Publications

Found 11 results
Filters: Author is Heppner, David E  [Clear All Filters]
A B C D E F G H I J K L M N O P Q R S T U V W X Y Z 
A
To, C., Beyett, T. S., Jang, J., Feng, W. W., Bahcall, M., Haikala, H. M., Shin, B. H., Heppner, D. E., Rana, J. K., Leeper, B. A., Soroko, K. M., Poitras, M. J., Gokhale, P. C., Kobayashi, Y., Wahid, K., Kurppa, K. J., Gero, T. W., Cameron, M. D., Ogino, A., Mushajiang, M., Xu, C., Zhang, Y., Scott, D. A., Eck, M. J., Gray, N. S., and Jänne, P. A. (2022) An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer. Nat Cancer. 3, 402-417
D
Wittlinger, F., Heppner, D. E., To, C., Günther, M., Shin, B. Hee, Rana, J. K., Schmoker, A. M., Beyett, T. S., Berger, L. M., Berger, B. - T., Bauer, N., Vasta, J. D., Corona, C. R., Robers, M. B., Knapp, S., Jänne, P. A., Eck, M. J., and Laufer, S. A. (2021) Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. J Med Chem. 10.1021/acs.jmedchem.1c00848
De Clercq, D. J. H., Heppner, D. E., To, C., Jang, J., Park, E., Yun, C. -hong, Mushajiang, M., Shin, B. Hee, Gero, T. W., Scott, D. A., Jänne, P. A., Eck, M. J., and Gray, N. S. (2019) Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors. ACS Med Chem Lett. 10, 1549-1553
I
Bhattacharjee, D., Bakar, J., Chitnis, S. P., Sausville, E. L., Ashtekar, K. Dilip, Mendelson, B. E., Long, K., Smith, J. C., Heppner, D. E., and Sheltzer, J. M. (2023) Inhibition of a lower potency target drives the anticancer activity of a clinical p38 inhibitor. Cell Chem Biol. 30, 1211-1222.e5
L
Wittlinger, F., Ogboo, B. C., Shevchenko, E., Damghani, T., Pham, C. D., Schaeffner, I. K., Oligny, B. T., Chitnis, S. P., Beyett, T. S., Rasch, A., Buckley, B., Urul, D. A., Shaurova, T., May, E. W., Schaefer, E. M., Eck, M. J., Hershberger, P. A., Poso, A., Laufer, S. A., and Heppner, D. E. (2024) Linking ATP and allosteric sites to achieve superadditive binding with bivalent EGFR kinase inhibitors. Commun Chem. 7, 38
M
Beyett, T. S., To, C., Heppner, D. E., Rana, J. K., Schmoker, A. M., Jang, J., De Clercq, D. J. H., Gomez, G., Scott, D. A., Gray, N. S., Jänne, P. A., and Eck, M. J. (2022) Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors. Nat Commun. 13, 2530
Q
Gero, T. W., Heppner, D. E., Beyett, T. S., To, C., Azevedo, S. C., Jang, J., Bunnell, T., Feru, F., Li, Z., Shin, B. Hee, Soroko, K. M., Gokhale, P. C., Gray, N. S., Jänne, P. A., Eck, M. J., and Scott, D. A. (2022) Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC. Bioorg Med Chem Lett. 10.1016/j.bmcl.2022.128718
S
To, C., Jang, J., Chen, T., Park, E., Mushajiang, M., De Clercq, D. J. H., Xu, M., Wang, S., Cameron, M. D., Heppner, D. E., Shin, B. Hee, Gero, T. W., Yang, A., Dahlberg, S. E., Wong, K. - K., Eck, M. J., Gray, N. S., and Jänne, P. A. (2019) Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. Cancer Discov. 9, 926-943
Beyett, T. S., Rana, J. K., Schaeffner, I. K., Heppner, D. E., and Eck, M. J. (2024) Structural Analysis of the Macrocyclic Inhibitor BI-4020 Binding to EGFR Kinase. ChemMedChem. 19, e202300343
Heppner, D. E., Günther, M., Wittlinger, F., Laufer, S. A., and Eck, M. J. (2020) Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors. J Med Chem. 10.1021/acs.jmedchem.0c00200
Heppner, D. E., Wittlinger, F., Beyett, T. S., Shaurova, T., Urul, D. A., Buckley, B., Pham, C. D., Schaeffner, I. K., Yang, B., Ogboo, B. C., May, E. W., Schaefer, E. M., Eck, M. J., Laufer, S. A., and Hershberger, P. A. (2022) Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). ACS Med Chem Lett. 13, 1856-1863