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Page 1
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: weinstabl h. Science. 2024 Sep 20;385(6715):1338-1347. doi: 10.1126/science.adm8684. Epub 2024 Sep 19. Science. 2024. PMID: 39298590
Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2-p53 Antagonist Suitable for Intermittent Dose Schedules.
Gollner A, Rudolph D, Weyer-Czernilofsky U, Baumgartinger R, Jung P, Weinstabl H, Ramharter J, Grempler R, Quant J, Rinnenthal J, Pérez Pitarch A, Golubovic B, Gerlach D, Bader G, Wetzel K, Otto S, Mandl C, Boehmelt G, McConnell DB, Kraut N, Sini P. Gollner A, et al. Among authors: weinstabl h. Mol Cancer Ther. 2024 Dec 3;23(12):1689-1702. doi: 10.1158/1535-7163.MCT-23-0783. Mol Cancer Ther. 2024. PMID: 39259562 Free PMC article. Clinical Trial.
Confounding Factors in Targeted Degradation of Short-Lived Proteins.
Vetma V, Perez LC, Eliaš J, Stingu A, Kombara A, Gmaschitz T, Braun N, Ciftci T, Dahmann G, Diers E, Gerstberger T, Greb P, Kidd G, Kofink C, Puoti I, Spiteri V, Trainor N, Weinstabl H, Westermaier Y, Whitworth C, Ciulli A, Farnaby W, McAulay K, Frost AB, Chessum N, Koegl M. Vetma V, et al. Among authors: weinstabl h. ACS Chem Biol. 2024 Jul 19;19(7):1484-1494. doi: 10.1021/acschembio.4c00152. Epub 2024 Jul 3. ACS Chem Biol. 2024. PMID: 38958654
Synthesis of Complex Tetracyclic Fused Scaffolds Enabled by (3 + 2) Cycloaddition.
Porte V, van Veen BC, Zhang H, Piacentini P, Matheu SA, Woolford S, Sokol KR, Shaaban S, Weinstabl H, Maulide N. Porte V, et al. Among authors: weinstabl h. Org Lett. 2024 Jun 14;26(23):4873-4876. doi: 10.1021/acs.orglett.4c01269. Epub 2024 May 31. Org Lett. 2024. PMID: 38820198 Free PMC article.
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.
28 results