Chromatin/Epigenetics
Epigenetics is the heritable modifications in gene expression that is not associated with changes in DNA sequence. Epigenetic modifications occur mostly on DNA or on the histone octamer. There are several types of epigenetics modifications, DNA methylation by DNA-methyl transferase (DNMT) and covalent modification of histones (e.g. acetylation, methylation, phosphorylation and ubiquitination). Histone acetylation by histone acetyltransferases (HATs) is involved in transcriptional activation, whereas histone deacetylation by histone deacetylases (HDACs) is connected with transcriptional repression. Histone demethylation is associated with lysine-specific demethylase (LSD) and JmjC domain containing histone demethylase (JHDM).
The nucleosome is consisted of four histone proteins (H2A, H2B, H3, and H4), they are primary building block of chromatin. The addition and removal of specific chemical groups refers to as epigenetic marks, it regulates chromatin structure and affects gene expression. Moreover, RNA is intimately involved in the formation of a repressive chromatin state.
Epigenetic mechanism responds to environmental changes at the cellular level and thus influences cellular plasticity. Chromatin and epigenetic regulation play a significant role in the programming of the genome during development and stress response, defects in epigenetics can lead to cancer, inflammation and metabolic disorders etc.
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B3272 InauhzinTarget: Sir2-like Family Deacetylases (Sirtuins)Summary: SIRT1 inhibitor
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A3556 LKB1 (AAK1 dual inhibitor)Target: PimSummary: Pim-1 kinase inhibitor
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A3692 OTX-0153 CitationTarget: BromodomainsSummary: BRD inhibitor
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A3760 ReversineTarget: Aurora KinasesSummary: A3 adenosine receptor antagonist,ARK-1/-2/-3 inhibitor
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A3937 XL019Target: JAKSummary: JAK2 inhibitor,potent and selective
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A4147 LY2784544Target: Aurora Kinases|FLT3|VEGFR|FGFR|Trk Receptors|JAK|ALK|TYK2|MUSK|MAP3KSummary: JAK2 inhibitor,highly potent and selective
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A4148 NVP-BSK805 2HClTarget: JAKSummary: JAK2 inhibitor
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A4150 WHI-P154Target: VEGFR|Src|EGFR|JAKSummary: JAK3 inhibitor
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A4160 A-966492Target: PARPSummary: PARP-1/-2 inhibitor, highly potent
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A4164 AZD2461Target: PARPSummary: Novel PARP inhibitor