What are exosites?

Targeting exosites represents a breakthrough approach to unlocking traditionally intractable targets through highly selective drugs that reprogram target proteins. To understand the significant advantages of exosite targeting, it helps to first understand how enzyme-drug interactions work.

Enzymes are proteins that work as biological catalysts molecules to accelerate specific chemical reactions in the body. They achieve this catalytic energy by binding with different substrates depending on the desired reaction.

Enzymes are proteins that catalyze reactions with substrates

Enzymes play key roles in all metabolic processes, such as destroying toxins and aiding digestion. This critical metabolic role can also make enzymes prime culprits in promoting disease states like cancer or inflammation. One way to treat these diseases is to block or modify enzyme activity, however traditional methods to drug enzymes do not work in many cases.

Traditional methods to drug enzymes do not work for many targets

Our solution is to target exosites, distal and unique binding pockets that modulate enzyme activity for precise and potent therapeutic effect.

Exosite Opportunity

Traditional methods of drug discovery have engaged ~7% of the known target space, but we have identified exosites in classes of enzymes that represent ~30% of the known target space. This prevalence of exosites may enable us to significantly expand the diversity of targets that we can pursue in drug discovery.

Exosite Discovery

Our ExoSight platform leverages a confluence of recent technologies that enable us to see, model, build, design and discover novel exosite-targeted small molecule drugs. While some of these tools may have been available to drug developers previously, Exo has built proprietary capabilities for their application in exosite identification and systematized ligand discovery.

Our ExoSight platform can be applied across enzyme classes to discover innovative therapeutic candidates for many diseases.