Cellular Metabolism

AUTOPHAGY

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Epigenetics

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Nuclear Receptors

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Ubiquitin Proteasome

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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.

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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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