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6th RSC/SCI Kinase Inhibitor Design Symposium Review

Nick C Martin

19 Jun 2014

With a generous bursary from SCI I was able to attend the '6th RSC/SCI Kinase inhibitor design symposium' at the idyllic Babraham research campus just outside Cambridge, from 19-20 May 2014, writes Nick C Martin. I am currently in my third year of PhD study centred on the design and synthesis of small molecule kinase inhibitors, which made this conference of particular relevance.

The event provided a programme of 16 high calibre speakers from leading pharmaceutical companies and renowned research institutes, accompanied by a poster session. An interactive panel discussion in the schedule allowed the audience to question the speakers on arising science in the field and the patterns in research to date. This portion of the conference was excellent, researcher leaders spoke off the cuff and frankly about real issues and the attendees left with a better understanding of the current attitudes and the future of the discipline.

A number of talks addressed problems with the pharmacokinetic profile of compounds and in particular efflux from cells by transporter proteins. This is something I have also studied during my studies and therefore gained a great deal from these talks.

The talk which most intrigued me was given by Dr Sharan Bagal, of Pfizer-Neusentis, entitled 'The discovery and optimisation of a series of potent, selective and CNS restricted pan-Trk ligands for pain'. Inhibition of this target had shown potential for a therapeutic response however inhibition in the central nervous system (CNS) is associated with toxicity and therefore a strategy was devised to keep the drug out of the CNS.

Dr Bagal's team purposefully designed their inhibitors to be substrates for the transporter proteins P-gp and BCRP, something which is not typically a desirable feature in a drug molecule as these proteins are responsible for eliminating foreign material from cells. These transporters however are more abundant in the CNS which effectively means that a substrate for the transporters will have a higher concentration in cells outside of the CNS and very little or no presence in the CNS and therefore the desired selectivity is achieved.

This was a really well-delivered and interesting talk early on in the conference and set the tone for the rest of the proceedings.

Overall this event was excellent and I would thoroughly recommend it to someone working in the kinase field. It was also a great opportunity to network, because the majority of attendees came from industry; as a PhD student in his final year I was especially glad of the chance to speak to a number of potential employers.

I would like to thank SCI for awarding this bursary and making my attendance at this conference possible.

Nick C Martin
Northern Institute for Cancer Research
Newcastle University

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