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E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points
Bricelj, Aleša, Steinebach, Christian, Kuchta, Robert, Gütschow, Michael, Sosič, Izidor
Published in Frontiers in chemistry (05.07.2021)
Published in Frontiers in chemistry (05.07.2021)
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3CL Protease Inhibitors with an Electrophilic Arylketone Moiety as Anti-SARS-CoV‑2 Agents
Konno, Sho, Kobayashi, Kiyotaka, Senda, Miki, Funai, Yuta, Seki, Yuta, Tamai, Ikumi, Schäkel, Laura, Sakata, Kyousuke, Pillaiyar, Thanigaimalai, Taguchi, Akihiro, Taniguchi, Atsuhiko, Gütschow, Michael, Müller, Christa E, Takeuchi, Koh, Hirohama, Mikako, Kawaguchi, Atsushi, Kojima, Masaki, Senda, Toshiya, Shirasaka, Yoshiyuki, Kamitani, Wataru, Hayashi, Yoshio
Published in Journal of medicinal chemistry (24.02.2022)
Published in Journal of medicinal chemistry (24.02.2022)
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Calcium-sensing receptors signal constitutive macropinocytosis and facilitate the uptake of NOD2 ligands in macrophages
Canton, Johnathan, Schlam, Daniel, Breuer, Christian, Gütschow, Michael, Glogauer, Michael, Grinstein, Sergio
Published in Nature communications (06.04.2016)
Published in Nature communications (06.04.2016)
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Homo-PROTACs for the Chemical Knockdown of Cereblon
Steinebach, Christian, Lindner, Stefanie, Udeshi, Namrata D, Mani, Deepak C, Kehm, Hannes, Köpff, Simon, Carr, Steven A, Gütschow, Michael, Krönke, Jan
Published in ACS chemical biology (21.09.2018)
Published in ACS chemical biology (21.09.2018)
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Dysfunction of the key ferroptosis-surveilling systems hypersensitizes mice to tubular necrosis during acute kidney injury
Tonnus, Wulf, Meyer, Claudia, Steinebach, Christian, Belavgeni, Alexia, von Mässenhausen, Anne, Gonzalez, Nadia Zamora, Maremonti, Francesca, Gembardt, Florian, Himmerkus, Nina, Latk, Markus, Locke, Sophie, Marschner, Julian, Li, Wenjun, Short, Spencer, Doll, Sebastian, Ingold, Irina, Proneth, Bettina, Daniel, Christoph, Kabgani, Nazanin, Kramann, Rafael, Motika, Stephen, Hergenrother, Paul J., Bornstein, Stefan R., Hugo, Christian, Becker, Jan Ulrich, Amann, Kerstin, Anders, Hans-Joachim, Kreisel, Daniel, Pratt, Derek, Gütschow, Michael, Conrad, Marcus, Linkermann, Andreas
Published in Nature communications (20.07.2021)
Published in Nature communications (20.07.2021)
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Can Cysteine Protease Cross-Class Inhibitors Achieve Selectivity?
Cianni, Lorenzo, Feldmann, Christian Wolfgang, Gilberg, Erik, Gütschow, Michael, Juliano, Luiz, Leitão, Andrei, Bajorath, Jürgen, Montanari, Carlos A
Published in Journal of medicinal chemistry (12.12.2019)
Published in Journal of medicinal chemistry (12.12.2019)
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Targeting the Main Protease of SARS‐CoV‐2: From the Establishment of High Throughput Screening to the Design of Tailored Inhibitors
Breidenbach, Julian, Lemke, Carina, Pillaiyar, Thanigaimalai, Schäkel, Laura, Al Hamwi, Ghazl, Diett, Miriam, Gedschold, Robin, Geiger, Nina, Lopez, Vittoria, Mirza, Salahuddin, Namasivayam, Vigneshwaran, Schiedel, Anke C., Sylvester, Katharina, Thimm, Dominik, Vielmuth, Christin, Phuong Vu, Lan, Zyulina, Maria, Bodem, Jochen, Gütschow, Michael, Müller, Christa E.
Published in Angewandte Chemie International Edition (26.04.2021)
Published in Angewandte Chemie International Edition (26.04.2021)
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Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV‑2 Main Protease Inhibitors with High Target Specificity and Low Toxicity
Gao, Shenghua, Sylvester, Katharina, Song, Letian, Claff, Tobias, Jing, Lanlan, Woodson, Molly, Weiße, Renato H., Cheng, Yusen, Schäkel, Laura, Petry, Marvin, Gütschow, Michael, Schiedel, Anke C., Sträter, Norbert, Kang, Dongwei, Xu, Shujing, Toth, Karoly, Tavis, John, Tollefson, Ann E., Müller, Christa E., Liu, Xinyong, Zhan, Peng
Published in Journal of medicinal chemistry (13.10.2022)
Published in Journal of medicinal chemistry (13.10.2022)
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Macrocyclic Azapeptide Nitriles: Structure-Based Discovery of Potent SARS-CoV‑2 Main Protease Inhibitors as Antiviral Drugs
Breidenbach, Julian, Voget, Rabea, Si, Yaoyao, Hingst, Alexandra, Claff, Tobias, Sylvester, Katharina, Wolf, Valentina, Krasniqi, Vesa, Useini, Abibe, Sträter, Norbert, Ogura, Yukino, Kawaguchi, Atsushi, Müller, Christa E., Gütschow, Michael
Published in Journal of Medicinal Chemistry (13.06.2024)
Published in Journal of Medicinal Chemistry (13.06.2024)
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X‑ray Structures of Target–Ligand Complexes Containing Compounds with Assay Interference Potential
Gilberg, Erik, Gütschow, Michael, Bajorath, Jürgen
Published in Journal of medicinal chemistry (08.02.2018)
Published in Journal of medicinal chemistry (08.02.2018)
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Influence of Linker Attachment Points on the Stability and Neosubstrate Degradation of Cereblon Ligands
Bricelj, Aleša, Dora Ng, Yuen Lam, Ferber, Dominic, Kuchta, Robert, Müller, Sina, Monschke, Marius, Wagner, Karl G, Krönke, Jan, Sosič, Izidor, Gütschow, Michael, Steinebach, Christian
Published in ACS medicinal chemistry letters (11.11.2021)
Published in ACS medicinal chemistry letters (11.11.2021)
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PROTAC-mediated crosstalk between E3 ligases
Steinebach, Christian, Kehm, Hannes, Lindner, Stefanie, Vu, Lan Phuong, Köpff, Simon, López Mármol, Álvaro, Weiler, Corinna, Wagner, Karl G, Reichenzeller, Michaela, Krönke, Jan, Gütschow, Michael
Published in Chemical communications (Cambridge, England) (05.02.2019)
Published in Chemical communications (Cambridge, England) (05.02.2019)
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Structural Optimization of Azadipeptide Nitriles Strongly Increases Association Rates and Allows the Development of Selective Cathepsin Inhibitors
Frizler, Maxim, Lohr, Friederike, Furtmann, Norbert, Kläs, Julia, Gütschow, Michael
Published in Journal of medicinal chemistry (13.01.2011)
Published in Journal of medicinal chemistry (13.01.2011)
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Small-Molecule Thioesters as SARS-CoV‑2 Main Protease Inhibitors: Enzyme Inhibition, Structure–Activity Relationships, Antiviral Activity, and X‑ray Structure Determination
Pillaiyar, Thanigaimalai, Flury, Philipp, Krüger, Nadine, Su, Haixia, Schäkel, Laura, Barbosa Da Silva, Elany, Eppler, Olga, Kronenberger, Thales, Nie, Tianqing, Luedtke, Stephanie, Rocha, Cheila, Sylvester, Katharina, Petry, Marvin R.I., McKerrow, James H., Poso, Antti, Pöhlmann, Stefan, Gütschow, Michael, O’Donoghue, Anthony J., Xu, Yechun, Müller, Christa E., Laufer, Stefan A.
Published in Journal of medicinal chemistry (14.07.2022)
Published in Journal of medicinal chemistry (14.07.2022)
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Solubility Enhanced Formulation Approaches to Overcome Oral Delivery Obstacles of PROTACs
Pöstges, Florian, Kayser, Kevin, Appelhaus, Jan, Monschke, Marius, Gütschow, Michael, Steinebach, Christian, Wagner, Karl G.
Published in Pharmaceutics (03.01.2023)
Published in Pharmaceutics (03.01.2023)
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Conversion of Daidzein and Genistein by an Anaerobic Bacterium Newly Isolated from the Mouse Intestine
Matthies, Anastasia, Clavel, Thomas, Gütschow, Michael, Engst, Wolfram, Haller, Dirk, Blaut, Michael, Braune, Annett
Published in Applied and Environmental Microbiology (01.08.2008)
Published in Applied and Environmental Microbiology (01.08.2008)
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Proteomic profiling reveals CDK6 upregulation as a targetable resistance mechanism for lenalidomide in multiple myeloma
Ng, Yuen Lam Dora, Ramberger, Evelyn, Bohl, Stephan R., Dolnik, Anna, Steinebach, Christian, Conrad, Theresia, Müller, Sina, Popp, Oliver, Kull, Miriam, Haji, Mohamed, Gütschow, Michael, Döhner, Hartmut, Walther, Wolfgang, Keller, Ulrich, Bullinger, Lars, Mertins, Philipp, Krönke, Jan
Published in Nature communications (23.02.2022)
Published in Nature communications (23.02.2022)
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Leveraging Ligand Affinity and Properties: Discovery of Novel Benzamide-Type Cereblon Binders for the Design of PROTACs
Steinebach, Christian, Bricelj, Aleša, Murgai, Arunima, Sosič, Izidor, Bischof, Luca, Ng, Yuen Lam Dora, Heim, Christopher, Maiwald, Samuel, Proj, Matic, Voget, Rabea, Feller, Felix, Košmrlj, Janez, Sapozhnikova, Valeriia, Schmidt, Annika, Zuleeg, Maximilian Rudolf, Lemnitzer, Patricia, Mertins, Philipp, Hansen, Finn K., Gütschow, Michael, Krönke, Jan, Hartmann, Marcus D.
Published in Journal of medicinal chemistry (09.11.2023)
Published in Journal of medicinal chemistry (09.11.2023)
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