Developments that Save Lives
Statistics reveal that 1 in 2 men and 1 in 3 women will be diagnosed with cancer in their lifetime, and 1 in 4 men and 1 in 5 women will die from this class of malignant diseases. A novel approach emerging in the fight against cancer is a technology called Proteolysis Targeting Chimeras, or PROTACs.
“This new approach has made undruggable targets druggable”
E3 and PROTACs
Unlike traditional inhibitors, which are defined by competitive and occupancy-driven processes, PROTACs are based on a catalytic mode of action. Specifically, they promote target protein degradation at low exposure concentrations. PROTACs have the potential to degrade the target pathogenic protein and completely shunt related signalling pathways, a process not achievable by traditional therapies (i.e., inhibitors/activators). This new approach has made “undruggable” targets (such as KRAS) “druggable,” thus expanding the repertoire of therapeutics available for use against multiple diseases. As a result, PROTACs have gained significant attention from the pharmaceutical and biotechnology industries.
A Range of Talent
Lead by a team of experts, E3 Therapeutics is founded on a diverse set of experiences.
To Change the World
Focused on treatments related to several diseases, our technology will be widely applicable.
With Statistical Success
With our PROTAC drug development platforms, we offer the best odds at preventing chemoresistance.
Despite advances in PROTAC technology, however, there remain a number of clinical development challenges. One such challenge is to increase the potential for clinical success while reducing chemoresistance. E3 ligases, for example, dictate ubiquitination/removal of the target molecules, but current PROTAC drug candidates target only a single E3 ubiquitin ligase. This factor increases the chances of a drug failing because the targeted E3 ubiquitin ligase may not be present in every cancer cell and tissue type, and the targeted E3 ubiquitin ligase also has the potential to mutate during acquired drug resistance.
To address this issue, E3 Therapeutics Inc. has designed a series of lead compounds that can simultaneously bind to three different homologous E3 ubiquitin ligases. This expands upon existing PROTAC viability and makes it possible to construct therapeutics with increased efficacy and decreased drug resistance.