.

Fesik Lab

TAEKYU LEE, Ph.D.

 
 

 

Research Assistant Professor of Biochemistry  

 

Office:      802 RRB

Phone:     615-936-8698

Email:      taekyu.lee@vanderbilt.edu

 

Medicinal Chemistry

 

Taekyu Lee, Ph.D. is a Research Assistance Professor of Biochemistry in Vanderbilt University School of Medicine. The focus of his research is on fragment- and structure-based cancer drug discovery. Dr. Lee is a synthetic organic/medicinal chemist with extensive knowledge and experience in all phases of drug discovery process. He was a Principal Scientist in the drug discovery department of DuPont Pharmaceutical and Bristol-Myers Squibb Companies for 11 years prior to joining the Professor Fesik’s group at Vanderbilt. Throughout his industrial carrier, he contributed to a number of drug discovery programs against CNS disorders, obesity and diabetes and also gained practical knowledge and experience in early drug discovery program development, hit to lead validation, optimization of efficacy and pharmaceutical properties of drugs through SAR, cheminformatics, molecular modeling and the preparation of patents. He also participated in discovery and advancing several compounds to the clinic. He received Ph.D. in organic chemistry under Professor J. Bryan Jones at University of Toronto and conducted a post-doctoral research in the professor Chi-Huey Wong’s laboratory at the Scripps Research Institute.  Dr. Lee has published 12 papers and 22 patents.

SELECTED PUBLICATIONS AND PATENTS

  1. Ruben J.-R. Hwu*, Taekyu Lee, and Bryant Gilbert  “Counterattack Reagent: Hexamethyldisilane in a Direct Synthesis of Ketene Dithioacetals and 2-Trimethylsilyl-1,3-dithiane Derivatives from 1,3-Dithiane.”  J. Chem. Soc., Perkin Trans. I   1992, 3219-3223
  2. Taekyu Lee and J. Bryan Jones* “Probing Enzyme Stereospecificity. Evaluation of β-Alkoxy-a-amino Acids with Two Stereocenters as Inhibitors of Serine Proteases.”  Tetrahedron  1995, 51, 7331-7346.
  3. Taekyu Lee and J. Bryan Jones*  “Probing the Abilities of Synthetically Useful Serine Proteases to Discriminate between the Configurations of Remote Stereocenters Using Chiral Aldehyde Inhibitors.”  J. Am. Chem. Soc. 1996, 118, 502-508.
  4. Pierre R. Bonneau, Richard Martin, Taekyu Lee, Roman Sakowicz, Valeri Martichonok, James K. Hogan, Marvin Gold and J. Bryan Jones*  “Enzymes in Organic Synthesis. Present and Future.”  J. Braz. Chem. Soc.  1996, 7, 357-369.
  5. Taekyu Lee, Roman Sakowicz, Valeri Martichonok, James K. Hogan, Marvin Gold and J. Bryan Jones*  “Probing Enzyme Specificity.”  Acta Chem. Scan.  1996, 50 (8), 697-706.
  6. Taekyu Lee  “Probing the Remote Stereocenter Selectivity of a-Chymotrypsin and Subtilisin Carlsberg.” Diss. Abstra. Int., B  1997, 57, 5056.
  7. Taekyu Lee and J. Bryan Jones*  “Probing the Abilities of Synthetically Useful Serine Proteases to Discriminate between the Configurations of Remote Stereocenters using Chiral Naphthyl-aldehyde Inhibitors.”  J. Am. Chem. Soc. 1997, 119, 10260-10268.
  8. Taekyu Lee, Gary S. Laco, Bruce E. Torbett, Howard S. Fox, Danica L. Lerner, John H. Elder*, Chi-Huey Wong*  “Analysis of the S3 and S3’ Subsites of FIV Protease Potent Inhibitors: Development of a Broad-based Protease Inhibitor Efficacious against FIV, SIV, and HIV in vitro and ex vivo."  Proc. Natl. Acad. Sci. 1998, 95, 939-944.
  9. Taekyu Lee, Van-Duc Le, Dongyeol Lim, Ying-Chuan Lin, Garrett M. Morris, Andrew L. Wong, Arthur J. Olson, John H. Elder, Chi-Huey Wong*  “Development of a New Type of Protease Inhibitors , Efficacious against FIV and HIV Variants.”  J. Am. Chem. Soc. 1999, 121, 1145-1155.
  10. Mi Li, Garrett M. Morris, Taekyu Lee, Gary S. Laco, Chi-Huey Wong, Arthur J. Olson, John H. Elder, Alexander Wlodawer, Alla Gustchina  “Structural Studies of FIV and HIV-1 Proteases Complexed with an Efficient Inhibitor of FIV Protease”  Proteins: Struct., Funct., Genet. 2000, 38, 29-40.
  11. Ying-Chuan Lin, Zachary Beck, Taekyu Lee, Van-Duc Le, Garrett M. Morris, Arthur J. Olson, Chi-Huey Wong, John H. Elder  “Alteration of Substrate and Inhibitor Specificity of Feline Immumodeficiency Virus Protease”  J. Virol. 2000, 74, 4710-4720.
  12. Taekyu Lee*, Albert J. Robichaud, Kristopher E. Boyle, Yimin Lu, David W. Robertson, Keith J. Miller, Larry W. Fitzgerald, John F. McElroy, Brian L. Largent  “Novel, highly potent, selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics”  Bioorganic. Med. Chem. Lett. 2003, 13, 767-770
  13. Taekyu Lee, Chi-Huey Wong, John H. Elder  "HIV/FIV Protease Inhibitors Having a Small P3 Residue.”  PCT Int, Appl. (1999), WO 9929311 A1 19990617.
  14. Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Wenting Chen, Christopher D. McClung, Emilie J. B. Calvello, David M. Zawrontny  “Substituted Heterocycle Fused Gamma-Carbolines” US Patent (2003), US 6548493 B1 20030415
  15. Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael G. Yang, Simon Haydar, Wenting Chen, Christopher D. McClung, Emilie J. B. Calvello, David M. Zawrontny  “Substituted Heterocycle Fused Gamma-Carbolines” US Patent (2003), US 6552017 B1 20030422
  16. Albert J. Robichaud, Ian S. Mitchell, Taekyu Lee, Wenting Chen  “Substituted Pyrazinoquinoxaline Derivatives as Serotonin Receptor Agonist and Antagonists Ligands”  US Patent (2003), US 6638934 B2 20031028
  17. Albert J. Robichaud, John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola “Substituted Pyridoindoles as Serotonin Agonists and Antagonists”  US Patent (2004), US 6699852 B2 20040302
  18. Taekyu Lee, Wenting Chen, Wei Deng, Albert J. Robichaud, Ruth Wexler  “Preparation of substituted tricyclic gamma-carbolines as serotonin receptor agonists and antagonists.”  PCT Int. Appl. (2004), 256 pp.  WO 04056324 A2 20040708.
  19. Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Simon Haydar, Wenting Chen, Christopher D. McClung, Emilie K.B. Calvello, David M. Zawrotny  “Substituted heterocycle fused gamma-carbolines”  U.S. Patent (2004), US 6713471 B1 20040330
  20. John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola  “Substituted pyrroloquinolines and pyridoquinolines as serotonin agonists and antagonists.”  U.S. Patent (2005), US 6777406 B2 20050418
  21. Taekyu Lee, Wei Deng, Albert J. Robichaud   “Substituted hexahydro-pyridoindole derivatives as serotonin receptor agonists and antagonists.”  U.S. Pat. Appl. (2005), US 2005239768 A1 20051027
  22. Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael G. Yang, Simon Haydar, Wenting Chen, Christopher D. McClung, Emilie K.B. Calvello, David M. Zawrotny  “Substituted heterocycle fused gamma-carbolines”  U.S. Patent (2006), US 7071186 B2 20060704
  23. Chongqing Sun, Yanting Huang, Doree F. Sitkoff, Guixue Yu, Amarendra B. Mikkilineni, Taekyu Lee, William R. Ewing “Preparation of Bicyclic Heterocycles as Cannabinoid-1 Receptor Modulators”  U.S. Pat. Appl. Publ. (2006),  US  2006287324  A1  20061221
  24. Taekyu Lee  “Substituted Tetrahydro 1H-Pyrido[4,3,B]Indoles as Serotonin Receptor Agonists and Antagonists” U.S. Pat. Appl. Publ. (2007),  US  2007027178  A1  20070201
  25. Wenting Chen, Taekyu Lee  “Preparation of tetrahydroazafluorenes and hexahydroazafluorenones as serotonin receptors agonists and antagonists for treating metabolic, CNS, and gastrointestinal disorders.”  U.S. Pat. Appl. Publ. (2007),  2007049613  A1  20070301
  26. Chongqing Sun, Philip M. Sher, Gang Wu, William R. Ewing, Yanting Huang, Taekyu Lee, Natesan Murugesan, Richard B. Sulsky  “Preparation of triazolopyridine derivatives as cannabinoid receptor 1 antagonists.” U.S. Pat. Appl. Publ. (2009),  US 7572808 B2 20090811.