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Azaindoles as Zinc-Binding Small-Molecule Inhibitors of the JAMM Protease CSN5.
Altmann E, Erbel P, Renatus M, Schaefer M, Schlierf A, Druet A, Kieffer L, Sorge M, Pfister K, Hassiepen U, Jones M, Ruedisser S, Ostermeier D, Martoglio B, Jefferson AB, Quancard J. Altmann E, et al. Among authors: martoglio b. Angew Chem Int Ed Engl. 2017 Jan 24;56(5):1294-1297. doi: 10.1002/anie.201608672. Epub 2016 Dec 16. Angew Chem Int Ed Engl. 2017. PMID: 27981705
Targeted inhibition of the COP9 signalosome for treatment of cancer.
Schlierf A, Altmann E, Quancard J, Jefferson AB, Assenberg R, Renatus M, Jones M, Hassiepen U, Schaefer M, Kiffe M, Weiss A, Wiesmann C, Sedrani R, Eder J, Martoglio B. Schlierf A, et al. Among authors: martoglio b. Nat Commun. 2016 Oct 24;7:13166. doi: 10.1038/ncomms13166. Nat Commun. 2016. PMID: 27774986 Free PMC article.
Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
Obst-Sander U, Ricci A, Kuhn B, Friess T, Koldewey P, Kuglstatter A, Hewings D, Goergler A, Steiner S, Rueher D, Imhoff MP, Raschetti N, Marty HP, Dietzig A, Rynn C, Ehler A, Burger D, Kornacker M, Schaffland JP, Herting F, Pao W, Bischoff JR, Martoglio B, Alice Nagel Y, Jaeschke G. Obst-Sander U, et al. Among authors: martoglio b. J Med Chem. 2022 Oct 13;65(19):13052-13073. doi: 10.1021/acs.jmedchem.2c00893. Epub 2022 Sep 30. J Med Chem. 2022. PMID: 36178776
Preclinical Characterization of a Next-Generation Brain Permeable, Paradox Breaker BRAF Inhibitor.
Wichmann J, Rynn C, Friess T, Petrig-Schaffland J, Kornacker M, Handl C, Emmenegger J, Eckmann J, Herting F, Frances N, Hunziker D, Krummenacher D, Rüttinger D, Ribeiro A, Bacac M, Brigo A, Hewings DS, Dummer R, Levesque MP, Schnetzler G, Martoglio B, Bischoff JR, Pettazzoni P. Wichmann J, et al. Among authors: martoglio b. Clin Cancer Res. 2022 Feb 15;28(4):770-780. doi: 10.1158/1078-0432.CCR-21-2761. Clin Cancer Res. 2022. PMID: 34782366
Aspartic proteases in drug discovery.
Eder J, Hommel U, Cumin F, Martoglio B, Gerhartz B. Eder J, et al. Among authors: martoglio b. Curr Pharm Des. 2007;13(3):271-85. doi: 10.2174/138161207779313560. Curr Pharm Des. 2007. PMID: 17313361 Review.
The intramembrane protease Sppl2a is required for B cell and DC development and survival via cleavage of the invariant chain.
Beisner DR, Langerak P, Parker AE, Dahlberg C, Otero FJ, Sutton SE, Poirot L, Barnes W, Young MA, Niessen S, Wiltshire T, Bodendorf U, Martoglio B, Cravatt B, Cooke MP. Beisner DR, et al. Among authors: martoglio b. J Exp Med. 2013 Jan 14;210(1):23-30. doi: 10.1084/jem.20121072. Epub 2012 Dec 24. J Exp Med. 2013. PMID: 23267013 Free PMC article.
Cellular Resistance Mechanisms to Targeted Protein Degradation Converge Toward Impairment of the Engaged Ubiquitin Transfer Pathway.
Ottis P, Palladino C, Thienger P, Britschgi A, Heichinger C, Berrera M, Julien-Laferriere A, Roudnicky F, Kam-Thong T, Bischoff JR, Martoglio B, Pettazzoni P. Ottis P, et al. Among authors: martoglio b. ACS Chem Biol. 2019 Oct 18;14(10):2215-2223. doi: 10.1021/acschembio.9b00525. Epub 2019 Oct 8. ACS Chem Biol. 2019. PMID: 31553577
42 results