Chemical Biology is a rapidly evolving field with the ambitious goal of dissecting biological processes in organisms and cells by producing highly-specific and tightly binding small molecules for each expressed protein.

Such direct small molecule-protein interactions can activate or inactivate the protein and trigger cellular or whole body phenotypic changes resulting in the identification of this protein function. There is no doubt that such work will also reveal new drug targets.

Medicinal Chemistry can be considered as a component of Chemical Biology with the more specific objective of producing small molecules having drug-like characteristics and regulating disease-related biological phenotypes by binding to specific proteins (although non-specific molecules can also be useful drugs).

These small molecules can be produced by organic chemistry, extraction from natural sources or by hemi-synthesis.

If synthetic molecules are often privileged in current drug research because they are more adapted to high throughput screening, optimization and industrial scale-up, the rich diversity and functionality of natural products associated with their potency and selectivity continue to be of major interest. Indeed, natural products can be viewed as a population of privileged structures selected by evolutionary pressures to interact with a wide variety of proteins. Therefore, there is no doubt that they will continue to generate indispensable chemical probes and excellent drugs. However, the strategies retained for total synthesis of natural products should ideally be adapted to the production of analogs which could have simpler structures, better affinity, selectivity and/or potency or which could be derivatized and coupled through a linker to various tags or solid supports to help identify their biochemical target(s).

This international conference on Medicinal Chemistry aims to bring together people concerned by the multiple aspects of Chemical Biology and Drug Discovery.

Jean-Pierre Maffrand, Ph.D.

Former VP, Director Discovery Research, Sanofi-Aventis