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U.S. National Institutes of Health
Last Updated: 10/28/10

University of Minnesota Chemical Diversity Center

Director: Dr. Gunda I. Georg

The University of Minnesota Chemical Diversity Center is based primarily on the capabilities of the Institute for Therapeutics Discovery and Development (ITDD) and the Department of Medicinal Chemistry in collaboration with the NCI-designated Masonic Comprehensive Cancer Center, the College of Pharmacy, the Center for Translational Medicine, and the Minnesota Supercomputing Institute. The University of Minnesota Chemical Diversity Center’s research focus is the discovery and development of anticancer agents, using stateof-the-art chemical, biological, computational, pharmacological and imaging approaches. Its mission is to become an effective partner in the NCI’s effort toward innovative cancer therapeutics discovery.

Drug Discovery Expertise in Synthetic Medicinal Chemistry, Computer-Aided Drug Design (CADD), and Structural Biology: The expertise of the University of Minnesota Center includes strong synthetic medicinal chemistry capabilities coupled with expertise in computer-aided drug design, molecular modeling and visualization, and experimental structural biology to fully exploit structural information in the selection and optimization of chemical series for lead development. The capabilities of the CADD/ molecular modeling group include docking, pharmacophore mapping, library refinement, and QSAR formulation to guide efficient compound optimization. The structural biology group can characterize compound-target molecular interactions based on X-ray crystallographic data. The synthetic capabilities include state-of-the-art parallel synthesis and high-throughput purification systems that allow rapid synthesis and purification of chemical libraries.

University of Minnesota Chemical Diversity Center

The Chemical Process Development facility allows the synthesis of lead molecules, drug candidates and advanced intermediates (mg to kg), chemical process development and optimization, scale up, and analytical method development. Small molecules, cell- and protein-therapeutics can be prepared under cGMP conditions for preclinical investigations and Phase I clinical trials in the University of Minnesota Molecular and Cellular Therapeutics facility.

Screening and Assay Development Expertise: The High-throughput Screening Laboratory provides rapid automated screening of large number of chemical compounds against various biological targets. The facility carries out assay development and screening using biochemical and cell based assays, including HCS and the development of secondary assays. The facility’s unique capabilities include a) the Caliper LabChip LC3000 microfluidic assay system that can profile the activity of compounds over the human kinome to assess selectivity. The LC3000 can also be used as an HTS platform for the identification of kinase and protease inhibitors; b) the FLIPR Tetra for assay and screening GPCRs; c) the Meso-Scale Discovery Electrochemiluminescence assay system that can be used for multiplexed ELISA assays and ligand-ligand interaction targets; and d) the BD-Atto Pathway 855 confocal high-content imaging system used for secondary assays for compound mechanistic profiling. The chemical library available for screening at the ITDD consists of a 200,000-compound commercial library. Additional small focused libraries of peptidomimetics, natural products, and current drugs are also available for screening.

Drug Development Capabilities: The Cancer Center, the College of Pharmacy, the Center for Translational Medicine and The Clinical and Translation Science Institute (CTSI) provide support for drug development, regulatory requirements, clinical trials, and data analysis. Available are animal models of cancer, preclinical testing support for small molecule-, cell-, protein-, tissue-based, and combination therapies. These include drug formulation, in vivo preclinical efficacy studies, safety pharmacology, preliminary toxicology, PK and metabolism studies, and help with the design and execution of clinical trials. In vivo high field magnetic resonance imaging of animals is available through the Center for Magnetic Resonance Research. GMP toxicology is under development in the Experimental Surgical Services (ESS) laboratories.