- Integrative Metabolic Production and Profiling as a Novel Strategy in Hit-to-Lead Selection
In modern drug discovery innovative, efficient and throughput-directed metabolic stability assessment and metabolic profiling, i.e. metabolite identification and active metabolite screening, is becoming of key-importance. In this TI Pharma project, a new consortium, of the Leiden-Amsterdam Center of Drug Research (LACDR) at the Vrije Universiteit (Amsterdam), the Institute of Molecules and Materials (IMM) at the Radboud Universiteit (Nijmegen) and Organon BioSciences (Oss) has been created to develop innovative and integrative strategies for metabolite production, metabolic stability assessment and metabolite profiling. The new strategies are based on integration of combinatorial biochemistry and biocatalysis with Cytochromes P450, high-information content LC-MS, high-efficient LC-NMR and structure identification software routines.