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Page 1
A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo.
Kofink C, Trainor N, Mair B, Wöhrle S, Wurm M, Mischerikow N, Roy MJ, Bader G, Greb P, Garavel G, Diers E, McLennan R, Whitworth C, Vetma V, Rumpel K, Scharnweber M, Fuchs JE, Gerstberger T, Cui Y, Gremel G, Chetta P, Hopf S, Budano N, Rinnenthal J, Gmaschitz G, Mayer M, Koegl M, Ciulli A, Weinstabl H, Farnaby W. Kofink C, et al. Nat Commun. 2022 Oct 10;13(1):5969. doi: 10.1038/s41467-022-33430-6. Nat Commun. 2022. PMID: 36216795 Free PMC article.
Discovery of Novel Spiro[3H-indole-3,2'-pyrrolidin]-2(1H)-one Compounds as Chemically Stable and Orally Active Inhibitors of the MDM2-p53 Interaction.
Gollner A, Rudolph D, Arnhof H, Bauer M, Blake SM, Boehmelt G, Cockroft XL, Dahmann G, Ettmayer P, Gerstberger T, Karolyi-Oezguer J, Kessler D, Kofink C, Ramharter J, Rinnenthal J, Savchenko A, Schnitzer R, Weinstabl H, Weyer-Czernilofsky U, Wunberg T, McConnell DB. Gollner A, et al. Among authors: kofink c. J Med Chem. 2016 Nov 23;59(22):10147-10162. doi: 10.1021/acs.jmedchem.6b00900. Epub 2016 Nov 15. J Med Chem. 2016. PMID: 27775892
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: kofink c. 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.
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: kofink c. ChemMedChem. 2021 May 6;16(9):1420-1424. doi: 10.1002/cmdc.202000839. Epub 2021 Jan 14. ChemMedChem. 2021. PMID: 33275320 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: kofink c. 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
Homo-BacPROTAC-induced degradation of ClpC1 as a strategy against drug-resistant mycobacteria.
Junk L, Schmiedel VM, Guha S, Fischel K, Greb P, Vill K, Krisilia V, van Geelen L, Rumpel K, Kaur P, Krishnamurthy RV, Narayanan S, Shandil RK, Singh M, Kofink C, Mantoulidis A, Biber P, Gmaschitz G, Kazmaier U, Meinhart A, Leodolter J, Hoi D, Junker S, Morreale FE, Clausen T, Kalscheuer R, Weinstabl H, Boehmelt G. Junk L, et al. Among authors: kofink c. Nat Commun. 2024 Mar 5;15(1):2005. doi: 10.1038/s41467-024-46218-7. Nat Commun. 2024. PMID: 38443338 Free PMC article.
Targeting cancer with small-molecule pan-KRAS degraders.
Popow J, Farnaby W, Gollner A, Kofink C, Fischer G, Wurm M, Zollman D, Wijaya A, Mischerikow N, Hasenoehrl C, Prokofeva P, Arnhof H, Arce-Solano S, Bell S, Boeck G, Diers E, Frost AB, Goodwin-Tindall J, Karolyi-Oezguer J, Khan S, Klawatsch T, Koegl M, Kousek R, Kratochvil B, Kropatsch K, Lauber AA, McLennan R, Olt S, Peter D, Petermann O, Roessler V, Stolt-Bergner P, Strack P, Strauss E, Trainor N, Vetma V, Whitworth C, Zhong S, Quant J, Weinstabl H, Kuster B, Ettmayer P, Ciulli A. Popow J, et al. Among authors: kofink c. Science. 2024 Sep 20;385(6715):1338-1347. doi: 10.1126/science.adm8684. Epub 2024 Sep 19. Science. 2024. PMID: 39298590
16 results