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Page 1
Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C.
Weiss A, Lorthiois E, Barys L, Beyer KS, Bomio-Confaglia C, Burks H, Chen X, Cui X, de Kanter R, Dharmarajan L, Fedele C, Gerspacher M, Guthy DA, Head V, Jaeger A, Núñez EJ, Kearns JD, Leblanc C, Maira SM, Murphy J, Oakman H, Ostermann N, Ottl J, Rigollier P, Roman D, Schnell C, Sedrani R, Shimizu T, Stringer R, Vaupel A, Voshol H, Wessels P, Widmer T, Wilcken R, Xu K, Zecri F, Farago AF, Cotesta S, Brachmann SM. Weiss A, et al. Among authors: voshol h. Cancer Discov. 2022 Jun 2;12(6):1500-1517. doi: 10.1158/2159-8290.CD-22-0158. Cancer Discov. 2022. PMID: 35404998 Free PMC article.
Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent.
Andraos R, Qian Z, Bonenfant D, Rubert J, Vangrevelinghe E, Scheufler C, Marque F, Régnier CH, De Pover A, Ryckelynck H, Bhagwat N, Koppikar P, Goel A, Wyder L, Tavares G, Baffert F, Pissot-Soldermann C, Manley PW, Gaul C, Voshol H, Levine RL, Sellers WR, Hofmann F, Radimerski T. Andraos R, et al. Among authors: voshol h. Cancer Discov. 2012 Jun;2(6):512-523. doi: 10.1158/2159-8290.CD-11-0324. Epub 2012 May 3. Cancer Discov. 2012. PMID: 22684457 Free PMC article.
Maximizing the Efficacy of MAPK-Targeted Treatment in PTENLOF/BRAFMUT Melanoma through PI3K and IGF1R Inhibition.
Herkert B, Kauffmann A, Mollé S, Schnell C, Ferrat T, Voshol H, Juengert J, Erasimus H, Marszalek G, Kazic-Legueux M, Billy E, Ruddy D, Stump M, Guthy D, Ristov M, Calkins K, Maira SM, Sellers WR, Hofmann F, Hall MN, Brachmann SM. Herkert B, et al. Among authors: voshol h. Cancer Res. 2016 Jan 15;76(2):390-402. doi: 10.1158/0008-5472.CAN-14-3358. Epub 2015 Nov 17. Cancer Res. 2016. PMID: 26577700
JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors.
Lorthiois E, Gerspacher M, Beyer KS, Vaupel A, Leblanc C, Stringer R, Weiss A, Wilcken R, Guthy DA, Lingel A, Bomio-Confaglia C, Machauer R, Rigollier P, Ottl J, Arz D, Bernet P, Desjonqueres G, Dussauge S, Kazic-Legueux M, Lozac'h MA, Mura C, Sorge M, Todorov M, Warin N, Zink F, Voshol H, Zecri FJ, Sedrani RC, Ostermann N, Brachmann SM, Cotesta S. Lorthiois E, et al. Among authors: voshol h. J Med Chem. 2022 Dec 22;65(24):16173-16203. doi: 10.1021/acs.jmedchem.2c01438. Epub 2022 Nov 18. J Med Chem. 2022. PMID: 36399068
CRISPR Screening Identifies Mechanisms of Resistance to KRASG12C and SHP2 Inhibitor Combinations in Non-Small Cell Lung Cancer.
Prahallad A, Weiss A, Voshol H, Kerr G, Sprouffske K, Yuan T, Ruddy D, Meistertzheim M, Kazic-Legueux M, Kottarathil T, Piquet M, Cao Y, Martinuzzi-Duboc L, Buhles A, Adler F, Mannino S, Tordella L, Sansregret L, Maira SM, Graus Porta D, Fedele C, Brachmann SM. Prahallad A, et al. Among authors: voshol h. Cancer Res. 2023 Dec 15;83(24):4130-4141. doi: 10.1158/0008-5472.CAN-23-1127. Cancer Res. 2023. PMID: 37934115 Free PMC article.
Discovery of WRN inhibitor HRO761 with synthetic lethality in MSI cancers.
Ferretti S, Hamon J, de Kanter R, Scheufler C, Andraos-Rey R, Barbe S, Bechter E, Blank J, Bordas V, Dammassa E, Decker A, Di Nanni N, Dourdoigne M, Gavioli E, Hattenberger M, Heuser A, Hemmerlin C, Hinrichs J, Kerr G, Laborde L, Jaco I, Núñez EJ, Martus HJ, Quadt C, Reschke M, Romanet V, Schaeffer F, Schoepfer J, Schrapp M, Strang R, Voshol H, Wartmann M, Welly S, Zécri F, Hofmann F, Möbitz H, Cortés-Cros M. Ferretti S, et al. Among authors: voshol h. Nature. 2024 May;629(8011):443-449. doi: 10.1038/s41586-024-07350-y. Epub 2024 Apr 24. Nature. 2024. PMID: 38658754 Free PMC article.
The tyrosine phosphatase PTPN14 is a negative regulator of YAP activity.
Michaloglou C, Lehmann W, Martin T, Delaunay C, Hueber A, Barys L, Niu H, Billy E, Wartmann M, Ito M, Wilson CJ, Digan ME, Bauer A, Voshol H, Christofori G, Sellers WR, Hofmann F, Schmelzle T. Michaloglou C, et al. Among authors: voshol h. PLoS One. 2013 Apr 16;8(4):e61916. doi: 10.1371/journal.pone.0061916. Print 2013. PLoS One. 2013. PMID: 23613971 Free PMC article.
52 results