Designing new molecules for Tomorrows Drugs
The laboratory is researching the design of new molecules that may eventually lead to the marketing of new drugs. Accordingly, the Caen-based laboratory is working jointly with the pharmaceutical industry, namely with the Servier Group with which the CERMN has set up a joint laboratory. Human life expectancy keeps increasing, at least in the so-called wealthy countries. But whether we want to or not, we all get old more or less quickly. Although medicine can now repair some of the damage caused by aging for a time, admittedly it can do virtually nothing when age causes brain disorders. Today, brain aging is a major focus at CERMN. Centre's Director Professor Sylvain Rault would actually like the laboratory to become a competency hub in this field. "We have special instruments, skills and expertise that are quite unique in France," he remarked. The laboratory research scientists are particularly interested in finding out whether characteristic signs or precursors exist that would make it possible to detect future disorders. Biologists are already working on brain markers. But are there also behavioral markers and when can we say that person begins to age and alter his or her relation with the world? "The loss or decrease of desires are, in my opinion, the first incontrovertible signs of aging," reported Sylvain Rault. Industrialization of two CERMN molecules underway Scientists now know that in brain neurotransmitters, serotonin plays a major part in our relation with the world. This little molecule that Sylvain Rault presents as "being able to produce many notes on a kind of piano" may settle on many sites in the human body to produce extremely varied and complex crossover actions. Indeed, serotonin enabled the design of the famous antidepressant called Prozac. Consequently, the work of the CERMN researchers focuses on understanding how serotonin works and on attempting to design drugs that could prevent brain aging. "It is essential to take care of the elderly and very elderly," said the research scientist who is also known as a man of his convictions (he has been an elected official in his town for twenty-five years) and who is not reluctant to man the battlements to defend them. The research on brain aging is conducted mainly with the Server Group at the joint laboratory. The CERMN has already proposed molecules that now have to be evaluated which is not an easy task. For clinicians, it is very hard to test the efficiency of these kinds of molecules serving to delay brain aging. Two of the molecules developed by the CERMN are now being industrialized. But it will take another five years before they can be marketed because the developments of a drug take a long time. "Ten to fifteen years can go by from the time when a molecule leaves the lab to when it is sold as a drug at the pharmacy. The best molecules cannot reach the end of the chain because they are toxic and cause side-effects," explained the CERMN Director. The scientists at the Caen-based laboratory are also developing oncology research, an extremely vast field, at the same time as their work on brain aging. Their purpose is to inhibit kinase, the enzymes that are involved in the development of cancer and cell death. Virology and antiviral research are other advanced fields at the laboratory. For the successful completion of the research, the scientists are now using very sophisticated methods. "Over the past years, we have gone from a time when pharmacologists had low-efficiency screening and testing tools, which forced them to use only a very small number of molecules, to a time of in vitro systems that we can work on directly to screen thousands of molecules." Consequently, the chemists should now be able to produce many molecules they can test, explaining the importance of new developments in chemical technologies such as combinatory chemistry. The considerable contribution of molecular modeling, providing 3D access to molecular interactions, should also be underscored. This represents an indispensable tool assisting new molecule design. The CERMN works a lot on all the chemical methodologies, especially doctoral work, conducive to the manufacture of molecules. A University Laboratory with Spin-offs Sylvain Rault, also a pharmacist, has devoted part of his career to the Ministry of the Environment. "I negotiated the protection of the ozone layer for the Montreal Protocol," he recalled with some satisfaction. Unsurprisingly, his laboratory has been working with the Ministry for a long time, especially on chemical product risk analysis. Actually, the CERMN Director has been Chairman of the Commission for the Assessment of the Environmental Toxicity of Chemical Substances at the Ministry of the Environment, for eleven years. Today, Sylvain Rault is very concerned about the problem of bees that has received much media coverage, and for good reason. Should certain pesticides be banned or not? As Co-Chairman of the Scientific and Technical Committee addressing this problem, he has always been an ardent advocate of the famous precautionary principle that he considers as, "a working principle and not as an excessively cautionary principle." "If we cannot incontrovertibly demonstrate a fact, we have to stop," he stated. Recently, the tireless man has also become Vice-Director of the National Chemical Product Library, a facility serving to list all the chemical products in the CNRS university laboratories. A job testifying to the fact that Sylvain Rault does not bear a grudge since he has long been asking for the CERMN to be granted the status of a joint CNRS laboratory. "It seems that we work well but still too much in applied research," he quipped sardonically before adding, "In the end, I prefer that CERMN is a joint laboratory with the pharmaceutical industry. That is my true calling as a pharmacist." He pointed out that the laboratory has efficient equipment, especially thanks to the support from the Region but also from the Servier Group whose yearly grant is one of the highest paid by an industrialist to research in Normandy. Although he regrets that he cannot hire more young research scientists. "There is no lack of work. If we had enough to pay them, we could immediately hire thirty of forty young scientists." Generally speaking, he deplores the many impediments to research development. On the other hand, he can be rightly proud of heading a university laboratory that has spin-offs, an approach so infrequent that it deserves to be acknowledged. After the setup of Syntheval a few years ago, another CERMN research scientist, Alexandre Bouillon, has just created his own business after winning the National Contest for the Creation of Innovative Enterprises.Contact -,CERMN - Phone +33 (0)2.31.93.41.69. Fax. +33 (0)2.31.93.11.38.,http://www.cermn.unicaen.fr,Professeur Sylvain Rault - Director, ,Source : ,ScienceTech Basse-Normandie Newsletter,http://www.basse-normandie.net/lettre/index_en.html,Free subscription : ,http://listes.cru.fr/wws/info/sciencetech.basse-normandie.en
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