研究领域
Center for Structural Biology
Chemical Biology
Biophysical Chemistry
Biochemistry
The focus of our lab is on cancer drug discovery using fragment-based approaches and structure-based design. To accomplish this goal, we have assembled a multidisciplinary team that includes structural biologists, medicinal chemists, and cell biologists. In our lab, we clone, express, and purify proteins, conduct fragment-based screens, determine the three-dimensional structures of protein/ligand complexes using NMR and/or X-ray crystallography, design and synthesize compounds, and test compounds in primary and secondary biological assays. The cancer drug targets that we are pursuing are highly validated but technically challenging such as K-Ras and c-Myc.
近期论文
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Frank, A.O., Vangamudi, B., Feldkamp, M.D., Souza-Fagundes, E.M., Luzwick, J.W., Cortez, D., Olejniczak, E.T., Waterson, A.G., Rossanese, O.W., Chazin, W.J., Fesik, S.W. Discovery of a Potent Stapled Helix Peptide That Binds to the 70N Domain of Replication Protein A. Journal of Medicinal Chemistry. 2014, 0 (0): [Epub ahead of print].
Burns, M.C., Sun, Q., Daniels, R.N., Camper, D., Kennedy, J.P., Phan, J., Olejniczak, E.T., Lee, T., Waterson, A.G., Rossanese, O.W., Fesik, S.W. Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange. Proceedings of the National Academy of Sciences. 2014, 111 (9): 3401-6.
Friberg, A., Vigil, D., Zhao, B., Daniels, R.N., Burke, J.P., Garcia-Barrantes, P.M., Camper, D., Chauder, B.A., Lee, T., Olejniczak, E.T., Fesik, S.W. Discovery of Potent Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods and Structure-Based Design. Journal of Medicinal Chemistry. 2013, 56 (1): 15-30.
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.
Souza-Fagundes, E.M., Frank, A.O., Feldkamp, M.D., Dorset, D.C., Chazin, W.J., Rossanese, O.W., Olejniczak, E.T., Fesik, S.W. A high-throughput fluorescence polarization anisotropy assay for the 70N domain of replication protein A. Analytical Biochemistry. 2012, 421 (2): 742-749.
Ackler, S. Mitten, M.J. Foster, K. Oleksijew, A. Refici, M. Tahir, S.K., Xiao, Y. Tse, C. Frost, D.J. Fesik, S.W. Rosenberg S.H., Elmore S.W., Shoemaker A.R. The Bcl-2 inhibitor ABT-263 enhances the response of multiple chemotherapeutic regimens in hematologic tumors in vivo. Cancer Chemotherapy and Pharmacology. 2010, 66 (5): 869-880.
Lin, X., C.A. David, J.B. Donnelly, M. Michaelides, N.S. Chandel, X. Huang, U. Warrior, F. Weinberg, K.V. Tormos, S.W. Fesik and Y. Shen. A chemical genomics screen highlights the essential role of mitochondria in HIF-1 regulation. Proc. Nat’l Acad. Sci. USA. 105, 174-179 2008.
Tse, C., A.R. Shoemaker, J. Adickes, M.G. Anderson, J. Chen, S. Jin, E.F. Johnson, K.C. Marsh, M.J. Mitten, P. Nimmer, L. Roberts, S.K. Tahir, Y. Xiao, X. Yang, H. Zhang, S. Fesik, S.H. Rosenberg, and S.W. Elmore. ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor. Cancer Res. 68, 3421-3428 2008.
Shoemaker, A.R., M.J. Mitten, J. Adickes, S. Ackler, M. Refici, D. Ferguson, A. Oleksijew, J.M. O’Connor, B. Wang, D.J. Frost, J. Bauch, K. Marsh, S.K. Tahir, X. Yang, C. Tse, S. W. Fesik, S.H. Rosenberg and S.W. Elmore. Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models. Clinical Cancer Research 14, 3268-3277 2008.
Ackler S, Xiao Y, Mitten MJ, Foster K, Oleksijew A, Refici M, Schlessinger S, Wang B, Chemburkar SR, Bauch J, Tse C, Frost DJ, Fesik SW, Rosenberg SH, Elmore SW, Shoemaker AR. ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo. Molecular Cancer Ther. 10, 3265-74 2008.
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