Groups
Discovery and Mechanistic Elucidation of NQO1-Bioactivatable Small Molecules That Overcome Resistance to Degraders
Bárbara M G Barbosa, Aikaterini Sfyaki, Sergi Rafael, Ferran José-Duran, Joan Pous, Carolina Sánchez-Zarzalejo, Carles Perez-Lopez, Mar Vilanova, Marko Cigler, Marina Gay, Marta Vilaseca, Georg E Winter, Antoni Riera, Cristina Mayor-Ruiz.Angew Chem Int Ed Engl. 2023 Dec 28:e202316730. doi: 10.1002/anie.202316730. Online ahead of print.
Abstract: https://pubmed.ncbi.nlm.nih.gov/38153885/
Discovery of Molecular Glue Degraders via Isogenic Morphological Profiling
Amanda Ng, Fabian Offensperger, Jose A Cisneros, Natalie S Scholes, Monika Malik, Ludovica Villanti, Andrea Rukavina, Evandro Ferrada, J Thomas Hannich, Anna Koren, Stefan Kubicek, Giulio Superti-Furga, Georg E Winter.ACS Chem Biol. 2023 Dec 15;18(12):2464-2473. doi: 10.1021/acschembio.3c00598. Epub 2023 Nov 21.
Abstract: https://pubmed.ncbi.nlm.nih.gov/38098458/
Discovery of a Drug-like, Natural Product-Inspired DCAF11 Ligand Chemotype
Gang Xue, Jianing Xie, Matthias Hinterndorfer, Marko Cigler, Lara Dötsch, Hana Imrichova, Philipp Lampe, Xiufen Cheng, Soheila Rezaei Adariani, Georg E Winter, Herbert Waldmann.Nat Commun. 2023 Nov 30;14(1):7908. doi: 10.1038/s41467-023-43657-6.
Abstract: https://pubmed.ncbi.nlm.nih.gov/38036533/
Proximity-inducing pharmacology
Georg E Winter, Cristina Mayor-Ruiz.Nat Chem Biol. 2023 Nov 17. doi: 10.1038/s41589-023-01492-2. Online ahead of print.
Abstract: https://pubmed.ncbi.nlm.nih.gov/37978259/
Design principles for cyclin K molecular glue degraders
Zuzanna Kozicka, Dakota J Suchyta, Vivian Focht, Georg Kempf, Georg Petzold, Marius Jentzsch, Charles Zou, Cristina Di Genua, Katherine A Donovan, Seemon Coomar, Marko Cigler, Cristina Mayor-Ruiz, Jonathan L Schmid-Burgk, Daniel Häussinger, Georg E Winter, Eric S Fischer, Mikołaj Słabicki, Dennis Gillingham, Benjamin L Ebert, Nicolas H Thomä.Nat Chem Biol. 2024 Jan;20(1):93-102. doi: 10.1038/s41589-023-01409-z. Epub 2023 Sep 7.
Abstract: https://pubmed.ncbi.nlm.nih.gov/37679459/
Pharmacological perturbation of the phase-separating protein SMNDC1
Lennart Enders, Marton Siklos, Jan Borggräfe, Stefan Gaussmann, Anna Koren, Monika Malik, Tatjana Tomek, Michael Schuster, Jiří Reiniš, Elisa Hahn, Andrea Rukavina, Andreas Reicher, Tamara Casteels, Christoph Bock, Georg E Winter, J Thomas Hannich, Michael Sattler, Stefan Kubicek.Nat Commun. 2023 Aug 16;14(1):4504. doi: 10.1038/s41467-023-40124-0.
Abstract: https://pubmed.ncbi.nlm.nih.gov/37587144/
Advancing Targeted Protein Degradation via Multiomics Profiling and Artificial Intelligence
Miquel Duran-Frigola, Marko Cigler, Georg E Winter.J Am Chem Soc. 2023 Feb 8;145(5):2711-2732. doi: 10.1021/jacs.2c11098. Epub 2023 Jan 27.
Abstract: https://pubmed.ncbi.nlm.nih.gov/36706315/
E3-Specific Degrader Discovery by Dynamic Tracing of Substrate Receptor Abundance
Alexander Hanzl, Eleonora Barone, Sophie Bauer, Hong Yue, Radosław P Nowak, Elisa Hahn, Eugenia V Pankevich, Anna Koren, Stefan Kubicek, Eric S Fischer, Georg E Winter.J Am Chem Soc. 2023 Jan 18;145(2):1176-1184. doi: 10.1021/jacs.2c10784. Epub 2023 Jan 5.
Abstract: https://pubmed.ncbi.nlm.nih.gov/36602777/
CIDE-stepping E3s
Gary Tin, Georg E Winter.Nat Chem Biol. 2023 Jan;19(1):3-4. doi: 10.1038/s41589-022-01217-x.
Abstract: https://pubmed.ncbi.nlm.nih.gov/36577874/
Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders
Alexander Hanzl, Ryan Casement, Hana Imrichova, Scott J Hughes, Eleonora Barone, Andrea Testa, Sophie Bauer, Jane Wright, Matthias Brand, Alessio Ciulli, Georg E Winter.Nat Chem Biol. 2023 Mar;19(3):323-333. doi: 10.1038/s41589-022-01177-2. Epub 2022 Nov 3.
Abstract: https://pubmed.ncbi.nlm.nih.gov/36329119/
BRD4 degradation blocks expression of MYC and multiple forms of stem cell resistance in Ph+ chronic myeloid leukemia
Barbara Peter, Gregor Eisenwort, Irina Sadovnik, Karin Bauer, Michael Willmann, Thomas Rülicke, Daniela Berger, Gabriele Stefanzl, Georg Greiner, Gregor Hoermann, Alexandra Keller, Dominik Wolf, Martin Čulen, Georg E Winter, Thomas Hoffmann, Ana-Iris Schiefer, Wolfgang R Sperr, Johannes Zuber, Jiří Mayer, Peter Valent.Am J Hematol. 2022 Sep;97(9):1215-1225. doi: 10.1002/ajh.26650. Epub 2022 Jul 18.
Abstract: https://pubmed.ncbi.nlm.nih.gov/35794848/
Target 2035 - update on the quest for a probe for every protein
Susanne Müller, Suzanne Ackloo, Arij Al Chawaf, Bissan Al-Lazikani, Albert Antolin, Jonathan B Baell, Hartmut Beck, Shaunna Beedie, Ulrich A K Betz, Gustavo Arruda Bezerra, Paul E Brennan, David Brown, Peter J Brown, Alex N Bullock, Adrian J Carter, Apirat Chaikuad, Mathilde Chaineau, Alessio Ciulli, Ian Collins, Jan Dreher, David Drewry, Kristina Edfeldt, Aled M Edwards, Ursula Egner, Stephen V Frye, Stephen M Fuchs, Matthew D Hall, Ingo V Hartung, Alexander Hillisch, Stephen H Hitchcock, Evert Homan, Natarajan Kannan, James R Kiefer, Stefan Knapp, Milka Kostic, Stefan Kubicek, Andrew R Leach, Sven Lindemann, Brian D Marsden, Hisanori Matsui, Jordan L Meier, Daniel Merk, Maurice Michel, Maxwell R Morgan, Anke Mueller-Fahrnow, Dafydd R Owen, Benjamin G Perry, Saul H Rosenberg, Kumar Singh Saikatendu, Matthieu Schapira, Cora Scholten, Sujata Sharma, Anton Simeonov, Michael Sundström, Giulio Superti-Furga, Matthew H Todd, Claudia Tredup, Masoud Vedadi, Frank von Delft, Timothy M Willson, Georg E Winter, Paul Workman, Cheryl H Arrowsmith.RSC Med Chem. 2021 Dec 3;13(1):13-21. doi: 10.1039/d1md00228g. eCollection 2022 Jan 27.
Abstract: https://pubmed.ncbi.nlm.nih.gov/35211674/
Abstract: https://pubmed.ncbi.nlm.nih.gov/35211674/
Abstract: https://pubmed.ncbi.nlm.nih.gov/34114371/
Abstract: https://pubmed.ncbi.nlm.nih.gov/34146481/
Abstract: https://pubmed.ncbi.nlm.nih.gov/33558760/
Abstract: https://pubmed.ncbi.nlm.nih.gov/33623882/
Abstract: https://pubmed.ncbi.nlm.nih.gov/33452497/
Abstract: https://pubmed.ncbi.nlm.nih.gov/33689749/
Abstract: https://pubmed.ncbi.nlm.nih.gov/33789091/
Abstract: https://pubmed.ncbi.nlm.nih.gov/33811812/
Abstract: https://pubmed.ncbi.nlm.nih.gov/31901786/
Abstract: https://pubmed.ncbi.nlm.nih.gov/32386596/
Abstract: https://pubmed.ncbi.nlm.nih.gov/32483291/
Abstract: https://pubmed.ncbi.nlm.nih.gov/32747809/
Abstract: https://pubmed.ncbi.nlm.nih.gov/33037285/
Abstract: https://pubmed.ncbi.nlm.nih.gov/32747809/
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/31951815
Abstract: https://pubmed.ncbi.nlm.nih.gov/31442425/
Abstract: https://pubmed.ncbi.nlm.nih.gov/31673055/
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/31133746
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/31200863.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/30912018
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/30595531
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/31209352