Epigenetic Lead Discovery

Epigenetics play a key role in the drug discovery process, especially in oncology, with over 90% of all cancers known to involve complex epigenetic mechanisms.

Despite that, the potential most promising targets are hard to access by conventional screening methodologies. Proteros´ has a pole position by deciphering these complex mechanisms by applying its highly adaptable Nucleosomal Epigenetic Assay Technology (NEATTM) platform for functional activity screening on the nucleosome level.

The NEAT discovery platform and Proteros´ owned premier in-house Discovery Service platform technologies are crucial elements of Proteros’ Epigenetic lead discovery strategy, approach and engine.

The research field of epigenetics turned out to be one of the most promising and signifying molecular sciences of our century. Nowadays, it is known that not only the DNA itself encodes the development process of multi – cellular organisms. On the contrary, all multi-cellular organisms display a variety of epigenetic mechanisms to define cellular identities.

Cellular identities emerge from the developmental history of the cell and are passed to new generations through successive rounds of DNA replication and cell division. Epigenetic enzymes alter gene expression programs through functional interactions with nucleosomes, which are the fundamental regulatory scaffolds of our genome.

 

For example, this functional interaction can be a covalent modification of the nucleosome catalyzed by epigenetic “writer” or “eraser” proteins to establish a permanent signature on the respective genome region or a more transient binding event as in the case of reader domains. Even a structural chromatin alteration, as catalyzed by epigenetic remodeling complexes, can occur. 

Ultimately, modification of the nucleosome can result in a change of gene expression, e.g. gene silencing or activation.

Human disease states can be causally linked to changes in their epigenetic cellular identity. Therefore, epigenetic targets have gained increased attention in the drug discovery community. Understanding the precise target biology can create an opportunity to influence or inhibit the disease process.

The potential most promising targets are hard to access by conventional screening methodologies. Proteros has a pole position for deciphering these complex mechanisms by applying its highly adaptable Nucleosomal Epigenetic Assay Technology (NEATTM) platform for functional activity screening on the nucleosome level.

Proteros aims to reverse the fundamental oncologic disease processes by developing next generation epigenetic compounds. We leverage the strengths of small molecule-based drug discovery by reproducing the disease relevant biochemical processes, starting from primary screening, over bio-structural research and medicinal chemistry, all the way up to lead selection and early exploratory pharmacological research to facilitate the nomination of a preclinical compound. 

 

Proteros proprietary Nucleosomal Epigenetics Assay Technology NEAT ™ platform, together with the smart, innovative and value-adding target discovery, validation and epigenetic lead discovery approach plus the integration of Proteros’ world-class discovery service technology platforms make Proteros a premier partner for drug discovery partnering in the field of immune-oncology targets.