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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: weinstabl h. Nat Commun. 2024 Mar 5;15(1):2005. doi: 10.1038/s41467-024-46218-7. Nat Commun. 2024. PMID: 38443338 Free PMC article.
Inhibition of p53-MDM2 binding reduces senescent cell abundance and improves the adaptive responses of skeletal muscle from aged mice.
Nolt GL, Keeble AR, Wen Y, Strong AC, Thomas NT, Valentino TR, Brightwell CR, Murach KA, Patrizia S, Weinstabl H, Gollner A, McCarthy JJ, Fry CS, Franti M, Filareto A, Peterson CA, Dungan CM. Nolt GL, et al. Among authors: weinstabl h. Geroscience. 2024 Apr;46(2):2153-2176. doi: 10.1007/s11357-023-00976-2. Epub 2023 Oct 24. Geroscience. 2024. PMID: 37872294 Free PMC article.
European Medicinal Chemistry Leaders in Industry (EMCL) - On the Status and Future of Medicinal Chemistry Research in Europe.
Ali A, Bauser M, Bertrand S, Blackaby W, Boss C, Bossart M, Hall A, Binch H, Czechtizky W, Gijsen H, Haning H, Hartung IV, Kilburn P, Lassalle G, Lücking U, Mack J, Missbach M, Otsomaa L, Torrens A, Wagner M, Walter M, Weinstabl H, van Hijfte L, von Nussbaum F. Ali A, et al. Among authors: weinstabl h. ChemMedChem. 2023 Jul 3;18(13):e202300127. doi: 10.1002/cmdc.202300127. Epub 2023 Jun 5. ChemMedChem. 2023. PMID: 37276375 Review.
Clp-targeting BacPROTACs impair mycobacterial proteostasis and survival.
Hoi DM, Junker S, Junk L, Schwechel K, Fischel K, Podlesainski D, Hawkins PME, van Geelen L, Kaschani F, Leodolter J, Morreale FE, Kleine S, Guha S, Rumpel K, Schmiedel VM, Weinstabl H, Meinhart A, Payne RJ, Kaiser M, Hartl M, Boehmelt G, Kazmaier U, Kalscheuer R, Clausen T. Hoi DM, et al. Among authors: weinstabl h. Cell. 2023 May 11;186(10):2176-2192.e22. doi: 10.1016/j.cell.2023.04.009. Epub 2023 May 2. Cell. 2023. PMID: 37137307 Free 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: weinstabl h. 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: weinstabl h. Nat Commun. 2022 Oct 10;13(1):5969. doi: 10.1038/s41467-022-33430-6. Nat Commun. 2022. PMID: 36216795 Free PMC article.
BacPROTACs mediate targeted protein degradation in bacteria.
Morreale FE, Kleine S, Leodolter J, Junker S, Hoi DM, Ovchinnikov S, Okun A, Kley J, Kurzbauer R, Junk L, Guha S, Podlesainski D, Kazmaier U, Boehmelt G, Weinstabl H, Rumpel K, Schmiedel VM, Hartl M, Haselbach D, Meinhart A, Kaiser M, Clausen T. Morreale FE, et al. Among authors: weinstabl h. Cell. 2022 Jun 23;185(13):2338-2353.e18. doi: 10.1016/j.cell.2022.05.009. Epub 2022 Jun 3. Cell. 2022. PMID: 35662409 Free PMC article.
24 results