...We Welcome You To The Resverlogix HUB withIn The AGORACOM COMMUNITY!

Free
Message: Interesting paper on BET inhibitors and Memory

I tried posting this article a couple times on Friday but it got auto-flagged and removed for some unknown reason. So I am just going to link to the article and PubMed link without copying the article title.

This study used JQ1, not apabetalone. JQ1 is a pan-BET inhibitor, whereas apabetalone is a bromodomain-2 selective BET inhibitor. Not all BET inhibitors are created equal or have the same tissue distribution/pharmacokinetic properties. Apabetalone may not cross the blood brain barrier as much as JQ1 and/or elicit the same effects on memory as JQ1 did in this paper. The effects documented in this paper may be specific to JQ1 and other pan-BET inhibitors that bind with equal affinity to both bromodomains.

There was a big focus on brain-derived neurotrophic factor in this paper, suggesting that BRD4 is necessary for its increased expression. However, in this post-hoc analysis of Phase 2 ASSURE, it seems that this brain-derived neurotrophic factor protein levels in the plasma increased, not decreased, with apabetalone treatment. Protein levels don't always correlate the mRNA gene expression levels. So it is tough to compare the two studies. We won't have to guess much longer since the BETonMACE cognition sub-study is right around the corner.

BearDownAZ

 

Share
New Message
Please login to post a reply