Cherry Picking in Drug Discovery

The 9th MipTec (International Conference and Exhibition on Drug Discovery) will bring together researchers from a wide variety of scientific disciplines in Basel from 8 to 11 May 2006.

The scientific committee has once again succeeded in drawing up a conference program with a number of major high points and some prestigious speakers.

The more quickly a new drug can be put on the market, the earlier patients will be able to benefit from it and the longer the company producing it will be able to enjoy the profits. High levels of efficiency and effectiveness therefore play a decisive role even in the early stages of the drug discovery process.

The scientific community will be gathering from 8 to 11 May 2006 for the 9th MipTec (International Conference and Exhibition on Drug Discovery) in Basel.

MipTec covers the broad spectrum of the first two phases of drug development: drug discovery and preclinical drug optimization.

Alongside the scientific conference there is also an exhibition with almost 100 exhibitors. MipTec has a multidisciplinary approach and brings together scientists from a wide range of disciplines, including molecular biology, biochemistry, biophysics, chemistry, engineering and medicine.

The program covers the themes that are critical to modern pharmaceutical research, from the identification and validation of new targets through to the generation and optimization of the most promising candidate drugs, using both computer-based and experimental approaches.

Technological progress: The importance of structure-based drug design has increased considerably in recent years, on the one hand for the identification of lead molecules and on the other hand for the development of biomolecular screening.

It is linked with huge developments in the technologies available, ranging from experimental proteomics and computational methods for protein modeling through to automated compound databases.

"These innovations have made it possible, for example, to search through collections of millions of chemical compounds rapidly and efficiently in order to identify their specific efficacy and, like picking cherries, to choose the most promising candidates, the best of the bunch," explains Dennis France, Chairman of the Program Committee of MipTec.

Milestones in drug discovery: The pre-conference on 8 May 2006 is dedicated to milestones in drug discovery. Project leaders for blockbuster drugs such as Glivec, Viagra and Avandia will explain the process that lies behind the development of these products, including the scientific and emotional highs and lows.

In the pre-conference keynote speech Joseph Schlessinger from Yale University will describe the development of Sutent (active ingredient: sunitinib) for the treatment of the advanced stages of renal cancer and gastrointestinal stromal tumors (GIST).

This drug has recently been approved by the FDA (Food and Drug Administration) in the context of an accelerated approval process. The drug blocks the actions of several receptor tyrosine kinases (RTKs). It is well established that dysfunction in RTKs causes a number of diseases.

Increasing efficiency and effectiveness: On 9 May 2006 Gianni Gromo, Head of Discovery Research (Roche Basel), in his opening keynote speech for the main conference will look at potential ways in which both the efficiency and the effectiveness of drug research can be improved.

The parameters of target choice and time are vital for efficiency. Improvements in effectiveness may result from the appropriate choice of therapeutic targets to speed up development and reduce marketing uncertainty.

The process is also subject to powerful influences from non-scientific parameters such as the organizational culture, the leadership style and the management of technology transfer.

On 10 May 2006 Timothy Wells, Head of Research at Serono, will give a special keynote speech on the combination of high throughput protein expression and biological assays.

His company uses this approach to develop biotechnological products, such as cytokines or antibodies, alongside methods which highlight the development and progression of the disease under the influence of drugs.

A complex and varied process: Drug discovery is often represented as a linear process, but the reality is much more complex. This simplified view fails to capture the many techniques that are used to find active molecules and establish safety and efficacy profiles.

Researchers at MipTec will be reporting on the limits of the predictability of in vitro and in vivo models and highlighting the huge differences between the development of small molecular weight drugs and protein therapeutics.

Virtual databases and real sample collections: 35,000 three-dimensional protein structures are now stored in databases and tens of millions of chemically feasible compounds are also available. More are being added every day.

This means that it is now possible to investigate the efficacy of huge numbers of substances in silico and to optimize their structure.

Experimental techniques such as crystallography and NMR provide support for searches of this kind. The use of the latest technology will be illustrated at the conference using concrete examples.

The storage and management of compound collections using automated systems is now commonplace in the pharmaceutical industry. The storage conditions play a decisive role in the quality of the samples.

At MipTec tools and applications will be presented which will improve the effectiveness and flexibility of high quality sample management operations.

New technologies open up innovative fields of research: Proteomic methods have made available a wide variety of biomarkers for drug discovery and for validation processes.

The latest developments in this field have increased the throughput of pharmacodynamic analyses and opened up innovative fields of research.

As a result multi-sensor imaging of neuronal activity can now be used to investigate the effect of psychotropic drugs on the brain. The new field of metabolomics allows biomarkers to be identified in biological fluids.

New technologies are also contributing to making drugs safer. The pharmaceutical industry is shifting the emphasis to higher quality and more relevant assays.

New technologies that are being presented at MipTec, such as image analysis applications, are currently being used in this context.

Scientific exchange: The aim of many researchers is to take a decisive step forward in the development of drugs to treat previously incurable illnesses.

As Christopher Lipinski from Pfizer, the inventor of the "Rule of 5", will demonstrate in his closing keynote speech, drug discovery works best when biological researchers interface with medicinal chemists in the context of competent project management.