A growing team of groundbreaking scientists around the world are now sharing their lab notebooks online
Preparation of CaMKK2 analogs Pursuant to our aim of preparing a library of small molecule chemical probes around our most promising core scaffold, furopyridine, we sought to develop different chemistries that would allow us to achieve this objective. In the original synthetic route, 5-bromofuro[2,3-b]pyridine, 1, was able to undergo the Suzuki cross-coupling reaction to install Read More …
As part of an ongoing collaboration with Meds4Kids Pharma (M4KPharma), we are testing a range of compounds identified and generated by them as being of interest in developing a molecule specific against ALK2 that has the right properties help treat some cases of DIPG. This also has significant implications for development of a drug that Read More …
These days CRISPR gene editing needs little introduction. From humble origins as a bacterial defence system evolved to thwart viral invaders, CRISPR-based technologies have recently made headlines for their promise to revolutionize medicine. While there is a lot of excitement surrounding the use of gene editing in the clinic, it is also an incredibly valuable tool for studying the Read More …
I’m sad to report that a couple of test expressions later, we’re still no wiser as to why ACVR1 isn’t expressing. It’s worked on a couple of small scale expression test plates, but just doesn’t want to scale up anymore. We may be looking at having to remake the virus. In the meantime, I had Read More …
It’s been a very busy few weeks, a fair amount of lab work but also a fair bit of outreach work (which is the other part of my job) and so I’ve sadly neglected to write my poor blog post. However, now I’ve got the chance to write a bit about what I’ve been Read More …
The experimental set-up and results covered in this post can be found here: 10.5281/zenodo.1323902 As I’ve been having problems overexpression HTT properly in my cancer cell lines, I decided to continue looking at other proteins of interest using our best overexpression model so far, which is in HEK293T cells. Although it may not be a cancer Read More …
Hello again! Here is my first attempt to find an EZH1 antibody. I have mainly focused on EZH2 in the PRC2 complex as the methyltransferase responsible for the H3K27me3 mark. However, EZH1 can functionally substitute for EZH2 in PRC2. We have a good antibody to detect EZH2 levels in patient AML samples. However, for some Read More …
A closer look at the hits generates 2 new hypotheses
NSD3 is located on a region of chromosome 8 (8p11-12) that is frequently amplified in several forms of cancer. It has been suggested that NSD3 (WHSC1L1) may be a driver of tumorigenesis in this context (Mahmood et al. 2013). However, it is still unclear how amplification of NSD3 contributes to the disease and whether or not it Read More …
The original compound donated by Pfizer PFE-PKIS 43 (thienopyrimidine scaffold), showed activity against 3 kinases greater than 70% inhibition in the KinomeSCAN at 1 µM (STK17B/DRAK2, AURKB and SRPK2). In the series of compounds recently synthesized as thienopyrimidine derivatives we seek selective and potent inhibitors for STK17B/DRAK2 only. To further identify off-target activity of these Read More …
