Novel compound for Melanoma cells

An international team of researchers has developed a novel compound that successfully inhibits growth of melanoma cells by targeting specific epigenetic modifying proteins in these cells. In the human body cells turn genes on and off by means of chemical modifications that change DNA and related proteins. These epigenetic changes are continuous and are at the core of how healthy cells transform into cancer cells.

These modifications contribute to a tumor's ability to grow indefinitely, as well as making tumor cells drug resistant and capable of surviving treatments intended to kill them. The new compound, Corin, specifically targets these epigenetic changes in cells and could therefore provide significant improvements in patients without unwanted side effects.

Currently there are few epigenetic drugs in clinical use, including histone deacetylase (HDAC 1) inhibitors, which are used to treat some lymphomas and histone demethylase inhibitors (LSD1) which are used to treat some leukemias. These reagents have not been more broadly useful in cancers due to their limited therapeutic window and untoward side effects.

Researchers at Boston University School of Medicine, Johns Hopkins University and Universiita di Pavia, Harvard Medical School and the University of Leicester collaborated to develop a unique compound, Corin that specifically act to inhibit both demethylase an deacetylase activity in cells. Corin is particularly attractive as an inhibitor of epigenetic modifications because it has dual-target specificity which allows for more selective targeting of epigenetic complexes in treated cells.

It is anticipated that this novel compound will have significant efficacy in human melanomas and other cancers either as a stand-alone therapy or in combination with other targeted or immune-based therapies.To evaluate the efficacy of this new compound, the researchers first tested it using a cell culture system to evaluate melanoma cell biology in vitro and found a variety of cancer-associated processes were affected, including cellular growth, differentiation and migration.

The compound then was tested in an experimental model for melanoma and found to significantly inhibit tumor cell growth without appreciable toxicities. The researchers believe there are other disease entities, apart from cancers, that may be significantly affected by targeted epigenetic therapies. Most notably, immune-mediated diseases are expected to be significantly influenced by such reagents as epigenetic changes have been widely noted to influence the immune system.
          haleplushearty.blogspot.com

Epigenetic reveals early breast cancer development

Changing the epigenetic code of a single gene is enough to cause a healthy breast cell to begin a chain reaction and become abnormal, Epigenetic changes are a hallmark of cancer, but up until now, it has not been known whether these changes on their own are sufficient to push healthy cells down the cancer path.

 Using a CRISPR-dCas9 epigenetic editing tool, the researchers methylated different genes in healthy breast cells and found that those changes were sufficient to cause the cells to undergo hyperproliferation - abnormally rapid cell division which is an early stage of tumour initiation.

The epigenetic changes are inherited as long as the cell divides, and that the team's manipulations permanently and negatively affected the biology of a normal breast cell from a healthy individual. Epigenetic editing could also be used to design novel therapies by initiating permanent changes to cell biology.

This may be a more viable or alternative way forward for gene editing as any potential mistakes would be less damaging than directly editing the DNA sequence, and epigenetic editing would be more easily reversible if needed. Epigenetic fluctuations happen all the time in human cells. During ageing, human epigenome is progressively distorted.
          haleplushearty.blogspot.com