Epigenetic Targets
     
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Epigenetic Targets

Protease focused librariesEpigenetic regulation of gene expression is a dynamic and reversible process that establishes normal cellular phenotypes but also contributes to human diseases. At the molecular level, epigenetic regulation involves hierarchical covalent modification of DNA and the proteins that package DNA, such as histones. Key protein families that mediate epigenetic signalling through the acetylation and methylation of histones are histone deacetylases, protein methyltransferases, lysine demethylases, bromodomain-containing proteins and proteins that bind to methylated histones. These protein families are emerging as druggable classes of enzymes and druggable classes of protein–protein interaction domains [1].

 

 

 
OTAVAchemicals offers Epigenetic Targeted Libraries designed with receptor-based approach. These libraries are proposed for screening in epigenetic regulation research and drug development projects.

  • the libraries contain drug-like compounds only

  • all the compounds are in stock

  • cherry picking is available

 

You can sort data by any column and use "Filter" option to search library's name:

Name Number of compounds Approach Details
DOT1-like histone H3 methyltransferase (DOT1L) inhibitor library 622 Receptor-based read more
Bromodomain-containing protein 4 (BRD4) inhibitor library 401 Receptor-based read more
Histone deacetylase (HDAC) inhibitor library 803 Receptor-based read more
DNA (cytosine-5)-methyltransferase 1 (DNMT1) inhibitor library 466 Receptor-based read more
DNA (cytosine-5)-methyltransferase 3 beta (DNMT3b) inhibitor library 1261 Receptor-based read more
Histone acetyltransferase (HAT) inhibitor library 814 Receptor-based read more
CREB binding protein (CREBBP) targeted library 576 Receptor-based read more
Protein Arginine Methyltransferases (PRMTs) Targeted Library 842 Receptor-based read more
Enhancer of Zeste Homolog 2 (EZH2) Targeted Library 979 Ligand-based read more
Lysine-specific demethylase 4C (GASC1) Targeted Library 966 Ligand-based read more

OTAVAchemicals Targeted Libraries Collection
Name Number
Kinases 69
Proteases 17
GPCRs 51
Ion channels 5
Disease-based libraries 74
Epigenetic targets 8
Protein-Protein Interaction 2
Peptidomimetic 2
Nuclear Receptors 12
Glycomimetic 1
RNA binding 1
SH2 binding 1
General Activities 128
Other 93

 

 

The libraries (SDF, XLS, PDF format) are available on request. Feel free to contact us or use on-line form below to send an inquiry if you are interested to obtain these libraries or if you need more information.

 

 

 

  1. Arrowsmith CH, Bountra C, Fish PV, Lee K, Schapira M. Epigenetic protein families: a new frontier for drug discovery. Nat Rev Drug Discov. 2012 Apr 13;11(5):384-400.
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