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Epilepsy is a chronic disorder affecting around 65 million people worldwide. This neurological disease is characterized by an enduring propensity for generation of seizures, which are usually treated with seizure medications. However, around 30% of the epilepsy patients (~20 million) do not respond to current treatments, which highlights the need of identifying novel targets for the treatment of this condition.

In the recent years, advances in Artificial Intelligence (AI) and Machine Learning (ML) have flooded the popular press and captured the attention of professionals from different backgrounds. A wide variety of applications of ML have sprung out and have entered with determination in the drug discovery arena.

Looking back at research landmarks of the already past year is a good starting point for this 2019. The unstoppable and continuous advance on scientific research gives its many fruits in a broad spectrum of fields. Today we would like to highlight the discoveries of a group of Virginia-based scientists in the field of the Central Nervous System and Epilepsy.

Mcl-1protein is a validated therapeutic cancer target that is involved in apoptosis inhibition. Therefore Mcl-1 plays a critical role in cancer cell survival. Furthermore, prevention of Mcl-1 functionality has been proved to be cytotoxic for some cancer cell lines. Mcl-1 interacts with Bcl-2 family proteins through a hydrophobic region in the α-helix motif BH3, which is present in Bcl-2 family proteins. Specifically, Mcl-1 is able to bind to pro-apoptotic proteins through the BH3 domain, thus avoiding programmed cell death.

Highly selective inhibition of histone demethylases by de novo macrocyclic peptides

Aberrant histone modifications are associated to several chronic and highly prevalent worldwide inflammatory and cardiovascular diseases, as well as cancer. One of the primary reasons leading to this scenario is the mutation or dys-regulation of proteins responsible to read and write post-translational histone modifications, particularly methyltransferases and demethylases, commonly known as KDMs.