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Allosteric Mechanisms
STABILIZATION
Misfolded Protein
Gain Binds to Rescue Folding
Restored Protein Function
- Gain of function approach
- Stabilizing native form of protein
- Restores natural protein function
DESTABILIZATION
Functional Protein
Gain Binds to Disrupt Folding
Loss of Protein Function
- Loss of function approach
- Allosteric PROTAC, targeted protein degradation
- Results in ubiquitination and protein degradation
Degradation
Functional Protein
Ubiquitination at Allosteric Site
Loss of Protein Function
- Loss of function approach
- Stabilizing non-native form of protein
- Results in protein dysfunction and/or degradation
Allosteric Inhibition
Inhibitor Binds
Active Site Changes
Substrate Can't Bind
- Loss of function approach
- Changing active site conformation to inhibit binding
Activation
Allosteric Activation
Active Site Changes
Substrate Bind
- Gain of function approach
- Changing active site conformation to induce binding
At Gain, we've developed a sophisticated, automated, selective and high-throughput method for drug discovery that is both highly efficient and cost-effective. Our streamlined approach dramatically shortens the conventional drug discovery timelines, enabling life-saving medications to reach patients sooner.
Posters
AD/PD™ 2024
GT-02287, A CLINICAL STAGE GLUCOCEREBROSIDASE REGULATOR FOR THE TREATMENT OF PD, EASES ER STRESS AND ENHANCES LYSOSOMAL ENZYME ACTIVITY
20th Annual WORLDSymposium®
GT-02287, a clinical stage GCase enhancer, displays neuroprotection and restores motor function in preclinical models of Parkinson’s disease following delayed administration