Structure‐Based Design of a New Scaffold for Cell‐Penetrating Peptidic Inhibitors of the Histone Demethylase PHF8
Sign Up to like & getrecommendations! Published in 2017 at "ChemBioChem"
DOI: 10.1002/cbic.201700109
Abstract: The histone demethylase PHF8 catalyzes demethylation of mono‐ and di‐methylated Lys9 on histone H3 (H3K9me1/2), and is a transcriptional activator involved in the development and cancer. Affinity and specificity of PHF8 towards H3K9me2 is affected… read more here.
Keywords: demethylase phf8; histone demethylase; structure based; cell penetrating ... See more keywords
Palmitate‐TLR4 signaling regulates the histone demethylase, JMJD3, in macrophages and impairs diabetic wound healing
Sign Up to like & getrecommendations! Published in 2020 at "European Journal of Immunology"
DOI: 10.1002/eji.202048651
Abstract: Chronic macrophage inflammation is a hallmark of type 2 diabetes (T2D) and linked to the development of secondary diabetic complications. T2D is characterized by excess concentrations of saturated fatty acids (SFA) that activate innate immune… read more here.
Keywords: jmjd3; histone demethylase; palmitate; inflammation ... See more keywords
GSK-J4: An H3K27 histone demethylase inhibitor, as a potential anti-cancer agent.
Sign Up to like & getrecommendations! Published in 2023 at "International journal of cancer"
DOI: 10.1002/ijc.34559
Abstract: Aberrant epigenetic modifications are emerging as potent drivers of tumor initiation and progression. The deregulation of H3K27me3 marks has shown to play an important role in cancer progression in several cancers. The H3K27me3 mark is… read more here.
Keywords: demethylase inhibitor; cancer; anti cancer; histone demethylase ... See more keywords
Targeting histone demethylase KDM5B for cancer treatment.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112760
Abstract: KDM5B (Lysine-Specific Demethylase 5B) erases the methyl group from H3K4me2/3, which performs wide regulatory effects on chromatin structure, and represses the transcriptional function of genes. KDM5B functions as an oncogene and associates with human cancers… read more here.
Keywords: histone demethylase; kdm5b; cancer; targeting histone ... See more keywords
Oncogenic and osteolytic functions of histone demethylase NO66 in castration-resistant prostate cancer
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DOI: 10.1038/s41388-019-0774-x
Abstract: Epigenetic changes that cause dysregulated gene expression during progression of androgen-independent prostate cancer (PCa) and metastatic skeletal lesions remain elusive. Here, we explored the role of histone demethylase NO66 in the pathogenesis of PCa and… read more here.
Keywords: prostate; histone demethylase; demethylase no66; prostate cancer ... See more keywords
Histone demethylase KDM4D inhibition suppresses renal cancer progression and angiogenesis through JAG1 signaling.
Sign Up to like & getrecommendations! Published in 2021 at "Cell death discovery"
DOI: 10.1038/s41420-021-00682-y
Abstract: Kidney cancer, especially clear cell renal cell carcinoma (ccRCC), is one of the representative genitourinary tumors. Investigation of underlying mechanisms of ccRCC development is crucial for patient management. Histone demethylase KDM4D has been reported to… read more here.
Keywords: ccrcc; histone demethylase; cancer; demethylase kdm4d ... See more keywords
The histone demethylase Phf2 acts as a molecular checkpoint to prevent NAFLD progression during obesity
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DOI: 10.1038/s41467-018-04361-y
Abstract: Aberrant histone methylation profile is reported to correlate with the development and progression of NAFLD during obesity. However, the identification of specific epigenetic modifiers involved in this process remains poorly understood. Here, we identify the… read more here.
Keywords: obesity; progression; histone demethylase; checkpoint ... See more keywords
The histone demethylase KDM6B fine-tunes the host response to Streptococcus pneumoniae
Sign Up to like & getrecommendations! Published in 2020 at "Nature Microbiology"
DOI: 10.1038/s41564-020-00805-8
Abstract: Streptococcus pneumoniae is a natural colonizer of the human respiratory tract and an opportunistic pathogen. Although epithelial cells are among the first to encounter pneumococci, the cellular processes and contribution of epithelial cells to the… read more here.
Keywords: histone demethylase; response; host response; streptococcus pneumoniae ... See more keywords
KDM4B histone demethylase and G9a regulate expression of vascular adhesion proteins in cerebral microvessels
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DOI: 10.1038/srep45005
Abstract: Intercellular adhesion molecule 1 (ICAM1) mediates the adhesion and transmigration of leukocytes across the endothelium, promoting inflammation. We investigated the epigenetic mechanism regulating ICAM1 expression. The pro-inflammatory cytokine TNF-α dramatically increased ICAM1 mRNA and protein… read more here.
Keywords: histone demethylase; kdm4b histone; adhesion; expression ... See more keywords
The histone demethylase JMJD2B regulates endothelial-to-mesenchymal transition
Sign Up to like & getrecommendations! Published in 2020 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.1913481117
Abstract: Significance Here we show that the histone demethylase JMJD2B is induced in endothelial cells by EndMT provoking stimuli and thereby contributes to the acquirement of a mesenchymal/smooth muscle phenotype. Silencing of JMJD2B inhibited EndMT in… read more here.
Keywords: demethylase jmjd2b; endothelial cells; histone demethylase; jmjd2b ... See more keywords
Nuclear-localized, iron-bound superoxide dismutase-2 antagonizes epithelial lineage programs to promote stemness of breast cancer cells via a histone demethylase activity
Sign Up to like & getrecommendations! Published in 2022 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2110348119
Abstract: Significance The main finding reported here is that acetylation converts superoxide dismutase-2 (SOD2) from a mitochondrial antioxidant to a nuclear histone demethylase. The change in function involves the binding of iron instead of the canonical… read more here.
Keywords: iron; superoxide dismutase; histone demethylase; histone ... See more keywords