Waterson, Alex G.

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

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Small-molecule inhibition of Wnt signaling through activation of casein kinase 1α

Thorne, C. A., Hanson, A. J., Schneider, J., Tahinci, E., Orton, D., Cselenyi, C. S., Jernigan, K. K., Meyers, K. C., Hang, B. I., Waterson, A. G., et al. (2010) · Nature Chemical Biology

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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

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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

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Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS G12C Inhibitor

Bröker, J., Waterson, A. G., Smethurst, C., Kessler, D., Böttcher, J., Mayer, M., Gmaschitz, G., Phan, J., Little, A., Abbott, J. R., et al. (2022) · Journal of Medicinal Chemistry

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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

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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

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Abstract 1271: In vitro and in vivo characterization of BI 1823911 - a novel KRASG12C selective small molecule inhibitor

Savarese, F., Gollner, A., Rudolph, D., Lipp, J., Popow, J., Hofmann, M. H., Arnhof, H., Rinnenthal, J., Trapani, F., Gmachl, M., et al. (2021) · Cancer Research

Protein Kinase Regulation and GTPase SignalingLung Cancer Treatments and Mutations

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