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Research Description:
Dr. Day's lab is interested in the discovery and development of drugs to treat solid tumors. The lab uses computational chemistry, synthetic medicinal chemistry, biochemical methods, cell biology, molecular techniques, radio- and stable isotope labeling syntheses, mass spectrometry and animal models to discover new agents then study their mechanisms of action. Projects include: design and synthesis of truncated versions of the potent microtubule stabilizer discodermolide; high-throughput biochemical and cell based screening of parallel and combinatorial libraries of anti-tubulin and anti-dynein agents; characterization of changes in signal transduction cascades by synthetic agents; parallel solid- and solution-phase synthesis of 1,1-dichloro-2,2,3-triarylcyclopropanes and 2,3-diarylcyclopropyl phenyl ketones as estrogen receptor modulators; and quantitative structure-activity relationship analyses of synthetic libraries. The lab also collaborates extensively both in and outside the university in the areas of computational design/discovery, synthesis, redox biochemistry and both small molecule and macromolecule mass spectrometry (proteomics).
Education:
B.S. (Chemistry & Biology), Oklahoma City University, 1982
Ph.D. (Medicinal Chemistry), University of Oklahoma, 1988
Postdoctoral Fellow, Massachusetts Institute of Technology, 1988-91
Important Publications:
- Buey, R.M., Calvo, E., Barasoain, I., Pineda, O., Edler, M.C., Matesanz, R., Cerezo, G., Vanderwal, C.D., Day, B.W., sorensen, E.J., Lopez, J.A., Andreu, J. M., Hamel, E., Diaz, J.F. Cyclostreptin binds covalently to microtubule pores and lumenal taxoid binding sites. Nature Chem. Biol. 2007, 3, 117-125., 2007
- Beckner, M.E., Zhang, Z., Agostino, N.R., Day, B.W., Pollack, I.F. Albumin marks pseudopodia of astrocytoma cells responding to hepatocyte growth factor or serum. Lab. Invest. 2006, 86, 1103-1114., 2006
- Hamel, E., Day, B.W., Miller, J.J., Jung, M.K., Northcote, P.T., Ghosh, A.K., Curran, D.P., Cushman, M., Nicolaou, K.C., Paterson, I., Sorensen, E.J. Synergistic effects of peloruside and laulimalide with taxoid site drugs, but not with each other, on tubulin assembly. Mon. Pharmacol. 2006, 70, 1555-1564., 2006
- Fan, Y., Schreiber, E.M., Giorgianni, A., Yalowich, J.C., Day, B.W. Myeloperoxidase-catalyzed metabolism of etoposide to its quinone and glutathione adduct forms in HL60 cells. Chem. Res. Toxicol. 2006, 19, 937-943, 2006
- Zhu, G., Yang, F., Balachandran, R., Hook, P., Vallee, R., Curran, D.P., Day, B.W. Synthesis and biological evaluation of purealin and analogues as cytoplasmic dynein heavy chain inhibitors. J. Med. Chem. 2006, 49, 2063-2076., 2006
- Kangani, C.O., Kelley, D.E., Day, B.W. One-pot direct synthesis of oxazolines, benzoxazoles, and oxadiazoles from carboxylic acids using the Deoxo-Fluor reagent. Tetrahedron Lett. 2006, 47, 6497-6499., 2006
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