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Getting a Grip on the Undrugged: Targeting β-Catenin with Fragment-Based Methods.
Kessler D, Mayer M, Zahn SK, Zeeb M, Wöhrle S, Bergner A, Bruchhaus J, Ciftci T, Dahmann G, Dettling M, Döbel S, Fuchs JE, Geist L, Hela W, Kofink C, Kousek R, Moser F, Puchner T, Rumpel K, Scharnweber M, Werni P, Wolkerstorfer B, Breitsprecher D, Baaske P, Pearson M, McConnell DB, Böttcher J. Kessler D, et al. Among authors: bottcher j. ChemMedChem. 2021 May 6;16(9):1420-1424. doi: 10.1002/cmdc.202000839. Epub 2021 Jan 14. ChemMedChem. 2021. PMID: 33275320 Free PMC article.
Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3.
Böttcher J, Dilworth D, Reiser U, Neumüller RA, Schleicher M, Petronczki M, Zeeb M, Mischerikow N, Allali-Hassani A, Szewczyk MM, Li F, Kennedy S, Vedadi M, Barsyte-Lovejoy D, Brown PJ, Huber KVM, Rogers CM, Wells CI, Fedorov O, Rumpel K, Zoephel A, Mayer M, Wunberg T, Böse D, Zahn S, Arnhof H, Berger H, Reiser C, Hörmann A, Krammer T, Corcokovic M, Sharps B, Winkler S, Häring D, Cockcroft XL, Fuchs JE, Müllauer B, Weiss-Puxbaum A, Gerstberger T, Boehmelt G, Vakoc CR, Arrowsmith CH, Pearson M, McConnell DB. Böttcher J, et al. Nat Chem Biol. 2019 Aug;15(8):822-829. doi: 10.1038/s41589-019-0310-x. Epub 2019 Jul 8. Nat Chem Biol. 2019. PMID: 31285596
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: bottcher j. 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.
One Atom Makes All the Difference: Getting a Foot in the Door between SOS1 and KRAS.
Ramharter J, Kessler D, Ettmayer P, Hofmann MH, Gerstberger T, Gmachl M, Wunberg T, Kofink C, Sanderson M, Arnhof H, Bader G, Rumpel K, Zöphel A, Schnitzer R, Böttcher J, O'Connell JC, Mendes RL, Richard D, Pototschnig N, Weiner I, Hela W, Hauer K, Haering D, Lamarre L, Wolkerstorfer B, Salamon C, Werni P, Munico-Martinez S, Meyer R, Kennedy MD, Kraut N, McConnell DB. Ramharter J, et al. Among authors: bottcher j. J Med Chem. 2021 May 27;64(10):6569-6580. doi: 10.1021/acs.jmedchem.0c01949. Epub 2021 Mar 15. J Med Chem. 2021. PMID: 33719426
Discovery of a Chemical Probe to Study Implications of BPTF Bromodomain Inhibition in Cellular and in vivo Experiments.
Martinelli P, Schaaf O, Mantoulidis A, Martin LJ, Fuchs JE, Bader G, Gollner A, Wolkerstorfer B, Rogers C, Balıkçı E, Lipp JJ, Mischerikow N, Doebel S, Gerstberger T, Sommergruber W, Huber KVM, Böttcher J. Martinelli P, et al. Among authors: bottcher j. ChemMedChem. 2023 Mar 14;18(6):e202200686. doi: 10.1002/cmdc.202200686. Epub 2023 Feb 6. ChemMedChem. 2023. PMID: 36649575
Drugging all RAS isoforms with one pocket.
Kessler D, Bergner A, Böttcher J, Fischer G, Döbel S, Hinkel M, Müllauer B, Weiss-Puxbaum A, McConnell DB. Kessler D, et al. Among authors: bottcher j. Future Med Chem. 2020 Nov;12(21):1911-1923. doi: 10.4155/fmc-2020-0221. Epub 2020 Aug 11. Future Med Chem. 2020. PMID: 32779487 Free article. Review.
HUWE1 employs a giant substrate-binding ring to feed and regulate its HECT E3 domain.
Grabarczyk DB, Petrova OA, Deszcz L, Kurzbauer R, Murphy P, Ahel J, Vogel A, Gogova R, Faas V, Kordic D, Schleiffer A, Meinhart A, Imre R, Lehner A, Neuhold J, Bader G, Stolt-Bergner P, Böttcher J, Wolkerstorfer B, Fischer G, Grishkovskaya I, Haselbach D, Kessler D, Clausen T. Grabarczyk DB, et al. Among authors: bottcher j. Nat Chem Biol. 2021 Oct;17(10):1084-1092. doi: 10.1038/s41589-021-00831-5. Epub 2021 Jul 22. Nat Chem Biol. 2021. PMID: 34294896 Free PMC article.
Pan-KRAS inhibitor disables oncogenic signalling and tumour growth.
Kim D, Herdeis L, Rudolph D, Zhao Y, Böttcher J, Vides A, Ayala-Santos CI, Pourfarjam Y, Cuevas-Navarro A, Xue JY, Mantoulidis A, Bröker J, Wunberg T, Schaaf O, Popow J, Wolkerstorfer B, Kropatsch KG, Qu R, de Stanchina E, Sang B, Li C, McConnell DB, Kraut N, Lito P. Kim D, et al. Among authors: bottcher j. Nature. 2023 Jul;619(7968):160-166. doi: 10.1038/s41586-023-06123-3. Epub 2023 May 31. Nature. 2023. PMID: 37258666 Free PMC article.
246 results