24 Feb 2012
Messel Travel Bursar Mark Rackham reports from The International Symposium on Advances in Synthetic and Medicinal Chemistry (ASMC) in St. Petersburg, Russia on the 21-25 August 2011.
I was given the opportunity to present a poster on my PhD project entitled: A Novel Approach to the Treatment of Malaria: Design and Synthesis of N-Myristoyltransferase (NMT) Inhibitors. By adaptation of anti-fungal NMT inhibitors developed by Roche, a series of selective inhibitors for plasmodial NMT with micromolar affinities were discovered. Utilising a scaffold-hopping approach yielded a structurally novel compound with an IC50 of 4 μM, which was further modified through iterative medicinal chemistry resulting in a series of lead compounds with inhibition constants < 20nM. The most valuable learning from presenting my work was the recognition that regardless of the quality of the medicinal chemistry, a complete understanding of the biological mechanisms of drug action is a pre-requisite for success for target based drug discovery.
From my perspective as a PhD student, one of the main advantages of this kind of symposium is the exposure to some of the cutting edge technologies that are being developed in the overlapping fields of medicinal and synthetic chemistry. Some of the highlights included two fascinating talks on the developing field of epigenetics by Dr. Mark Bunnage (Pfizer) and Dr. Jason Witherington (GSK). The field offers a lot of potential to reveal more robust drug targets due to the importance of epigenetic mechanisms in multiple biological processes. Prof. Flygare (Stanford and Genentech) also delivered a fascinating talk on using the high selectivity of antibodies to efficiently target cytotoxic drugs to cancer cells, resulting in chemotherapies with fewer side effects. On the synthesis side, one particular highlight was the incredible work of Prof. Yu (Scripps), who is working on assembling natural products entirely using C-H activation. Although my main interest is medicinal chemistry, these technologies are likely to have a lot of utility in the synthesis of bioactive compounds.
This conference will have a large impact on my career, principally due to the contacts made during the symposium. I was able to meet many high profile figures in Medicinal Chemistry from both industrial and academic institutions, and the opportunity to do this in an informal context was really valuable. Aside from the science discussed at the conference, it was fascinating to get their opinions on the directions the industry is headed, as well as what they look for in a post-doctoral candidate!
I have presented a short conference report to my research group, highlighting some of the biggest advances in complementary (and competing) research groups. More unofficially, getting a broad overview of world class research in the field can allow me to suggest promising post-doctoral opportunities to some of my co-workers.
I would like to thank SCI for providing me with a travel bursary, without which I would not have been able to attend this fantastic conference.
Mark Rackham
Imperial College, London
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