Kyle A. Emmitte, Ph.D.

Research Assistant Professor of Pharmacology,
Associate Director of Medicinal Chemistry for the Vanderbilt Center for Neuroscience Drug Discovery,
Co-Director, The Vanderbilt Specialized Chemistry Center for Accelerated Probe Development

    B.S.    Texas A&M University, 1996


    Ph.D.  University of North Carolina at Chapel Hill, 2001

              Organic Chemistry

Phone: (615) 936-8401
Fax: (615) 322-8577
Email: kyle.a.emmitte@vanderbilt.edu
Location: 12415 MRB IV (Langford)

Biosketch and Research Interests

Kyle A. Emmitte received his Ph.D. under the direction of Professor Michael T. Crimmins. His work focused on the development of an asymmetric alkylation–ring-closing metathesis strategy for the synthesis of medium ring ethers. This strategy was applied to the total synthesis of complex marine natural products. Kyle successfully completed the total synthesis of (+)-laurencin and (-)-isolaurallene during this time. He also initiated the work within the Crimmins laboratory directed toward the application of the asymmetric alkylation/aldol–ring-closing metathesis strategy to the ladder ether Brevetoxin A.

Kyle joined GlaxoSmithKline as a member of the Oncology Medicinal Chemistry Department in Research Triangle Park, North Carolina in 2002. He was involved in research directed toward the discovery of novel kinase inhibitors for cancer therapy. Kyle was a key driver on the polo-like kinase 1 team that discovered GSK461364, a molecule currently under evaluation in clinical trials. He was awarded the GSK Exceptional Science Award in recognition of his contribution to the polo-like kinase inhibitor program. Subsequent to that work, Kyle led the effort focused on the discovery of novel inhibitors of insulin-like growth factor-1 receptor.

In 2008, Kyle joined the Vanderbilt Center for Neuroscience Drug Discovery as Associate Director of Medicinal Chemistry. He is also a Research Assistant Professor in the Department of Pharmacology in the Vanderbilt University School of Medicine. His current research is focused on the discovery of novel small molecule therapeutics for the treatment of central nervous system disorders.

Selected Publications

Sabbatini, P.; Rowand, J. L.; Groy, A.; Korenchuk, S.; Liu, Q.; Leperi, D.; Atkins, C.; Dumble, M.; Yang, J.; Anderson, K.; Wilson, B. J.; Emmitte, K. A.; Rabindran, S. K.; Kumar, R. ‘Antitumor Activity of GSK1904529A, a Small Molecule Inhibitor of the IGF-1R Receptor Tyrosine Kinase’ Clin. Cancer Res. (2009), manuscript submitted for publication.

Emmitte, K. A.; Andrews, C. W.; Badiang, J. G.; Davis-Ward, R. G.; Dickson, H. D.; Drewry, D. H.; Emerson, H. K.; Hassler, D. F.; Knick, V. B.; Kuntz, K. W.; Lansing, T. J.; Linn, J. A.; Mook Jr., R. A.; Nailor, K. E.; Salovich, J. M.; Spehar, G. M.; Cheung, M. ‘Discovery of Thiophene Inhibitors of Polo-like Kinase’ Bioorg. Med. Chem. Lett. (2009), Vol. 19, 1018-1021.

Emmitte, K. A.; Wilson, B. J.; Baum, E. W.; Emerson, H. K.; Kuntz, K. W.; Nailor, K. E.; Salovich, J. M.; Smith, S. C.; Cheung, M.; Gerding, R. M.; Stevens, K. L.; Uehling, D. E.; Mook Jr., R. A.; Moorthy, G. S.; Dickerson, S. H.; Hassell, A. M.; Leesnitzer, M. A.; Shewchuk, L. M.; Groy, A.; Rowand, J. L.; Anderson, K.; Atkins, C. L.; Yang, J.; Sabbatini, P.; Kumar, R. ‘Discovery and Optimization of Imidazo[1,2-a]pyridine Inhibitors of Insulin-like Growth Factor-1 Receptor (IGF-1R)’ Bioorg. Med. Chem. Lett. (2009), Vol. 19, 1004-1008.

Crimmins, M. T.; Zuccarello, J. L.; Ellis, J. M.; McDougall, P. J.; Haile, P. A.; Parrish, J. D.; Emmitte, K. A. ‘Total Synthesis of Brevetoxin A’ Org. Lett. (2009), Vol. 11, 489-492.

Hornberger, K. H.; Badiang, J. G.; Salovich, J. M.; Kuntz, K. W.; Emmitte, K. A.; Cheung, M. ‘Regioselective Synthesis of Benzimidazole Thiophene Inhibitors of Polo-like Kinase 1’ Tetrahedron Lett. (2008), Vol. 49, 6348-6351.

Lansing, T. J.; McConnell, R. T.; Duckett, D. R.; Spehar, G. M.; Knick, V. B.; Hassler, D. F.; Noro, N.; Furuta, M.; Emmitte, K. A.; Gilmer, T. M.; Mook, Jr., R. A.; Cheung, M. ‘In vitro Biological Activity of a Novel Small-molecule Inhibitor of Polo-like Kinase 1’ Mol. Cancer Ther. (2007), Vol. 6, 450-459.

Crimmins, M. T.; McDougall, P. J.; Emmitte, K. A. ‘Strategy for the Formation of Polycyclic Ethers: Stereoselective Synthesis of the BCDE Fragment of Brevetoxin A’ Org. Lett. (2005), Vol. 7, 4033-4036.

Crimmins, M. T.; Diaz, C. J.; Emmitte, K. A. ‘A Unified Approach to the Enantioselective Synthesis of 2,6-cis- and trans-Disubstituted Tetrahydropyranones’ Heterocycles (2004), Vol. 62, 179-183.

Crimmins, M. T.; Emmitte, K. A.; Choy, A. L. ‘Ring Closing Metathesis for the Formation of Medium Ring Ethers: The Total Synthesis of (-)-Isolaurallene’ Tetrahedron (2002), Vol. 58, 1817-1834.

Crimmins, M. T.; Emmitte, K. A. ‘Asymmetric Total Synthesis of (-)-Isolaurallene’ J. Am. Chem. Soc. (2001), Vol. 123, 1533-1534.

Crimmins, M. T.; Emmitte, K. A. ‘An Efficient Strategy for the Synthesis of alpha, alpha'-cis and trans-Disubstituted Medium Ring Ethers’ Synthesis (2000), 899-903.

Crimmins, M. T.; Emmitte, K. A.; Katz, J. D. ‘Diastereoselective Alkylations of Oxazolidinone Glycolates: A Useful Extension of the Evans Asymmetric Alkylation’ Org. Lett. (2000), Vol. 2, 2165-2167.

Crimmins, M. T.; Emmitte, K. A. ‘Total Synthesis of (+)-Laurencin: An Asymmetric Alkylation-Ring-Closing Metathesis Approach to Medium Ring Ethers’ Org. Lett. (1999), Vol. 1, 2029-2032.

Kyle sitting...er...working

Curriculum Vita

Mailing Address:
Vanderbilt University Medical Center

Department of Pharmacology

1205 Light Hall
Nashville, TN 37232-0697