Fesik, Stephen W.

Drugging the undruggable RAS: Mission Possible?

Cox, A. D., Fesik, S. W., Kimmelman, A. C., Luo, J., & Der, C. J. (2014) · Nature Reviews Drug Discovery

Protein Kinase Regulation and GTPase SignalingProtein Tyrosine Phosphatases

Cited by 1,997

ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor

Tse, C., Shoemaker, A. R., Adickes, J., Anderson, M. G., Chen, J., Jin, S., Johnson, E. F., Marsh, K. C., Mitten, M. J., Nimmer, P., et al. (2008) · Cancer Research

Cell death mechanisms and regulationCancer-related Molecular Pathways

Cited by 1,992

Structure of Bcl-x L -Bak Peptide Complex: Recognition Between Regulators of Apoptosis

Sattler, M., Liang, H., Nettesheim, D., Meadows, R. P., Harlan, J. E., Eberstadt, M., Yoon, H. S., Shuker, S. B., Chang, B. S., Minn, A. J., et al. (1997) · Science

Cell death mechanisms and regulationProtein Structure and Dynamics

Cited by 1,476

Twenty years on: the impact of fragments on drug discovery

Erlanson, D. A., Fesik, S. W., Hubbard, R. E., Jahnke, W., & Jhoti, H. (2016) · Nature Reviews Drug Discovery

Computational Drug Discovery MethodsChemical Synthesis and Analysis

Cited by 1,000

Structural biology of the Bcl-2 family of proteins

Petros, A. M., Olejniczak, E. T., & Fesik, S. W. (2004) · Biochimica et Biophysica Acta (BBA) - Molecular Cell Research

Cell death mechanisms and regulationEnzyme Structure and Function

Cited by 745

Discovery of Small Molecules that Bind to K‐Ras and Inhibit Sos‐Mediated Activation

Sun, Q., Burke, J. P., Phan, J., Burns, M. C., Olejniczak, E. T., Waterson, A. G., Lee, T., Rossanese, O. W., & Fesik, S. W. (2012) · Angewandte Chemie International Edition

Protein Kinase Regulation and GTPase SignalingComputational Drug Discovery Methods

Cited by 490

Drugging an undruggable pocket on KRAS

Kessler, D., Gmachl, M., Mantoulidis, A., Martin, L. J., Zoephel, A., Mayer, M., Gollner, A., Covini, D., Fischer, S., Gerstberger, T., et al. (2019) · Proceedings of the National Academy of Sciences

Protein Kinase Regulation and GTPase SignalingProtein Tyrosine Phosphatases

Cited by 449

Interaction with WDR5 Promotes Target Gene Recognition and Tumorigenesis by MYC

Thomas, L. R., Wang, Q., Grieb, B. C., Phan, J., Foshage, A. M., Sun, Q., Olejniczak, E. T., Clark, T., Dey, S., Lorey, S., et al. (2015) · Molecular Cell

Genomics and Chromatin DynamicsChromatin Remodeling and Cancer

Cited by 310

Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange

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., et al. (2014) · Proceedings of the National Academy of Sciences

Protein Kinase Regulation and GTPase SignalingProtein Tyrosine Phosphatases

Cited by 199

Solution structure of the ets domain of Fli-1 when bound to DNA

Liang, H., Mao, X., Olejniczak, E. T., Nettesheim, D. G., Yu, L., Meadows, R. P., Thompson, C. B., & Fesik, S. W. (1994) · Nature Structural & Molecular Biology

Protein Structure and DynamicsGenomics and Chromatin Dynamics

Cited by 104

Discovery of WD Repeat-Containing Protein 5 (WDR5)–MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design

Chacón Simon, S., Wang, F., Thomas, L. R., Phan, J., Zhao, B., Olejniczak, E. T., Macdonald, J. D., Shaw, J. G., Schlund, C., Payne, W., et al. (2020) · Journal of Medicinal Chemistry

Computational Drug Discovery MethodsProtein Degradation and Inhibitors

Cited by 76

Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5–MYC Protein–Protein Interaction

Macdonald, J. D., Chacón Simon, S., Han, C., Wang, F., Shaw, J. G., Howes, J. E., Sai, J., Yuh, J. P., Camper, D., Alicie, B. M., et al. (2019) · Journal of Medicinal Chemistry

Computational Drug Discovery MethodsHeterocyclic Compound Synthesis and Bioactivity

Cited by 66