Georgetown University Medical Center

The chemical diversity center at Georgetown University Medical Center has expertise in computational modeling, synthetic and medicinal chemistry, cancer biology, and preclinical modeling. Computational support includes:

• structure-guided modeling
• homology modeling
• ligand-based modeling, including pharmacophore-based approaches
• virtual screening resources including a >150-million compound virtual library

Our PhD chemistry expertise includes both medicinal and organic chemistry. Our medicinal chemists support:

• analog synthesis for hit-to-lead studies
• structure-activity analysis
• optimization
• development of spectroscopic ligands

Our synthetic organic chemistry supports:

• asymmetric synthesis of lead compounds
• small peptide and peptidomimetic synthesis
• library hit and standard re-synthesis
• natural product chemistry
• non-GMP scale-up (gram to kilogram)

Taking advantage of our location within the Lombardi Comprehensive Cancer Center, we have amassed a strong team of cancer biologists with expertise for specialized assays including:

• siRNA validation of targets in human cancer cells
• dose-dependent evaluation of compounds with low to medium throughput in human cancer cell lines (IC₅₀, etc.)
• compound evaluation on human cancer cell lines for effects on cell cycle, migration, apoptosis, and cell signaling (Western analysis)
• cellular chemosensitization and radiosensitization models
• cellular fluorescent imaging
• angiogenesis models (e.g., scratch assay, tube formation, aortic ring, and endothelial cell proliferation and selectivity)

Finally, our preclinical capabilities include:

• an array of mouse xenograft models
• mouse toxicity models (acute and chronic)
• state-of-the-art live animal imaging of fluorescent compounds to assist in tracking pharmacodynamic properties and drug localization
• animal histology
• human tissue distribution studies (for fluorescent compounds)