Metabolic stability assessment
On a yearly basis, thousands of new molecules are developed by the pharmaceutical industry in the Netherlands alone. Those compounds have to be tested by pharmacologists and toxicologists for properties like their effect on diseases, the way they react in the human body and the way the human body reacts to them. The current method of producing compounds is usually through chemical means.

This project aims to develop ways to use human genes to develop certain molecules. To achieve this a mutated version of a certain enzyme is used. One of the big advantages of using a biological route to produce molecules is that it opens up a completely new scale of molecules that could not be produced chemically. Additionally, some of the produced molecules are more effective towards or selective for certain targets. So far several mutants have been developed, capable of producing biosynthetic compounds. To increase efficiency, a technological platform was designed to measure the effectiveness of the developed compounds as well as creating a library with dozens of mutants. This combination can grant bioinformaticians insight in the mechanics of enzymes. This knowledge can eventually lead to more precise and efficient medicines.

Fast facts
Full project title: Metabolic stability assessment as a new tool in the Hit-to-Lead selection process and the generation of new lead compound libraries
Start date: September 2007
End date: September 2012
Goal: Development and application of biosynthetics and analytical technologies to generate and fully characterize new compound libraries for drug discovery
Principal investigator: Maarten Honing
Project size: 6,5 FTE's
Partners: MSD, Radboud University Nijmegen, VU University Amsterdam, Xendo Drug Development BV 

PhD theses from this project

Ard Kolkman (project D2-102)
NMR Spectroscopy in Drug Discovery

“What TI Pharma can deliver from collaborations is more efficient healthcare, faster time to market and quicker patient benefit.”

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