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Webster L. Santos, Ph.D.


Phone: (540)231-5742
Mailing Address:
Department of Chemistry (0212)
Davidson Hall Rm 480, Virginia Tech
1040 Drillfield Drive
Blacksburg, VA 24061

Curriculum Vitae (04/2024) Download

Prof. Webster Santos received his BS and PhD from the University of Virginia under Prof. Timothy Macdonald. Following his doctoral studies, he moved to Harvard University as a Ruth Kirschtein NIH fellow with Prof. Gregory Verdine. At Harvard, he performed chemical biology studies targeting RNA structures as well as HIV-1 integrase. In 2006, he started as an assistant professor of chemistry at Virginia Tech and was promoted to associate then full professor in 2018. He held a chaired position as the Blackwood Junior Faculty fellow of Life Science and is currently the Agnes and Cliff Lilly faculty fellow of drug discovery. He is a co-founder of three biotech companies and received the Schug Research Award as well as an Innovator’s award at Virginia Tech. He is on the editorial advisory board of current topics in medicinal chemistry, medicinal research reviews as well as boron in the Americas. His current research centers on developing drugs towards fatty liver disease, cancer, and multiple sclerosis, synthetic methodology of installing boron and silicon onto carbon bonds and chemical biology of targeting HIV-1 RNAs.


  • 2024 Director, Virginia Tech Center for Drug Discovery
  • 2023 College of Science Faculty Fellowship
  • 2022-2023 Outstanding Undergraduate Research Faculty Mentor
  • 2022-2025 Standing Member, Chemical Biology and Probes (CBP) NIH study section
  • 2021 Executive Committee, Virginia Drug Discovery Consortium
  • 2021 Outstanding Mentor Award, Virginia Tech
  • 2021-2022 Standing member, Synthetic and Biological Chemistry B (SBCB) NIH study section
  • 2019 Fellow of the Royal Society of Chemistry
  • 2019 Editorial Board, Molecules, Medicinal Chemistry Section
  • 2019 Co-Founder, S1P Therapeutics, Inc. 
  • 2017 Editorial Board, Medicinal Research Reviews
  • 2017 Co-Founder, Continuum Biosciences, Inc.
  • 2015-present Editorial Advisory Board, Current Topics in Medicinal Chemistry
  • 2014 Innovators Award, Virginia Tech
  • 2014-present Cliff and Agnes Lilly Faculty Fellow of Drug Discovery
  • 2014 John C. Schug Research Award
  • 2014-present Associate Editor, Diversity Oriented Synthesis
  • 2013-present Alternate Councilor, Division of Biological Chemistry, American Chemical Society
  • 2012 ACS Young Academic Investigator
  • 2011 Molecular Biosystems Emerging Investigator
  • 2010-2015 Co-founder, SphynKx Therapeutics, LLC
  • 2010 Chemical Communications Emerging Investigator
  • 2010-2014 Blackwood Junior Faculty Fellow of Life Sciences
  • 2009 Molecular BioSystems Emerging Investigator
  • 2002-2006 Ruth Kirstein NRSA Post Doctoral Fellowship
  • 2002 Third Prize Winner, Robert J. Huskey Graduate Research Symposium, University of Virginia
  • 1998 Outstanding Graduate Teaching Assistant Award
  • 1996 Semi-finalist for Seven Society Teaching Fellowship, Secret Seven Society, University of Virginia

The Sphingosine Kinase Inhibitors below are licensed to Avanti Polar and are available from their website

857380 –  SLP7111228 

857381 – SLM6031434

857382 – SLC5111312


  1. Santos, W.L.; Lynch, K.R., Kharel, Y.; Fritzemeier, R. “Inhibitors of Spinster Homology 2 (SPNS2) of use in therapy”, US Patent Application Serial No.: 63/076,105, PCT Application No. PCT/US2021/049534. September 9, 2021.   
  2. Santos, W.L.; Lynch, K.R., Kharel, Y.; Peralta, A.; Fritzemeier, R. “Inhibitors of Spinster Homology 2 (SPNS2) of use in therapy”, US Patent Application Serial No.: 63/076,111, PCT Application No. PCT/US2021/049531. September 9, 2021. 
  3. Santos, W.L.; Lynch, K.R., Kharel, Y.; Peralta, A.; Fritzemeier, R.; Foster, D. “Inhibitors of Spinster Homology 2 for Use in Therapy”, January 25, 2019, U.S. Patent Application Serial No.: 62/797,054.
  4. Santos, W.L.; Murray, J.; Dai, Y.; Santiago-Rivera, J. “Imidazopyridines Useful as Mitochondrial Uncouplers”, April 22, 2019, PCT International Application No.: PCT/US2019/028555.
  5. Santos, W.L.; Salamoun, J.; Murray, J.; Garcia, J. “Oxadiazolopyrazines and Oxadiazolopyridines useful as Mitochondrial Uncouplers”, April 22, 2019, PCT International Application No.: PCT/US2019/028544.
  6. Santos, W.L; Murray, J.; Nekvinda, J.; Burgio, A. “Aminopyrazines and Related Compounds Useful as Mitochondrial Uncouplers”, April 22, 2019, PCT International Application No.: PCT/US2019/028560.
  7. Santos, W.L.; Fritzemeier, R. “A process for making 3-substituted-1,2-oxaborol-2(5H)-ol”, July 8, 2019, U.S. Patent Application Serial No.: 62/871,564
  8. Santos, W.L.; Lynch, K.R.; Li, H.; Kharel, Y. “Compositions and Methods for Preparing and Using Pyrrolidine-Based Inhibitors Of Sphingosine Kinase 1”, U.S. Provisional Patent Application Serial No. 62/547,276, August 18, 2017.
  9. Santos, W.L.; Hoehn, K. Childress, E. “Compositions and Methods for Preparing and Using Mitochondrial Uncouplers”, U.S. Provisional Patent Application Serial No. 62/509,249, Priority filing date: May 22, 2017.
  10. Thorpe, B. T.; Santos, W.L.; Lynch, K.R. “Sphingosine Kinase Inhibitor Prodrugs”, March 2017, PCT/US2017/024852.
  11. Santos, W.L.; Lynch, K.R.; Childress, E.; Kharel, Y. “Guanidine-Based Aminothiazole Inhibitors of Sphingosine Kinase”, U.S. Patent Application No: 62/205,196, Priority filing date: August 14, 2015.
  12. Santos, W.L.; Lynch, K.R. “Sphingosine Kinase Inhibitors”, US Patent Patent No. 10,100,022 issued October 16, 2018.
  13. Santos, W.L.; Raje, M.R.; Lynch, K.R.; Macdonald, T.L.; Kennedy, A. and Kharel, Y. “Long Chain Base Sphingosine Kinase Inhibitors”, PCT/US2013/025341, February 8, 2013. Priority filing date: February 8, 2012. US Patent No. 14377300 Issued June 27, 2017.
  14. Santos, W.L. and Lynch K.R. Sphingosine kinase inhibitors and therapeutic use thereof. US Patent Appl. 61/375,478, Aug. 2010.
  15. Santos, W.L. Branched peptides as therapeutics for structured RNA targets. US Patent Appl. 61/269,571, June 2009.
  16. Santos, W.L. and Gao, M. Synthesis and uses of mixed diboron reagents. US Patent Appl.61/225,032 July 2009.
  17. Santos, W.L. Inhibition of proteases using N‐terminal peptidic boronic acids. US Patent Appl. 61/234,399 August 2009.
  18. Santos, W.L. and Verdine, G.L. Oligonucleotide microarrays comprising nucleic acid analogs for hybridization with target RNA, including RNA in nucleoprotein complexes. PCT Int. Appl. 2005, 60 pp.
  19. Lynch, K.R.; Macdonald, T. L.; Heise, C.H.; Santos , W. L . and Okusa, M.D. Novel Lysophosphatidic Acid Receptor Agonists and Antagonists. PCT Int. Appl. 2002, 81 pp.