Boron in Québec

Last night my second year PhD student Adam Zajdlik came back from Sherbrooke, where he attended the QOMSBOC meeting (Québec-Ontario Minisymposium in Synthetic and Biological Chemistry). This is an annual event that gathers together students, postdocs and faculty in either Québec or Ontario (alternating years). This year it was Québec’s turn and from what I hear Guillaume Bélanger did a great job organizing the conference. The format is such that it is mainly students who give talks and posters. Two invited academic faculty members and one industrial lecturer are also included in the program. I organized one of these conferences in Toronto back in 2008. It was a blast working with the students on the logistics of the conference.

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Adam gave a talk and received one of the prizes for his oral presentation, which made us all very happy. I also commend him for waking up early on Sunday to deliver his talk (at 8:30am). I recall the amount of alcohol consumed by the participants at our own event back in 2008. I was happy to see people walk the next morning, let alone think about science! Adam and I salute all of those students who had the strength to get up and show up in the early Sunday hours. In terms of chemistry, Adam is continuing his inroads in the area of boron-containing bioactive molecules. We remain committed to exploring the potential of boron. Boromorpholinone is one of Adam’s favorite scaffolds. On particular boromorpholinone he developed is a nanomolar inhibitor of proteasome 20S (this finding comes from our joint with Professor Aaron Schimmer). We are still debating on the mode of action of our compound and are currently leaning towards in cellulo linearization. A view is shown above. This covalent docking result was obtained using Glide and we will be trying to get a co-crystal now. You can see that, due to its oxophilicity, boron binds to the hydroxyl group of Thr1 (boron is green). This finding has enabled us to start a collaboration with Professor Ben Cravatt of Scripps (http://www.scripps.edu/cravatt/). I hope to disclose the details of this work one day soon, when the paper is ready. Suffice is to say that there are some really interesting leads Ben and his student Micah have been getting.

Again, congrats to Adam!

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