination by the E3 ubiquitin ligase Not4 and turnover by the proteasome...
April 15, 2009: Genes & Development
https://www.readbyqxmd.com/read/18375980/characterization-of-drosophila-melanogaster-jmjc-n-histone-demethylases
#20
Marta Lloret-Llinares, Clément Carré, Alejandro Vaquero, Natalia de Olano, Fernando Azorín
In this article, we characterize histone demethylase activity of the entire family of JmjC+N proteins of Drosophila melanogaster. Our results show that Lid (little imaginal discs), which is structurally homologous to JARID1, demethylates H3K4me3. However, contrary to what would be inferred from its demethylase activity, lid contributes to the establishment of transcriptionally competent chromatin states as: (i) is required for histone H3 acetylation; (ii) contributes to expression of the homoeotic gene Ultrabithorax (Ubx); and (iii) antagonizes heterochromatin-mediated gene silencing (PEV)...
May 2008: Nucleic Acids Research
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