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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: gmaschitz g. Nat Commun. 2024 Mar 5;15(1):2005. doi: 10.1038/s41467-024-46218-7. Nat Commun. 2024. PMID: 38443338 Free PMC article.
Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor.
Bröker J, Waterson AG, Smethurst C, Kessler D, Böttcher J, Mayer M, Gmaschitz G, Phan J, Little A, Abbott JR, Sun Q, Gmachl M, Rudolph D, Arnhof H, Rumpel K, Savarese F, Gerstberger T, Mischerikow N, Treu M, Herdeis L, Wunberg T, Gollner A, Weinstabl H, Mantoulidis A, Krämer O, McConnell DB, W Fesik S. Bröker J, et al. Among authors: gmaschitz g. J Med Chem. 2022 Nov 10;65(21):14614-14629. doi: 10.1021/acs.jmedchem.2c01120. Epub 2022 Oct 27. J Med Chem. 2022. PMID: 36300829 Free PMC article.
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. Among authors: gmaschitz g. Nat Commun. 2022 Oct 10;13(1):5969. doi: 10.1038/s41467-022-33430-6. Nat Commun. 2022. PMID: 36216795 Free PMC article.
Targeted Synthesis of Complex Spiro[3H-indole-3,2'-pyrrolidin]-2(1H)-ones by Intramolecular Cyclization of Azomethine Ylides: Highly Potent MDM2-p53 Inhibitors.
Gollner A, Weinstabl H, Fuchs JE, Rudolph D, Garavel G, Hofbauer KS, Karolyi-Oezguer J, Gmaschitz G, Hela W, Kerres N, Grondal E, Werni P, Ramharter J, Broeker J, McConnell DB. Gollner A, et al. Among authors: gmaschitz g. ChemMedChem. 2019 Jan 8;14(1):88-93. doi: 10.1002/cmdc.201800617. Epub 2018 Dec 11. ChemMedChem. 2019. PMID: 30458062 Free PMC article.