DEPRECATED
This site is no longer maintained as of January 16th, 2013. Due to the increased security risks of this out-dated application , it will be decommissioned July 1st 2013. Please migrate use over to its replacement http://bioconnect.bio5.org. Direct questions and concerns to bio5admin@bio5.org. Thank you.
Josef Vagner
Associate Research Professor
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Lead of the Ligand Discovery Lab (LDL) at Bio5, University of Arizona. The current research projects deal with the development of ligands, inhibitors, and diagnostic probes in collaboration with the AZCC, UNMCC, TGen, Department of Radiology and Department of Biochemistry.
The Ligand Discovery Laboratory (LDL) is a complex chemistry center supporting investigators with libraries of chemical compounds and provides their screening.
The primary objective of the LDL is the design, synthesis, purification, characterization and screening of arrays of unique compounds for drug discovery. The LDL uses the following technologies:
- Solid-phase synthesis (small organic compounds, biopolymers)
- High throughput synthesis (96-well plates)
- One-bead-one-compound (OBOC) library synthesis
- Rational design of small molecule ligands, multimeric ligands, peptidomimetics
- Lanthanide-based time-resolved fluorometry in vivo binding assay
- In vivo cell-adhesion-to-bead assay for OBOC library
- HT synthesis of labeled probes (fluorescent, DOTA-Eu)
- Logistics and QC
Lead structures can undergo multiple development cycles. At each cycle, we will look for improvement in binding affinity, selectivity, physico-chemical properties (solubility, stability), and suitability for imaging, which is the most important parameter. Structural, analytical and storage data are entered into a database (ChemOffice, CambridgeSoft) which is compliant with the Molecular Libraries and Imaging Initiative (MLII) database.
Selected Publications
. Jan 2008. Gold nanorods targeted to delta opioid receptor: plasmon-resonant contrast and photothermal agents. Mol Imaging, 7:50-7
. Mar 2008. A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists. J Med Chem, 51:1369-76
. Jan 2008. Heterobivalent ligands crosslink multiple cell-surface receptors: the human melanocortin-4 and delta-opioid receptors. Angew Chem Int Ed Engl, 47:1685-8