Why EZHIP may be a drug target?

PFA ependymomas are pediatric brain tumors with very poor prognosis. They represent about 10% of all pediatric tumors of the central nervous system (CNS), and up to 30% of CNS tumors in children under 3. (1) 9.4% of PFA tumors aberrantly express EZHIP (aka CXorf67), a protein that inhibits Polycomb repressive complex 2 (PRC2). PRC2 Read More …

Testing USP5 ZnF-UBD analogues with a Displacement Assay and SPR

If you’ve been following along my open notebook journey over the last two years, you’ll be excited to hear I’ve published my work on the first antagonists of USP5 ZnF-UBD in a peer-reviewed journal. Check it out here! In a previous post, I outlined my selection of the next set of analogues in my chemical Read More …

The protein WDR41, and its role in ALS.

Amyotrophic lateral sclerosis (ALS) is a terrible disease that affects the way a person speaks, moves and even breaths, and is responsible for as many as 5 deaths for every 100,000 people over the age of 20. ALS is a progressive disease, affecting the neurons in the both the upper and lower brain way[2], as Read More …

Purification of more ALK2 GS loop mutants and fresh ACVR2.

So I’m still ‘trying to catch them all’ as the young folks say (!) and building up my collection of purified GS loop mutations so that I can test them all together and start building up a picture of what phosphorylation sites are necessary for SMAD1 activation and which are not. This time around I Read More …

HDAC11 cellular assay validation with catalytic mutants and inhibitors

My previous results showed that overexpression of HDAC11 decrease basal acetylation levels of exogenous histones as well as decrease the acetylation increase caused by histone acetyltransferases. In order to determine if the observed effect is caused by catalytic activity of HDAC11, I used catalytic HDAC11 mutants Y304H and H142,143A (PIMID: 30819897, 28927261) and published HDAC11 Read More …