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Webster L. Santos

Associate Professor

Bioorganic and Medicinal Chemistry

Office: 3101 Hahn Hall South
Phone: 540-231-5742
Fax: 540-231-3255
Group Web Pages:

BS University of Virginia, Charlottesville, VA, 1997
PhD University of Virginia, Charlottesville, VA, 2002
NIH Postdoctoral Fellow, Harvard University, Cambridge, MA, 2002-2006

Assistant Professor of Chemistry, Virginia Tech, 2006
Associate Professor of Chemistry, Virginia Tech, 2013

Honors and Awards:

ACS Young Academic Investigator, Philadelphia, PA, 2012
Molecular Biosystems Award Symposium, 2011
Co-founder, SphynKx Therapeutics, 2010
Chemical Communications Emerging Investigator, 2010
Blackwood Junior Faculty Fellow of Life Sciences, 2010-present
Molecular BioSystems Emerging Investigator, 2009
Ruth Kirstein NRSA Fellow, 2003-2006

We are interested in using chemistry to understand biological processes. Central to our theme is organic chemistry as a tool that intersects with molecular life sciences such as molecular and cell biology. Our primary focus is the development of chemical toolboxes to address problems in biology. Currently, our work is aimed at the following:

  • Development of novel diboron reagents for the mild and selective boration of activated carbon-carbon bonds
  • Development of medium-sized branched peptides to target RNA structures associated with HIV as the next generation anti-HIV therapeutics
  • Defining the roles of sphingosine kinases in hyperproliferative diseases by developing cell permeable small molecule libraries as probes
  • Development of N-terminal peptidic boronic acids as protease inhibitors
  1. Zhang, W.; Bryson, D.I.; Crumpton, J.B.; Wynn, J. and Santos, W. L. Branched Peptide Boronic Acids (BPBAs): A Novel Mode of Binding Towards RNA. Chem. Commun. 201349, 2436-2438. DOI: 10.1039/C3CC00243H.
  2. Bryson, D.R.; Zhang, W.; McLendon, P.M.; Reineke, T.M. and Santos, W.L. Toward Targeting RNA Structure: Branched Peptides as Cell-Permeable Ligands to TAR RNA. ACS Chem. Biol. 2012, 7, 210–217. DOI: 10.1021/cb200181v.
  3. Kharel, Y.; Raje, M.; Gao, M.; Gellett, A.M.; Tomsig, J.L.; Lynch, K.R. and Santos, W.L. Sphingosine kinase type 2 inhibition elevates circulating sphingosine-1-phosphate. Biochem. J. 2012447, 149-157.doi:10.1042/BJ20120609
  4. Raje, M.R.; Knott, K.; Kharel, Y.; Bissel, P.; Lynch, K.R. and Santos, W.L. Design, synthesis and biological activity of sphingosine kinase 2 selective inhibitors. Bioorg. Med. Chem. 201220, 183-194.DOI:10.1016/j.bmc.2011.11.011.
  5. Calderone, J.A. and Santos, W.L. Copper(II)-Catalyzed Silyl Conjugate Addition to α,β-Unsaturated Conjugated Compounds: Brønsted Base-Assisted Activation of Si–B Bond in Water. Org. Lett. 2012, 14, 2090-2093. DOI: 10.1021/ol300618j
  6. Thorpe, S.B.; Calderone, J.A. and Santos, W.L. Unexpected copper (II) catalysis:  Catalytic amine base promoted β-borylation of α,β-unsaturated carbonyl compounds in water. Org. Lett. 201214, 1918-1921. DOI:10.1021/ol300575d.

    Webster Santos