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Epigenetics and its role in human cancer

Cancer is often associated with heritable epigenetics changes,
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Cancer is often associated with heritable epigenetics changes, which are characterized by the change in gene expression profile without changing the underlying DNA sequence. The most prominent epigenetic modification is methylation of DNA; which to a large extent is connected to modifications of histone proteins. Epigenetic modifications resulting in a normal gene are reversible, thus endow functional flexibility and diversity to the genome and these modifications can be cured with selective epigenetic target inhibitors. Role of epigenetics in human cancer has been vastly studied and reported in recent decade with emerging evidences about the significance of epigenetic alterations to comprehend various cellular mechanisms. The cellular mechanisms which are crucial for controlling the growth & progression were seen to be impaired by epigenetic changes, which results into development of various human cancer diseases. Although several targets for cancer epigenetics have been identified and annotated in recent past, the development of novel anticancer treatments for these targets are still in nascent stage. By recognizing the spectrum of cancer epigenetics, an array of new drug discoveries was been possible these days. In this chapter, we presented an overview of such epigenetic modifications which occurs and resulted into human cancer; relationship between those epigenetic enzyme classes and cancer types, with a note on pre-clinical utilizations of inhibitors for the treatment of such cancer types.

CEMdb

CEMdb is a freely available, specialist, electronic database dedicated to facilitate interactive exploring of epigenetic proteins and their modulators. The database consists of diverse epigenetic protein families, their reported inhibitors & associated pharmacokinetic properties, structural data, toxicological and chemoinformatic information. The database can be browsed utilizing protein family names, ligand names, ligand structures, substructures. In its present rendition, CEMdb would facilitate SAR studies, statistical analysis & scaffold-based drug design. . In general, this database will be helpful for designing new drugs and therapies for disease like cancer and other ones like cardiovascular diseases, neurodegenerative disorders, diabetes etc. read more

CEMdb is a freely available, specialist, electronic database dedicated to facilitate interactive exploring of epigenetic proteins and their modulators. The database consists of diverse epigenetic protein families, their reported inhibitors, pharmacokinetic properties, structural data, toxicological and chemoinformatic information. The database can be browsed utilizing protein family names, ligand names, ligand structures, substructures. In its present rendition, CEMdb would facilitate SAR studies, statistical analysis & scaffold-based drug design. . In general, this database will be helpful for designing new drugs and therapies for disease like cancer and other ones like cardiovascular diseases, neurodegenerative disorders, diabetes etc. The fundamental point of the database is to give computational and and medicinal chemistry tools for researchers who are interested in medicinal chemistry, biology and biochemistry of epigenetic protein families. We trust that the set of tools presented in the database will welcome researchers from diverse background to start drug designing outline and improvement in the field of cancer epigenetics. This infobase would be of use to biology researchers, especially those interested in epigenetic regulation. We welcome suggestions from the scientific community.


Recent Findings on Cancer epigenetic markers

Exploring dual inhibitors for STAT1 and STAT5 receptors utilizing virtual screening and dynamics simulation validation
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Molecular docking and dynamics simulation study of flavonoids as BET bromodomain inhibitors
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Structural insights into conformational stability of both wild-type and mutant EZH2 receptor
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Identification of Novel Inhibitors for Disrupting EZH2-EED Interactions Involved in Cancer Epigenetics: An In-Silico Approach
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Latest Updates

Epigenetics and it's role in Humar Cancer
A book Chapter has been published by Springer Publications: Translational Bioinformatics and Its Application
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Related tools & repositories

CpG Island Identification tool
The CpG sites or CG sites are regions of DNA where a cytosine nucleotide is followed by a guanine nucleotide in the linear sequence of bases along its 5' → 3' direction.
Click here

Few Important epigenetic targets and their Inhibitors
Epigenetic targets involved in Cancer and list of their reported inhibitors with their properties.
Click here
Epigenetics Databases & Tools