ApoRx Drug Discovery platform

ApoRx technology allows us to develop drug candidates for unmet medical needs by targeting the ‘undruggable proteome’. Our discovery platform integrates target identification, target validation, structural biology information, biochemical, and biophysical knowledge with ApoRx proprietary 'Apeiron library' of RING E3 ubiquitin ligases binders to accelerate the design of novel proteolysis targeting degraders.

 

The RING (Really Interesting New Gene) family is the largest type of E3 ubiquitin ligases. RING finger domains bind two zinc ions in a unique "cross-brace" arrangement through a defined motif of cysteine and histidine residues. RING E3 ubiquitin ligases, play an essential role in the regulation of many biologic processes and defects in some of them are involved in cancer development. Furthermore, some RING E3 ligases are frequently overexpressed in human cancers. Thus, targeting specific RING E3 ligases could lead to the development of a novel class of anticancer drugs.

The ‘Apeiron Library'

Based on years of work in the ubiquitin system the core of our technology is a unique library of compounds specifically designed to bind to RING finger E3 ubiquitin ligases.

Proprietary Chemistry

Our expertise in uncovering the molecular principles responsible for the properties of RING E3 ubiquitin ligases provided us the opportunity to design a proprietary library of small molecules that can be specifically tailored to generate efficient and selective binders to a variety of distinct RING ubiquitin ligases. These novel binders are the backbone of the ApoRx Proteolysis targeting degraders and are designed to have optimized pharmaceutical properties ideal for targeting proteins for breakdown in the proteasome.

Diversifying the degraders' arsenal

The Aperion selective RING E3 ligases binders enrich the arsenal of E3 binders that can be used to generate Proteolysis targeting degraders, and hence expand the pool of medically relevant therapeutic targets that can be sent for proteasomal degradation.

 

Targeting ligases for selective proteasomal degradation

Aperion binder molecules can be designed and used to send unwanted RING E3 ubiquitin ligase proteins for breakdown. For that purpose, we apply a unique methodology that allows us to control the direction of the degradation process. The ability to target a wide range of different E3 ligases adds hundreds of regulatory proteins as tractable drug targets.

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Scientist