A Virtual Professor Teaching Virtual ADME, Screening and Drug Design

Since the summer of 2005, Peter Grootenhuis started as "bijzonder hoogleraar", i.e. 'extra-ordinary professor' Virtual ADME, Screening & Drug Design in the division of Molecular Toxicology at the LACDR-VU in Amsterdam. Don't expect to see Grootenhuis walking around in the VU hallways or labs; he actually resides and works in San Diego, California. Most of his contacts with the VU will therefore be via internet, e-mail and telephone, although he plans to visit and stay at the VU 5-10 days a year.

Grootenhuis studied chemistry in Utrecht, and got his PhD with prof. David Reinhoudt in Twente. After that he worked as post-doc at the UC San Francisco with prof. Peter Kollman. In 1989 he returned to the Netherlands and started to work at Organon, Oss. "After nine years I was ready for a change", says Grootenhuis, and change is what he got when he accepted an offer to move to a small biotech in San Diego called CombiChem. This turned out to be the start of a roller coaster ride of rapid acquisitions and spin-offs involving four companies in less than four years. However, since 2002 Grootenhuis works with Vertex Pharmaceuticals in San Diego, where he is responsible for medicinal and computational chemistry. "A recent very extensive review in Drug Discovery Today on 'High-througput Cyt P450 inhibition screens in early drug discovery illustrates' that I am still in the position to publish good articles together with my co-workers, while I am having this responsibility", says Grootenhuis.

It is not the first time Grootenhuis is taking on a part-time professorship. Earlier he was appointed in Groningen and Twente, and he is still involved with teaching a medicinal course at the UC San Diego. "My contacts with the VU date back to my time with Organon when professor Timmerman invited me to teach some lectures in his medicinal chemistry course. Timmerman thought it would be insightful for students to learn about medicinal chemistry from an industrial perspective."

Peter Grootenhuis' position is a new part-time chair paid for by the Stichting Het Vrije Universiteitsfonds and positioned within the division of Molecular Toxicology, directed by professor Nico Vermeulen. In addition to teaching Grootenhuis is also interested in collaborating with Vermeulen's group on computational modelling of cytochrome P450 - ligand interactions. "By combining the expertise Vermeulen's group has in this area with a unique experimental Cyt P450 inhibition data set for hundreds of drugs that was generated at Vertex, we hope to push Cyt P450 modelling and prediction to the next level. This is of great interest to the pharmaceutical industry, since poor pharmacokinetics and toxicology are important factors in the attrition of drugs in clinical development." Grootenhuis continues: "If we could in an earlier research stage flag molecules with a potential for drug-drug interactions due to potent Cyt P450 inhibition or steer away from molecules with a risk for in vivo toxic metabolite formation, it could save millions of dollars and increase the chance of success." The latter is needed urgently. In 2005 only 20 new drugs were approved by the FDA despite multi-billion dollar investments by the drug industry.

Why become a professor nine time zones away from where you live? "I still have many friends in Dutch science and industry and I'd like to keep those contacts going. Thus I initiated a collaboration between Syncom (Groningen) and Vertex and we also collaborate with Hugo de Jonge from the Erasmus University in the area of cystic fibrosis (CF)." As project leader Grootenhuis is closely involved in CF research at Vertex. "I feel that it is extremely important that the drug industry also works on orphan diseases. If we can generate a therapeutic breakthrough in a genetic orphan disease like CF it will benefit patients but also may positively impact the rather bad image the pharmaceutical industry currently has."

What do you do in your free time in San Diego? "Our three children pretty much keep my wife and myself busy during the weekends. Like many other parents we spend a lot of time transporting our kids to and from the soccer or baseball field or beach. We live close to the desert and I enjoy stargazing in the dark desert skies." Any time for sports? "I am training very hard to get my karate black belt. As a student at Utrecht I already was involved with martial arts. I picked it up again only four years ago and really enjoy it."

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