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.
- A4111 VX-680 (MK-0457,Tozasertib)Target: Aurora KinasesSummary: Aurora kinase inhibitor
- A4112 Barasertib (AZD1152-HQPA)3 CitationTarget: Aurora KinasesSummary: Aurora Kinase B inhibitor, Potent and selective
- A4130 ENMD-2076Target: Aurora Kinases|FLT3|RET|Src|VEGFR3/FLT4|NTRK1/TRKA|CSF-1R/c-FmsSummary: Selective Aurora A/Flt3 inhibitor
- A4132 CCT137690Target: Aurora KinasesSummary: Aurora A/B/C inhibitor
- A4114 MLN8054Target: Aurora KinasesSummary: Aurora A inhibitor
- A4115 JNJ-77066211 CitationTarget: Cyclin-Dependent Kinases|Aurora KinasesSummary: Potent CDK/Aurora kinase inhibitor
- A4116 Danusertib (PHA-739358)2 CitationTarget: Aurora KinasesSummary: Pan-aurora kinase inhibitor
- A4121 SNS-314 MesylateTarget: Aurora KinasesSummary: Aurora A/B/C kinases inhibitor, potent and selective
- A4122 PHA-680632Target: Aurora Kinases|PLK|FGFRSummary: Aurora kinase inhibitor,novel and potent
- A4124 TAK-901Target: Aurora Kinases|FLT3|Src|JAK|LRRK2|Hck|FGR|YES|Fyn|ARGSummary: Novel Aurora A/B inhibitor