A growing team of groundbreaking scientists around the world are now sharing their lab notebooks online
Hello again, Three weeks have now passed since my first blog, and the response has been overwhelming, who knew this kid with a love of dinosaurs could become an internet blogger. Your encouragement to make my t-Rex has motivated me to do just that, so let’s see how it all goes. Also fun fact, the Read More …
Update on meetings, manuscripts and mighty cool experiments…
In a collaboration between SGC-University of North Carolina-Chapel Hill and M4K Pharma, we plan to synthesize 3 different imidazopyridin pyrazines as promiscuous kinase ALK2 inhibitors, compounds 1-3, Scheme 1. The first step will be the synthesis of key intermediate 10, Scheme 2. The proposed synthesis begins with a nucleophilic aromatic substitution on compound 4 to Read More …
In this post I’d like to return to looking at my work on phosphorylation. Phosphorylation is a key signalling method for activating the BMP pathway and inducing activity. Specifically activation of ALK2 by phosphorylation leads to phosphorylation of SMAD1 which leads to gene transcription that ultimately is responsible for bone formation. In this post I’m Read More …
In a previous post, I tested hit analogues against USP5 Zf-UBD using a SPR assay. Compound AE-641/11456811, now aptly re-named XSR00035795a (an SGC global ID- since our database infrastructure is finally re-vamped), had a binding affinity of approximately 60 µM. The addition of a methyl group on the carboxylic chain of the compound increased potency Read More …
Did you know as many as 30% of the cells in labs could be misidentified? And what a nightmare it would be to find out years of your work are just completely wrong because you got your skin cells mixed up with your brain cells… So to avoid that catastrophe, I took some time to Read More …
Hello SGC members and to the millions of scientific readers across the globe, My name is Thomas Durcan, and I am an assistant professor at the Montreal Neurological Institute (MNI) and McGill University, where I also lead the SGC tissue platform in Montreal. You can call me the stem cell guy, as everything I and my Read More …
We have received some very interesting biological data for our CaMKK2 inhibitor series (furopyridine, Azaindole and quinoline) and I will be sharing the data in the coming weeks, but before that, I wanted to share my synthetic efforts towards our quinoline series. Initial synthesis of quinoline analogs: Starting with 6-Bromo-4-chloroquinoline, a two (2) step synthetic Read More …
ZFYVE9C (Otherwise known as SARA) is a scaffold protein involved in the association of various protein components as part of the TGFB signalling pathway. The equivalent in the BMP signalling pathway is a protein known as Endofin so studying SARA (which is slightly easier) might give us useful insights for both proteins. For more details Read More …
I’ve not posted in a while, mainly because things have been really busy, but good busy, as I now have 3 new datasets/structures, of ALK2 with M4K2118, M4K2149 and, amazingly, M4K2009. As you know, this is our lead candidate, which until now has not behaved very well in crystal trials, and it hasn’t been possible Read More …
