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Message: Re: BET inhibition and epilepsy
4
Jun 08, 2021 02:08AM
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Jun 08, 2021 02:58AM

Interesting potential connection between epilepsy and BET inhibition. This is all pre-clinical so far, so must be taken in that contect. Since JQ1 is a pan-BET inhibitor and apabetalone is more selective towards BD2, there is incomplete overlap between their effects on bromodomain inhibition and downstream transcriptional changes. Furthermore, the biodistribution/pharmacokinetic properties of individual drugs varies. If the BET inhibitor in question needs to cross the blood brain barrier in sufficient quantities to elicit an anti-epileptic effect, then some drugs may be better than others. Thus far, there has been scant evidence that apabetalone gets across the blood brain barrier and into the brain/central nervous system. The BETonMACE cognition sub-study does not directly address this; the effects could very well be indirect due to effects of drug on circulating factors (lipoproteins, inflammatory mediators, etc). 

BDAZ

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Jun 09, 2021 01:35AM
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Jun 09, 2021 02:06AM
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Jun 09, 2021 05:53AM
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Jun 11, 2021 06:47AM
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