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BI-3406, a Potent and Selective SOS1-KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition.
Hofmann MH, Gmachl M, Ramharter J, Savarese F, Gerlach D, Marszalek JR, Sanderson MP, Kessler D, Trapani F, Arnhof H, Rumpel K, Botesteanu DA, Ettmayer P, Gerstberger T, Kofink C, Wunberg T, Zoephel A, Fu SC, Teh JL, Böttcher J, Pototschnig N, Schachinger F, Schipany K, Lieb S, Vellano CP, O'Connell JC, Mendes RL, Moll J, Petronczki M, Heffernan TP, Pearson M, McConnell DB, Kraut N. Hofmann MH, et al. Among authors: gerlach d. Cancer Discov. 2021 Jan;11(1):142-157. doi: 10.1158/2159-8290.CD-20-0142. Epub 2020 Aug 19. Cancer Discov. 2021. PMID: 32816843 Free PMC article.
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 CA, Albrecht C, Alpar D, Arnhof H, Bergner O, Bosch K, Feng N, Gao S, Gerlach D, Gmachl M, Hinkel M, Lieb S, Jeschko A, Machado AA, Madensky T, Marszalek ED, Mahendra M, Melo-Zainzinger G, Molkentine JM, Jaeger PA, Peng DH, Schenk RL, Sorokin A, Strauss S, Trapani F, Kopetz S, Vellano CP, Petronczki M, Kraut N, Heffernan TP, Marszalek JR, Pearson M, Waizenegger IC, Hofmann MH. Thatikonda V, et al. Among authors: gerlach d. Nat Cancer. 2024 Sep;5(9):1352-1370. doi: 10.1038/s43018-024-00800-6. Epub 2024 Aug 5. Nat Cancer. 2024. PMID: 39103541 Free PMC article.
Pan-KRAS inhibitors BI-2493 and BI-2865 display potent anti-tumor activity in tumors with KRAS wild-type allele amplification.
Tedeschi A, Schischlik F, Rocchetti F, Popow J, Ebner F, Gerlach D, Geyer A, Santoro V, Boghossian AS, Rees MG, Ronan MM, Roth JA, Lipp J, Samwer M, Gmachl M, Kraut N, Pearson M, Rudolph D. Tedeschi A, et al. Among authors: gerlach d. Mol Cancer Ther. 2024 Dec 23. doi: 10.1158/1535-7163.MCT-24-0386. Online ahead of print. Mol Cancer Ther. 2024. PMID: 39711431
Discovery of potent and selective HER2 inhibitors with efficacy against HER2 exon 20 insertion-driven tumors, which preserve wild-type EGFR signaling.
Wilding B, Scharn D, Böse D, Baum A, Santoro V, Chetta P, Schnitzer R, Botesteanu DA, Reiser C, Kornigg S, Knesl P, Hörmann A, Köferle A, Corcokovic M, Lieb S, Scholz G, Bruchhaus J, Spina M, Balla J, Peric-Simov B, Zimmer J, Mitzner S, Fett TN, Beran A, Lamarre L, Gerstberger T, Gerlach D, Bauer M, Bergner A, Schlattl A, Bader G, Treu M, Engelhardt H, Zahn S, Fuchs JE, Zuber J, Ettmayer P, Pearson M, Petronczki M, Kraut N, McConnell DB, Solca F, Neumüller RA. Wilding B, et al. Among authors: gerlach d. Nat Cancer. 2022 Jul;3(7):821-836. doi: 10.1038/s43018-022-00412-y. Epub 2022 Jul 26. Nat Cancer. 2022. PMID: 35883003
Zongertinib (BI 1810631), an Irreversible HER2 TKI, Spares EGFR Signaling and Improves Therapeutic Response in Preclinical Models and Patients with HER2-Driven Cancers.
Wilding B, Woelflingseder L, Baum A, Chylinski K, Vainorius G, Gibson N, Waizenegger IC, Gerlach D, Augsten M, Spreitzer F, Shirai Y, Ikegami M, Tilandyová S, Scharn D, Pearson MA, Popow J, Obenauf AC, Yamamoto N, Kondo S, Opdam FL, Bruining A, Kohsaka S, Kraut N, Heymach JV, Solca F, Neumüller RA. Wilding B, et al. Among authors: gerlach d. Cancer Discov. 2025 Jan 13;15(1):119-138. doi: 10.1158/2159-8290.CD-24-0306. Cancer Discov. 2025. PMID: 39248702 Free PMC article.
Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2-p53 Antagonist Suitable for Intermittent Dose Schedules.
Gollner A, Rudolph D, Weyer-Czernilofsky U, Baumgartinger R, Jung P, Weinstabl H, Ramharter J, Grempler R, Quant J, Rinnenthal J, Pérez Pitarch A, Golubovic B, Gerlach D, Bader G, Wetzel K, Otto S, Mandl C, Boehmelt G, McConnell DB, Kraut N, Sini P. Gollner A, et al. Among authors: gerlach d. Mol Cancer Ther. 2024 Dec 3;23(12):1689-1702. doi: 10.1158/1535-7163.MCT-23-0783. Mol Cancer Ther. 2024. PMID: 39259562 Free PMC article. Clinical Trial.
254 results