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Alex G. Waterson

Title and Contact Information

Research Assistant Professor of Pharmacology & Chemistry
Office: 802C RRB
Phone: (615) 322-9971
Email

Education

Ph.D., Emory University, 1999

Specialties

VICB
Synethic Organic Chemistry
Organic Chemistry
Medicinal Chemistry
Chemical Biology

In the News

VICC-VU Joins Effort To Develop New Cancer Therapies

Waterson

Research

Alex G. Waterson, Ph.D. is a Research Assistant Professor of Pharmacology and Chemistry and a medicinal chemist in the Fesik lab for cancer drug discovery. He is interested in the application of synthetic and medicinal chemistry to questions of biological interest. He joined Vanderbilt in 2008 as the Director of the Vanderbilt Institute of Chemical Biology Chemical Synthesis Core and subsequently joined the group of Professor Stephen Fesik the following year. Alex is involved in a number of medicinal chemistry projects at Vanderbilt, including the fragment-based drug discovery efforts in the Fesik lab, a project to discover inhibitors of the T790M drug resistant mutant of the Epidermal Growth Factor Receptor, and two discovery efforts within Vanderbilt's GI SPORE that are aimed at discovering novel treatments of colon cancer.

Alex earned his Ph.D. in Chemistry in 1999 at Emory University in Atlanta, Georgia under the direction of Professor Albert Padwa and completed his formal training as a postdoctoral research fellow at Colorado State University in the group of the late Professor Albert I. Meyers. In 2001, Alex joined the medicinal chemistry department at GlaxoSmithKline in the Research Triangle Park area of North Carolina, where he contributed to the development of a new series of (unexpectedly) covalent modifying inhibitors of the ErbB family of kinases for the treatment of breast cancers and discovered a novel chemical series that led to a bRaf kinase drug candidate. This molecule is currently being evaluated in Phase III clinical trials for melanoma. Along with managing a triple inhibitor kinase backup project and a target validation stage program, he also became active in an oncology-based new target initiative and was involved in the proposal and initiation of kinase and non-kinase targets important at the intersection of inflammation and oncology signaling pathways and in the Wnt pathway. Alex received numerous awards and recognitions for his work at GlaxoSmithKline, including thirteen GSK R&D awards and an Exceptional Science Award. Along the way, Alex developed a significant expertise in the evaluation of the physical properties of inhibitors and the use of calculated properties to drive molecular design.

Alex is a member of the American Chemical Society and the American Association of Cancer Research and serves on the Scientific Advisory Board of Cumberland Emerging Technologies. He also serves as a reviewer for the Journal of Organic Chemistry and BioOrganic and Medicinal Chemistry Letters. Within Vanderbilt, Alex is a member of the VICB operating committee and Co-Principal Investigator of the Vanderbilt Chemical Diversity Center, an entry in the National Cancer Institute's Chemical Biology Consortium.

Selected Publications

Taylor, R. W.; Romaine, I. M.; Liu, C.; Murthi, P.; Jones, P. L.; Waterson, A. G.; Sulikowski, G. A.; Zwiebel, L. J. Structure-Activity Relationship of a Broad-Spectrum Insect Odorant Receptor Agonist. ACS Chemical Biology. 2012, 7 (10): 1647-1652.

Sun, Q.; Burke, J. P.; Phan, J.; Burns, M. C .; Olejniczak, E. T.; Waterson, A. G.; Lee, T.; Rossanese, O. W.; Fesik, S. W. Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation. Angewandte Chemie-International Edition. 2012, 51 (25): 6140-6143.

Stoops, S. L.; Pearson, A. S.; Weaver, C.; Waterson, A. G.; Days, E.; Farmer, C.; Brady, S.; Weaver, C. D.; Beauchamp, R. D.; Lindsley, C. W. Identification and Optimization of Small Molecules That Restore E-Cadherin Expression and Reduce Invasion in Colorectal Carcinoma Cells. ACS Chemical Biology. 2011, 6 (5): 452-465.

Thorne, C. A.; Schneider, J.; Tahinci, E.; Orton, D.; Cselenyi, C. S.; Jernigan, K. K.; Hanson, A., J.; Meyers, K. C.; Hang, B. I.; Waterson; A. G.; LaFleur, B.; Salic, A.; Lee, L. A.; Miller, III, D. M.; Lee, E. Small-molecule inhibition of Wnt signaling through activation of Casein Kinase 1 alpha. Nature Chemical Biology. 2010, 6 (11): 829-836.

Adjabeng, G. M.; Bifulco, N.; Davis-Ward, R. G.; Dickerson, S. H.; Hornberger, K. H.; Petrov, K.; Rheault, T. R.; Uehling, D. E.; Waterson, A. G. Preparation of thiazole and oxazole kinase inhibitors for cancer treatment. Patent Applications. 2009: 301 WO2009076140 A1.

Adjabeng, G. M.; Bifulco, N.; Davis-Ward, R. G.; Dickerson, S. H.; Donaldson, K. H.; Petrov, K.; Rheault, T. R.; Schaaf,. G. M.; Stellwagen, J. C.; Uehling, D. E.; Waterson, A. G. Thiazole and oxazole kinase inhibitors. Patent Applications. 2009: 278 WO2009032667 A1.

Stevens, K. L; Alligood, K. J.; Alberti, J. G. B.; Caferro, T. R.; Chamberlain, S. D.; Dickerson, S. H.; Disckson, H. D.; Emerson, H. K.; Griffin, R. J.; Hubbard, R. D.; Keith, B. R.; Mullin, R. J.; Petrov, K. G.; Gerding, R. M.; Reno, M. J.; Rheault, T. R.; Rusnak, D. W.; Sammond, D. M.; Smith, S. C.; Uehling, D. E.; Waterson, A. G.; Wood, E. R. Synthesis and stereochemical effects of pyrrolidyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors. Bioorganic & Medicinal Chemistry Letters. 2009: 21-26.

Waterson, A. G.; Petrov,L. P.; Hornberger, K. R.; Hubbard, R. D.; Sammond, D. M.; Smith, S. C.; Hinkle, K. W.; Uehling, D. E.; Dickerson, S. H.; Rusnak, D. W.; Spehar, G. M.; Wood, E. R.; Griffin, R. J.; Kitrinos, N. P. Synthesis and evaluation of novel aniline headgroups for thienopyrimidine-based covalent dual EGFR/ErbB2 kinase inhibitors. Bioorganic & Medicinal Chemistry Letters. 2009, 19: 1332-1336.