A growing team of groundbreaking scientists around the world are now sharing their lab notebooks online
A major therapeutic avenue for chordoma is targeting the receptor tyrosine kinase, EGFR. Its ligand, EGF, is overexpressed as a transcriptional target of Brachyury and polysomy of EGFR’s region of chromosome 7 is frequent in chordoma. To this extent I, in collaboration with SGC-UNC’s post-doc Chris Asquith, am working on the profiling of a number Read More …
Deposition: In the past two weeks my work has mostly been full of dealing with structures. The first thing I needed to do was deposit some structures of ALK2 co-crystallised with three drug molecules that I had solved for our collaborators Swen Hoelder and Liam Hudson at ICR, who had been developing compounds against ALK2. Read More …
Another small set of compounds was recently synthesized, the major change in Set2 is the substitution of the sulfur atom by oxygen or nitrogen. The change was made in position 6 of the pyrimidine ring. These compounds along with others from Set1 are currently under screening in the NanoBRET cellular assay (performed by Carrow Wells).
Full-length huntingtin protein aggregation and first attempts to co-purify HTT-HAP40 from insect cells
Greetings! My first post here will be a brief introduction. More in-depth experiment and data posts are coming soon! I am a post-doctoral research associate in the UNC Catalyst for Rare Diseases1. Throughout my education and training, I have been interested in cancer – I worked on epigenetics of ovarian cancer as an undergraduate and Read More …
I have had little success with DSF and FP assay development for USP5 Zf-UBD to identify small molecule ligands of this domain. I decided to try 19F NMR as a potential screening assay. NMR spectroscopy can be used to visualize changes in protein spectra upon addition of low complexity molecules as well as to quantify Read More …
As you are probably aware by now, if you’ve read a few of my blogs, we are testing ATP competitive inhibitors to inhibit ALK2 but not any of the other 6 ALK family members. Thus, most of our activity and cellular assays test ALK2 as well as ALK5 activity in order to check the specificity Read More …
After preparation of a set of GW807982X analogs, the next step was to get screening data against CLK1/2/3 at concentration of 1 uM at Luceome. For compounds that showed an inhibition of >75% on target they get a full dose response curve to generated IC50 values. To date, a set of 60 compounds have been synthesized Read More …
Hello there! This week I won’t be filling you in on my latest experiment, because instead I spent three days at the first ever Cancer Research UK Brain Tumour Conference held in the Royal Society of Medicine in London! (Also the biggest conference I’ve been to so far). The conference gathered over 30 great speakers Read More …
One of the more unpredictable parts of crystallography is also one of the most fundamental – will the protein crystallise? Despite decades of work done on protein crystallisation, and numerous ‘tricks of the trade’ to maximise the chances, whether a protein will actually form a crystal is still relatively random. With ALK2 we’ve crystallised it Read More …
