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Year
Paper
2023

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/
2023

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/
2023

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/
2023

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/
2023

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/
2023

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/
2023

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/
2023

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/
2022

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/
2022

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/
2022

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/
2022

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/
Year
Paper
2021
Müller S, Ackloo S, Al Chawaf A, Al-Lazikani B, Antolin A, Baell JB, Beck H, Beedie S, Betz UAK, Bezerra GA, Brennan PE, Brown D, Brown PJ, Bullock AN, Carter AJ, Chaikuad A, Chaineau M, Ciulli A, Collins I, Dreher J, Drewry D, Edfeldt K, Edwards AM, Egner U, Frye SV, Fuchs SM, Hall MD, Hartung IV, Hillisch A, Hitchcock SH, Homan E, Kannan N, Kiefer JR, Knapp S, Kostic M, Kubicek S, Leach AR, Lindemann S, Marsden BD, Matsui H, Meier JL, Merk D, Michel M, Morgan MR, Mueller-Fahrnow A, Owen DR, Perry BG, Rosenberg SH, Saikatendu KS, Schapira M, Scholten C, Sharma S, Simeonov A, Sundström M, Superti-Furga G, Todd MH, Tredup C, Vedadi M, von Delft F, Willson TM, Winter GE, Workman P, Arrowsmith CH. Target 2035 - update on the quest for a probe for every protein. 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/
2021
Ciulli A, Hamann L, Jahnke W, Kalgutkar AS, Magauer T, Ritter T, Steadman V, Williams SD, Winter G, Hoegenauer K, Krawinkler KH, Stepan AF. The 2(nd) Alpine Winter Conference on Medicinal and Synthetic Chemistry. ChemMedChem. 2021 Aug 5;16(15):2417-2423. doi: 10.1002/cmdc.202100372. Epub 2021 Jun 10.
Abstract: https://pubmed.ncbi.nlm.nih.gov/34114371/
2021
Žumer K, Maier KC, Farnung L, Jaeger MG, Rus P, Winter G, Cramer P. Two distinct mechanisms of RNA polymerase II elongation stimulation in vivo. Mol Cell. 2021 Aug 5;81(15):3096-3109.e8. doi: 10.1016/j.molcel.2021.05.028. Epub 2021 Jun 18.
Abstract: https://pubmed.ncbi.nlm.nih.gov/34146481/
2021
Schick S, Grosche S, Kohl KE, Drpic D, Jaeger MG, Marella NC, Imrichova H, Lin JG, Hofstätter G, Schuster M, Rendeiro AF, Koren A, Petronczki M, Bock C, Müller AC, Winter GE, Kubicek S. Acute BAF perturbation causes immediate changes in chromatin accessibility. Nat Genet. 2021 Mar;53(3):269-278. doi: 10.1038/s41588-021-00777-3. Epub 2021 Feb 8.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33558760/
2021
Valent P, Orfao A, Kubicek S, Staber P, Haferlach T, Deininger M, Kollmann K, Lion T, Virgolini I, Winter G, Hantschel O, Kenner L, Zuber J, Grebien F, Moriggl R, Hoermann G, Hermine O, Andreeff M, Bock C, Mughal T, Constantinescu SN, Kralovics R, Sexl V, Skoda R, Superti-Furga G, Jäger U. Precision Medicine in Hematology 2021: Definitions, Tools, Perspectives, and Open Questions. Hemasphere. 2021 Feb 17;5(3):e536. doi: 10.1097/HS9.0000000000000536. eCollection 2021 Mar.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33623882/
2021
Mayor-Ruiz C, Bauer S, Brand M, Kozicka Z, Siklos M, Imrichova H, Kaltheuner IH, Hahn E, Seiler K, Koren A, Petzold G, Fellner M, Bock C, Müller AC, Zuber J, Geyer M, Thomä NH, Kubicek S, Winter GE. Publisher Correction: Rational discovery of molecular glue degraders via scalable chemical profiling. Nat Chem Biol. 2021 Mar;17(3):361. doi: 10.1038/s41589-021-00735-4.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33452497/
2021
Jaeger MG, Winter GE. Fast-acting chemical tools to delineate causality in transcriptional control. Mol Cell. 2021 Apr 15;81(8):1617-1630. doi: 10.1016/j.molcel.2021.02.015. Epub 2021 Mar 8.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33689749/
2021
Kiely-Collins H, Winter GE, Bernardes GJL. The role of reversible and irreversible covalent chemistry in targeted protein degradation. Cell Chem Biol. 2021 Mar 25:S2451-9456(21)00144-6. doi: 10.1016/j.chembiol.2021.03.005. Online ahead of print.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33789091/
2021
Scholes NS, Mayor-Ruiz C, Winter GE. Identification and selectivity profiling of small-molecule degraders via multi-omics approaches. Cell Chem Biol. 2021 Mar 29:S2451-9456(21)00146-X. doi: 10.1016/j.chembiol.2021.03.007. Online ahead of print.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33811812/
2020
Hanzl A, Winter GE. Targeted protein degradation: current and future challenges. Curr Opin Chem Biol. 2020 Jun;56:35-41. doi: 10.1016/j.cbpa.2019.11.012. Epub 2020 Jan 2. PMID: 31901786.
Abstract: https://pubmed.ncbi.nlm.nih.gov/31901786/
2020
Bensimon A, Pizzagalli MD, Kartnig F, Dvorak V, Essletzbichler P, Winter GE, Superti-Furga G. Targeted Degradation of SLC Transporters Reveals Amenability of Multi-Pass Transmembrane Proteins to Ligand-Induced Proteolysis. Cell Chem Biol. 2020 Jun 18;27(6):728-739.e9. doi: 10.1016/j.chembiol.2020.04.003. Epub 2020 May 7.
Abstract: https://pubmed.ncbi.nlm.nih.gov/32386596/
2020
Jaeger MG, Schwalb B, Mackowiak SD, Velychko T, Hanzl A, Imrichova H, Brand M, Agerer B, Chorn S, Nabet B, Ferguson FM, Müller AC, Bergthaler A, Gray NS, Bradner JE, Bock C, Hnisz D, Cramer P, Winter GE. Selective Mediator dependence of cell-type-specifying transcription. Nat Genet. 2020 Jul;52(7):719-727. doi: 10.1038/s41588-020-0635-0. Epub 2020 Jun 1.
Abstract: https://pubmed.ncbi.nlm.nih.gov/32483291/
2020
Mayor-Ruiz C, Bauer S, Brand M, Kozicka Z, Siklos M, Imrichova H, Kaltheuner IH, Hahn E, Seiler K, Koren A, Petzold G, Fellner M, Bock C, Müller AC, Zuber J, Geyer M, Thomä NH, Kubicek S, Winter GE. Rational discovery of molecular glue degraders via scalable chemical profiling. Nat Chem Biol. 2020 Nov;16(11):1199-1207. doi: 10.1038/s41589-020-0594-x. Epub 2020 Aug 3. Erratum in: Nat Chem Biol. 2021 Mar;17(3):361.
Abstract: https://pubmed.ncbi.nlm.nih.gov/32747809/
2020
Gaviraghi M, Rabellino A, Andolfo A, Brand M, Brombin C, Bagnato P, De Feudis G, Raimondi A, Locatelli A, Tosoni D, Mazza D, Gianni L, Tonon G, Yarden Y, Tacchetti C, Daniele T. Direct stimulation of ERBB2 highlights a novel cytostatic signaling pathway driven by the receptor Thr(701) phosphorylation. Sci Rep. 2020 Oct 9;10(1):16906. doi: 10.1038/s41598-020-73835-1.
Abstract: https://pubmed.ncbi.nlm.nih.gov/33037285/
2020
C Mayor-Ruiz, S Bauer, M Brand, Z Kozicka, M Siklos, H Imrichova, IH Kaltheuner, E Hahn, K Seiler, A Koren, G Petzold, M Fellner, C Bock, AC Müller, J Zuber, M Geyer, NH Thomä, S Kubicek, G E Winter. Rational discovery of molecular glue degraders via scalable chemical profiling. Nat Chem Biol. 2020 Nov;16(11):1199-1207.doi: 10.1038/s41589-020-0594-x. Epub 2020 Aug 3.
Abstract: https://pubmed.ncbi.nlm.nih.gov/32747809/
2020
Jaeger MG, Winter GE. Expanding the Degradable Proteome: Designing PROTACs by the Book. Cell Chem Biol. 2020 Jan 16;27(1):14-16. doi: 10.1016/j.chembiol.2019.12.009.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/31951815
2019
Mayor-Ruiz C, Jaeger MG, Bauer S, Brand M, Sin C, Hanzl A, Mueller AC, Menche J, Winter GE. Plasticity of the Cullin-RING Ligase Repertoire Shapes Sensitivity to Ligand-Induced Protein Degradation. Mol Cell. 2019 Aug 22;75(4):849-858.e8. doi: 10.1016/j.molcel.2019.07.013.
Abstract: https://pubmed.ncbi.nlm.nih.gov/31442425/
2019
Ferreira da Silva J, Salic S, Wiedner M, Datlinger P, Essletzbichler P, Hanzl A, Superti-Furga G, Bock C, Winter G, Loizou JI. Genome-scale CRISPR screens are efficient in non-homologous end-joining deficient cells. Sci Rep. 2019 Oct 31;9(1):15751. doi: 10.1038/s41598-019-52078-9.
Abstract: https://pubmed.ncbi.nlm.nih.gov/31673055/
2019
Sdelci S, Rendeiro AF, Rathert P, You W, Lin JG, Ringler A, Hofstätter G,Moll HP, Gürtl B, Farlik M, Schick S, Klepsch F, Oldach M, Buphamalai P,Schischlik F, Májek P, Parapatics K, Schmidl C, Schuster M, Penz T, Buckley DL,Hudecz O, Imre R, Wang SY, Maric HM, Kralovics R, Bennett KL, Müller AC, MechtlerK, Menche J, Bradner JE, Winter GE, Klavins K, Casanova E, Bock C, Zuber J,Kubicek S. MTHFD1 interaction with BRD4 links folate metabolism to transcriptional regulation. Nat Genet. 2019 Jun;51(6):990-998. doi:10.1038/s41588-019-0413-z. Epub 2019 May 27.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/31133746
2019
Mayor-Ruiz C, Winter GE. Identification and characterization of cancer vulnerabilities via targeted protein degradation. Drug Discov Today Technol. 2019Apr;31:81-90. doi: 10.1016/j.ddtec.2018.12.003. Epub 2019 Jan 2. Review.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/31200863.
2019
Brand M, Winter GE. Locus-Specific Knock-In of a Degradable Tag for Target Validation Studies. Methods Mol Biol. 2019;1953:105-119. doi:10.1007/978-1-4939-9145-7_7.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/30912018
2019
Brand M, Jiang B, Bauer S, Donovan KA, Liang Y, Wang ES, Nowak RP, Yuan JC,Zhang T, Kwiatkowski N, Müller AC, Fischer ES, Gray NS, Winter GE.Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML.Cell Chem Biol. 2019 Feb 21;26(2):300-306.e9. doi:10.1016/j.chembiol.2018.11.006. Epub 2018 Dec 27.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/30595531
2019
Brand M, Winter GE. Stick it to E3s. Nat Chem Biol. 2019 Jul;15(7):655-656.doi: 10.1038/s41589-019-0312-8.
Abstract: https://www.ncbi.nlm.nih.gov/pubmed/31209352