Breaking Down the Silos

MipTec was preceded by a one-day symposiumon "Chemical Genomics", and although there was no universal consensus on the definition of chemical genomics, it was agreed that this content-rich symposium will be merged into the MipTec track on structure-based drug discovery.Among a number of good talks in this track was one by Dr.Robert McDowell of Sunesis Pharmaceuticals that detailed a fundamental breakthrough method in increasing the potency of protein-protein antagonists.

MipTec attracts a wide range of scientists including medicinal chemists,chemoinformaticians, biochemist assay developers, molecular biologists, and automation specialists.This eclectic mixture of scientists suggested to me that these subdisciplines are indeed starting to speak the same language and are increasingly working together in focused teams both within Biotech and large Pharma. A highlight of the Miptec conference was the presence of Dr.Chris Lipinski as the keynote speaker, author of the "Rule of Five",the guidelines for assessing the drug-like properties of small molecules. And while our compound libraries become increasingly large, the sessions on compound management were among the most popular. The MipTec poster award was shared by 3 groups.Firstly, Michael Arlt and colleagues from Merck AG were recognized for their poster on integrity issues of compounds stored in DMSO.Secondly, Dr.Maria Paola Costi and colleagues from Universita di Modena e Reggio, Emilia Italy also received an award for their poster entitled "Developing New Beta-Lactamase Inhibitors Through Structure-Based Design and Pharmacokinetic Properties Improvement". And finally, Dr.Stanislaw Piluk and his colleagues from Avalon Pharmaceuticals won for "Forward Chemical Genomics-A Novel Drug-Discovery Process Based on Genomics Technology".

Once again,the range of these topics present a flavor of the diversity of the science at this conference. The award for the best oral presentation came from the target validation session, given to Dr.Barbara Froesch of the Genetics Company Inc., Zurich, for her presentation entitled "From Fruit Flies to Potential Cures for Human Disease". This group identified candidate genes that inhibit growth and are involved in colon cancer in humans. Their work led to a molecular target that appears to be drugable, indeed an impressive example of organismal functional genomics. During the 1990's, HTS technologies dominated conferences like this, but the toolkits of the molecular biologists and the computational chemists are starting to bear fruit with more and better validated targets and better chemical starting points.Although many new disciplines have borrowed concepts and automation from the biomolecular screeners, HTS is now seen as an important, albeit less glamorous,component of the drug discovery process.

In summary, if MipTec 2003 was a snapshot of the convergence of several key disciplines finally starting to "deliver the goods",at the same time,and in the right proportions, I remain quite optimistic that this decade will bring a marked in-crease in innovative new medicines to alleviate human suffering.