GSK-126 inhibit EZH2 activity - first potential POTS cure

[mitoMAN]

GSK-126 inhibit EZH2 activity - first potential POTS cure

Targeting Treatment Refractory NET by EZH2 Inhibition in Postural Tachycardia Syndrome
https://www.ahajournals.org/doi/abs/10.1161/CIRCRESAHA.119.315654

Researchers have discovered how genes that protect against Postural Orthostatic Tachycardia Syndrome (POTS) become silent or ‘switched off’ and have identified a drug to switch them on again.
We predicted that inhibiting this epigenetic condition could reactivate NET gene function and used a pharmacological drug called GSK-126 that could specifically inhibit EZH2 activity with dramatic results,” Professor Sam El-Osta said. “This is the first description of NET reactivation using a drug. The beauty is that it allows us to target very specifically the enzyme to reactivate gene function.”

Resources:
https://www.drugtargetreview.com/ne...stural-orthostatic-tachycardia-syndrome-pots/

Importantly the researchers, including first author Dr Harikrishnan Kaipananickal, from Professor El-Osta’s lab, have used a highly selective drug, called GSK-126, that inhibits this enzyme and restores the functioning of the NET gene, effectively restoring gene behaviour in pre-clinical studies, using blood cells derived from POTS patients.

According to Professor El-Osta, the data is “encouraging because there has been a paucity of new therapeutic approaches and our studies address an unmet need in POTS” because it is one of the few examples where a drug has been found to alter not only a gene but the way that the gene manifests itself, in this case with poor circulation and fainting. “The results have actually unlocked the NET gene which was previously thought as too difficult to restore in cells,” he said.

Resources:
https://www.monash.edu/medicine/new...-fainting-syndrome-affecting-one-in-100-teens



So I decided to host a 3rd Party laboratory testing of a `GSK-126 Supplier from Alibaba.
Anyone interested to join, please PM me or post here.

I will provide you with our Discord Server that is dedicated to analysie and custom synthesize research medications useful for ME/CFS.

 

[mitoMAN]

Anyone has the energy and time to look for more studies of GSK-126 and see if you can find any that already injected it to animals? So we can get an idea of human equivalent dosages? I am already very fatigued with managing all the other medications and I am mostly bedbound 20 hours per day.