James W. Janetka Research Assistant Professor Dept. of Biochemistry and Molecular Biophysics

Research

The Janetka group is working on the discovery, design, and chemical synthesis of small-molecule inhibitors of therapeutically relevant protein targets important in cancer and infectious disease. In addition to several collaborative projects including the development of FimH adhesion antagonists for the treatment of urinary tract infections and inhibitors of the ERCC1/XPA protein-protein interaction (PPI) important in DNA-damage repair, the group is interested in developing novel antagonists of the c-Met/HGF pathway important in oncology.

Selected Publications

• Aronov, A.A., Tang, Q., Martinez-Botella,G., Bemis, G.W., Cao, J., Chen, G., Ewing, N.P., Ford, P.J., Germann, U.A., Green, J., Hale, M.R., Jacobs, M., Janetka, J.W., Maltais, F., Markland, W., Namchuk M.N., Nanthakumar, S., Poondru, S., Straub, J., ter Haar, E. and Xie, X. Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control. J Medicinal Chemistry 52:6362-6368 (2009).

• Janetka, J.W. and Ashwell, S. Checkpoint kinase inhibitors: A review of the patent literature. Expert Opinion on Therapeutic Patents 19:165-197 (2009).

• Zabludoff, S.D., Deng C., Grondine, M.R., Sheehy, A.M., Ashwell, S., Cale, B.L., Green, S., Haye, H.R., Horn, C.L., Janetka, J.W., Liu, D., Mouchet, E., Ready, S., Rosenthal, J.L., Queva, C., Schwartz, G.K., Taylor, K.J., Tse, A.N., Walker, G.E., and White, A.M. AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies. Molecular Cancer Therapeutics 7:2955-2966 (2008).

• Ashwell, S., Janetka, J.W. and Zabludoff, S. Keeping checkpoint kinases in line: New selective inhibitors in clinical trials. Expert Opin Investig Drugs 17:1331-1340 (2008).

• Janetka, J.W., Almeida, L., Ashwella, S., Brassil, P.J., Daly, K., Deng C., Gero, T., Glynn, R.E., Horn, C.L., Ioannidis, S., Lyne, P., Newcombe, N.J., Oza, V.B., Pass, M., Springer, S.K., Su, M., Toader, D., Vasbinder, M.M., Yu, D., Yu, Y. and Zabludoff, S.D. Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors. Bioorganic & Medicinal Chemistry Letters 18:4242-4248 (2008).