Epigenetics drug development // Drug Repurposing

Epigenetics drug development

Digitally Generated DNA StrandsEpigenetics research has expanded rapidly over the last several years, as evidenced by the exponential increase in published literature in this field. Breakthroughs have been made in the elucidation of basic epigenetic mechanisms such as histone modification, and with these advances have come an understanding of the critical role epigenetic modifications play in the development and progression of cancer. For example, deregulation of specific histone H3 methylation sites has been associated with tumor suppessor down-regulation and the development of several types of cancer.1 Not surprisingly, there has been an increased focus on the identification of clinical treatments for aberrant epigenetic states, and in particular on targeted inhibitors of the dozens of enzymes that carry out histone post-translational modifications. Histone modification enzymes can be classified as Writers, which add epigenetic marks such as methyl, acetyl or phospho- groups, and Erasers, which catalyze the removal of these marks.Figure 1. Histone H3 and p53 epigenetic modifications measurable with LANCE and AlphaLISA homogenous immunoassays. For example, tumor suppressor down-regulation has been correlated with the loss of H3K4me2 and H3K4me3 marks (di- and trimethylation at lysine 4 of histone H3) and with loss of the H3K9ac mark through deacetylation.2 Thus, a targeted inhibitor for one of these eraser enzymes could be a valuable drug candidate.

Challenges to epigenetic drug discovery

As clinical research identifies an increasing number of correlations between epigenetic marks and disease states, drug discovery efforts have focused on screening compound libraries for candidate molecules capable of targeted inhibition of epigenetic writer or eraser enzymes. These efforts have been hampered by limitations of available technologies as well as a lack of high quality reagents. Assays for epigenetic drug discovery must be capable of distinguishing between generalized and specific effects, since a lead compound with a narrowly targeted effect is less likely to have off-target effects in clinical application. Epigenetic assays should also be as biologically relevant as possible, ideally measuring epigenetic marks on endogenous histone proteins.

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by flaveur

Marijuana smoking 'permanently lowers IQ'
Teenagers who regularly smoke cannabis are putting themselves at risk of permanently damaging their intelligence, according to a landmark study.
Researchers found persistent users of the drug, who started smoking it at school, had lower IQ scores as adults.
They were also significantly more likely to have attention and memory problems in later life, than their peers who abstained.
Furthermore, those who started as teenagers and used it heavily, but quit as adults, did not regain their full mental powers, found academics at King’s College London and Duke University in the US

Parents,talk to your kids about marijuana.

by flaveur

Marijuana smoking 'permanently lowers IQ'
Teenagers who regularly smoke cannabis are putting themselves at risk of permanently damaging their intelligence, according to a landmark study.
Researchers found persistent users of the drug, who started smoking it at school, had lower IQ scores as adults.
They were also significantly more likely to have attention and memory problems in later life, than their peers who abstained.
Furthermore, those who started as teenagers and used it heavily, but quit as adults, did not regain their full mental powers, found academics at King’s College London and Duke University in the US

Brain damage & permanently lowered IQ

by flaveur

Marijuana smoking 'permanently lowers IQ'
Teenagers who regularly smoke cannabis are putting themselves at risk of permanently damaging their intelligence, according to a landmark study.
Researchers found persistent users of the drug, who started smoking it at school, had lower IQ scores as adults.
They were also significantly more likely to have attention and memory problems in later life, than their peers who abstained.
Furthermore, those who started as teenagers and used it heavily, but quit as adults, did not regain their full mental powers, found academics at King’s College London and Duke University in the US

In the news again ... marijuana & brain damage

by flaveur

Parents, talk to your kids about marijuana. It is an extremely harmful, illegal drug.
Dec 16, 2013 - Research released Monday in the journal Schizophrenia Bulletin showed the brains of young heavy marijuana users were altered in sub-cortical regions — primitive structures that are part of the memory and reasoning circuits. And young people with such alterations performed worse on memory tests than non-using controls, despite the fact that the heavy users had not indulged for more than two years, on average, before the testing.
Teenagers who regularly smoke cannabis are putting themselves at risk of permanently damaging their intelligence, according to a landmark study

Inform Genomics and Translational Drug Development (TD2) Announce ..  — MarketWatch
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