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science (accordion)

 

 

Allosteric Mechanisms

STABILIZATION

 

STABILIZATION-FunctionalProtein

Misfolded Protein

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SRABILIZATION-GainBindstoRescueFolding

Gain Binds to Rescue Folding

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SRABILIZATION-ProteasonalDegradation

Restored Protein Function

 

 

  • Gain of function approach
  • Stabilizing native form of protein
  • Restores natural protein function

DESTABILIZATION

 

DESTABILIZATION-FunctionalProtein

Functional Protein

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DESTABILIZATION-GainBindstoDisruptFolding

Gain Binds to Disrupt Folding

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DESTABILIZATION-LossofProteinFunction

Loss of Protein Function

 

 

  • Loss of function approach
  • Allosteric PROTAC, targeted protein degradation
  • Results in ubiquitination and protein degradation

Degradation

 

Degradation-FunctionalProtein

Functional Protein

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Degradation-UbiquitinationatAllostericSite

Ubiquitination at Allosteric Site

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Degradation-ProteasonalDegradation

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

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Active Site Changes

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Substrate Can't Bind

 

 

  • Loss of function approach
  • Changing active site conformation to inhibit binding

Activation

 

Allosteric Activation

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Active Site Changes

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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

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

2023 International Congress of Parkinson's Disease and Movement Disorders®

GT-02287, a brain-penetrant structurally targeted allosteric regulator for glucocerebrosidase shows evidence of pharmacological efficacy in an animal model of Parkinson’s disease

2023 International Congress of Parkinson's Disease and Movement Disorders®

Neuroprotective effect of GT-02287, a brain-penetrant structurally targeted allosteric regulator of glucocerebrosidase, leads to a significant reduction of plasma NfL levels and improvement in behavioural deficits in a mouse model of GBA1 Parkinson’s dise

 

 

publications

PLOS One

Validation of a highly sensitive HaloTag-based assay to evaluate the potency of a novel class of allosteric β-Galactosidase correctors-min

Nature Scientific Reports

Tau accumulation in degradative organelles is associated to lysosomal stress

Current Drug Discovery Technologies

Extracting Atomic Contributions to Binding Free Energy Using Molecular Dynamics Simulations with Mixed Solvents (MDmix)