Cellular Metabolism
AUTOPHAGY
Ion & Other Channels
Epigenetics
Cytoskeleton
Kinases
Mitochondria
Nuclear Receptors
Bioactive Lipids
Ubiquitin Proteasome
VIEW ALL Biochemical Targets
Covalent modifications to DNA or histone proteins with various chemical groups can determine whether genes are turned on or off and can thus influence the production of proteins in a cell. This genetic control without altering DNA sequences is crucial in many normal cellular functions. Aberrant epigenetic alterations are present in myriad disease states. Pharmacological manipulation of the various enzymes involved in epigenetic changes in pathological states is an important new target in drug discovery. Writers (methyl and acetyl transferases) are enzymes capable of modifying nucleotide bases and amino acid residues on histones. Erasers (demethylases and deacetylases) remove these same modifications. Readers (bromodomains) are enzymes capable of recognizing specific epigenetic marks that direct a particular transcriptional outcome.
Bromodomains
Bromosporine
Bromosporine is a pan-bromodomain inhibitor
I-BET762
I-BET762 is a potent inhibitor of the BET family of bromodomains
Histone Deacetylation
Mocetinostat
Class I, isoform-selective HDAC inhibitor
RGFP966
Potent and selective HDAC3 inhibitor
Tubastatin A
Potent and selective HDAC6 inhibitor
Histone Methylation
(R)-PFI-2
Potent and selective SAM-dependent inhibitor of the methyltransferase SETD7
A-196
Potent and selective inhibitor of the methyltransferase SUV420H1/H2
EPZ015666
Potent and selective inhibitor of the arginine methyltransferase PRMT5
DNA Methylation
RG-108
Non-nucleoside DNA methyltransferase inhibitor
Decitabine
Decitabine is a DNA methyltransferase inhibitor
Histone Demethylation
SP2509
SP2509 is a potent and reversible inhibitor of LSD1
ML324
ML324 is an inhibitor of JMJD2 histone demethylases
CPI-455
CPI-455 is a potent and selective inhibitor of the lysine demethylase KDM5
Histone Acetylation
Anacardic acid
Anacardic acid is an inhibitor of the acetyltransferases p300 and PCAF
CPTH2
CPTH2 is a selective inhibitor of the acetyl transferase Gcn5P
CTPB
CTPB is a selective activator of the acetyltransferase p300. Selective over PCAF.
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