Gmachl, Michael

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

BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition

Hofmann, M. H., Gmachl, M., Ramharter, J., Savarese, F., Gerlach, D., Marszalek, J. R., Sanderson, M. P., Kessler, D., Trapani, F., Arnhof, H., et al. (2021) · Cancer Discovery

Protein Kinase Regulation and GTPase SignalingMelanoma and MAPK Pathways

Cited by 444

KRAS Secondary Mutations That Confer Acquired Resistance to KRAS G12C Inhibitors, Sotorasib and Adagrasib, and Overcoming Strategies: Insights From In Vitro Experiments

Koga, T., Suda, K., Fujino, T., Ohara, S., Hamada, A., Nishino, M., Chiba, M., Shimoji, M., Takemoto, T., Arita, T., et al. (2021) · Journal of Thoracic Oncology

Lung Cancer Treatments and MutationsProtein Kinase Regulation and GTPase Signaling

Cited by 265

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

Protein Kinase Regulation and GTPase SignalingProtein Tyrosine Phosphatases

Cited by 96

Co-targeting SOS1 enhances the antitumor effects of KRASG12C inhibitors by addressing intrinsic and acquired resistance

Thatikonda, V., Lyu, H., Jurado, S., Kostyrko, K., Bristow, C. A., Albrecht, C., Alpar, D., Arnhof, H., Bergner, O., Bosch, K., et al. (2024) · Nature Cancer

Protein Kinase Regulation and GTPase SignalingMelanoma and MAPK Pathways

Cited by 76

Abstract 1091: BI-3406 and BI 1701963: Potent and selective SOS1::KRAS inhibitors induce regressions in combination with MEK inhibitors or irinotecan

Gerlach, D., Gmachl, M., Ramharter, J., Teh, J., Fu, S.-C., Trapani, F., Kessler, D., Rumpel, K., Botesteanu, D.-A., Ettmayer, P., et al. (2020) · Cancer Research

Protein Kinase Regulation and GTPase SignalingMelanoma and MAPK Pathways

Cited by 53

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

Cited by 25

Abstract CT210: Trial in Process: Phase 1 studies of BI 1701963, a SOS1::KRAS Inhibitor, in combination with MEK inhibitors, irreversible KRASG12C inhibitors or irinotecan.

Hofmann, M. H., Lu, H., Duenzinger, U., Gerlach, D., Trapani, F., Machado, A. A., Daniele, J. R., Waizenegger, I., Gmachl, M., Rudolph, D., et al. (2021) · Cancer Research

Protein Kinase Regulation and GTPase SignalingMelanoma and MAPK Pathways

Cited by 20