Therapeutic hijacking of E3 Ligases

Project Information

Glue2Degrade

Grant agreement ID: 851478

DOI

10.3030/851478

Project closed

EC signature date 15 October 2019

Start date 1 January 2020

End date 31 December 2024

Funded under

• EXCELLENT SCIENCE - European Research Council (ERC)

Total cost

€ 1 331 340,00

EU contribution

€ 1 331 340,00

Coordinated by

CEMM - FORSCHUNGSZENTRUM FUER MOLEKULARE MEDIZIN GMBH
Austria

CORDIS provides links to public deliverables and publications of HORIZON projects.

Links to deliverables and publications from FP7 projects, as well as links to some specific result types such as dataset and software, are dynamically retrieved from OpenAIRE .

Publications

Non-peer reviewed articles (2)

Monovalent Pseudo-Natural Product Degraders Supercharge the Native Degradation of IDO1 by KLHDC3

Author(s): Hennes E , Lucas B , Scholes NS , Cheng X , Scott DC , Bischoff M , Reich K , Gasper R , Lucas M , Xu TT , Pulvermacher L , Dötsch L , Imrichova H , Brause A , Naredla KR , Sievers S , Kumar K , Janning P , Gersch M , Murray PJ , Schulman BA , Winter GE , Ziegler S , Waldmann H
Published in: bioRxiv, 2024, ISSN 2692-8205
Publisher: bioRxiv
DOI: 10.1101/2024.07.10.602857

Inhibitor-induced supercharging of kinase turnover via endogenous proteolytic circuits

Author(s): Natalie S. Scholes, Martino Bertoni, Arnau Comajuncosa-Creus, Katharina Kladnik, Fabian Frommelt, Matthias Hinterndorfer, Hlib Razumkov, Polina Prokofeva, Martin P. Schwalm, Hana Imrichova, Eleonora Barone, Caroline Schätz, Andrea Rukavina, Anna Koren, Stefan Kubicek, Stefan Knapp, Nathanael S. Gray, Giulio Superti-Furga, Bernhard Kuster, Patrick Aloy, Georg E. Winter
Published in: bioRxiv, 2024, ISSN 2692-8205
Publisher: bioRxiv
DOI: 10.1101/2024.07.10.602881

Peer reviewed articles (11)

Discovery of Molecular Glue Degraders via Isogenic Morphological Profiling.

Author(s): 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
Published in: ACS Chemical Biology, Issue 18(12), 2023, ISSN 1554-8929
Publisher: American Chemical Society
DOI: 10.1021/acschembio.3c00598

Rational discovery of molecular glue degraders via scalable chemical profiling

Author(s): Cristina Mayor-Ruiz, Sophie Bauer, Matthias Brand, Zuzanna Kozicka, Marton Siklos, Hana Imrichova, Ines H. Kaltheuner, Elisa Hahn, Kristina Seiler, Anna Koren, Georg Petzold, Michaela Fellner, Christoph Bock, André C. Müller, Johannes Zuber, Matthias Geyer, Nicolas H. Thomä, Stefan Kubicek, Georg E. Winter
Published in: Nature Chemical Biology, Issue 16/11, 2020, Page(s) 1199-1207, ISSN 1552-4450
Publisher: Nature Publishing Group
DOI: 10.1038/s41589-020-0594-x

Discovery of a Drug-like, Natural Product-Inspired DCAF11 Ligand Chemotype

Author(s): Gang Xue, Jianing Xie, Matthias Hinterndorfer, Marko Cigler, Lara Dötsch, Hana Imrichova, Philipp Lampe, Xiufen Cheng, Soheila Rezaei Adariani, Georg E. Winter & Herbert Waldmann
Published in: Nature Communications, Issue 14(1), 2023, ISSN 2041-1723
Publisher: Nature Publishing Group
DOI: 10.1038/s41467-023-43657-6

Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders

Author(s): Hanzl, A., Casement, R., Imrichova, H., Hughes, S. J., Barone, E., Testa, A., Bauer, S., Wright, J., Brand, M., Ciulli, A., & Winter, G. E.
Published in: Nature Chemical Biology, 2022, ISSN 1552-4450
Publisher: Nature Publishing Group
DOI: 10.1038/s41589-022-01177-2

Targeted protein degradation via intramolecular bivalent glues

Author(s): Hsia O., Hinterndorfer M., Cowan A. D., Iso, K., Ishida T., Sundaramoorthy R., Nakasone M. A., Imrichova H., Schätz C., Rukavina A., Husnjak K., Wegner M., Correa-Sáez A., Craigon C., Casement R., Maniaci C., Testa A., Kaulich M., Dikic I., Winter G. E., Ciulli A.
Published in: Nature, Issue 627, 2024, Page(s) 204-211, ISSN 2041-1723
Publisher: Nature Publishing Group
DOI: 10.1038/s41586-024-07089-6

E3-Specific Degrader Discovery by Dynamic Tracing of Substrate Receptor Abundance

Author(s): Alexander Hanzl, Eleonora Barone, Sophie Bauer, Hong Yue, Radosław P. Nowak, Elisa Hahn, Eugenia V. Pankevich, Anna Koren, Stefan Kubicek, Eric S. Fischer, and Georg E. Winter
Published in: Journal of the American Chemical Society, Issue 2023 Jan, 2023, Page(s) 1176–1184, ISSN 0002-7863
Publisher: American Chemical Society
DOI: 10.1021/jacs.2c10784

Degradome analysis to identify direct protein substrates of small-molecule degraders

Author(s): Marco Jochem, Anna Schrempf, Lina-Marie Wagner, Dmitri Segal, Jose Cisneros, Amanda Ng, Georg E. Winter, Jeroen Krijgsveld
Published in: Cell Chemical Biology, Issue 32, 2025, Page(s) 192-200.e6, ISSN 2451-9456
Publisher: Elsevier Ltd
DOI: 10.1016/j.chembiol.2024.10.007

Advancing Targeted Protein Degradation via Multiomics Profiling and Artificial Intelligence

Author(s): Miquel Duran-Frigola; Marko Cigler; Georg E. Winter
Published in: Journal of the American Chemical Society, Issue 145(5), 2023, Page(s) 2711-2732, ISSN 0002-7863
Publisher: American Chemical Society
DOI: 10.1021/jacs.2c11098

Leveraging Dual-Ligase Recruitment to Enhance Protein Degradation via a Heterotrivalent Proteolysis Targeting Chimera

Author(s): Adam G. Bond, Miquel Muñoz i Ordoño, Celia M. Bisbach, Conner Craigon, Nikolai Makukhin, Elizabeth A. Caine, Manjula Nagala, Marjeta Urh, Georg E. Winter, Kristin M. Riching, Alessio Ciulli
Published in: Journal of the American Chemical Society, Issue 146, 2024, Page(s) 33675-33711, ISSN 0002-7863
Publisher: American Chemical Society
DOI: 10.1021/jacs.4c11556

Discovery of a DCAF11-dependent cyanoacrylamide-containing covalent degrader of BET-proteins

Author(s): Gary Tin, Marko Cigler, Matthias Hinterndorfer, Kevin D. Dong, Hana Imrichova, Steven P. Gygi, Georg E. Winter
Published in: Bioorganic & Medicinal Chemistry Letters, Issue Volume 107, 2024, ISSN 0960-894X
Publisher: Pergamon Press Ltd.
DOI: 10.1016/j.bmcl.2024.129779

Alkylamine-tethered molecules recruit FBXO22 for targeted protein degradation

Author(s): Chrysanthi Kagiou, Jose A. Cisneros, Jakob Farnung, Joanna Liwocha, Fabian Offensperger, Kevin Dong, Ka Yang, Gary Tin, Christina S. Horstmann, Matthias Hinterndorfer, Joao A. Paulo, Natalie S. Scholes, Juan Sanchez Avila, Michaela Fellner, Florian Andersch, J. Thomas Hannich, Johannes Zuber, Stefan Kubicek, Steven P. Gygi, Brenda A. Schulman & Georg E. Winter
Published in: Nature Communications, Issue 15(1), 2024, ISSN 2041-1723
Publisher: Nature Publishing Group
DOI: 10.1038/s41467-024-49739-3

Other (1)

Identification and selectivity profiling of small-molecule degraders via multi-omics approaches

Author(s): Natalie S Scholes, Cristina Mayor-Ruiz, Georg E Winter
Published in: Cell Chemical Biology, Issue Volume 28, Issue 7, 2021, Page(s) P1048-1060
Publisher: Elsevier Ltd
DOI: 10.1016/j.chembiol.2021.03.007

Conference proceedings (1)

Proximity-inducing pharmacology

Author(s): Winter GE, Mayor-Ruiz C
Published in: Nature Chemical Biology, Issue 20(1), 2024, Page(s) 13-14, ISSN 2041-1723
Publisher: Nature Publishing Group
DOI: 10.1038/s41589-023-01492-2

Intellectual Property Rights

Patent (2)

METHOD FOR IDENTIFYING A CHEMICAL COMPOUND OR AGENT INDUCING UBIQUITINATION OF A PROTEIN OF INTEREST

Application/Publication number: 20 21078696
Date: 2019-10-16
Applicant(s): CEMM - FORSCHUNGSZENTRUM FUER MOLEKULARE MEDIZIN GMBH

CULLIN RING UBIQUITIN LIGASE COMPOUNDS AND USES THEREOF

Application/Publication number: 20 21078696
Date: 2021-10-15
Applicant(s): CEMM - FORSCHUNGSZENTRUM FUER MOLEKULARE MEDIZIN GMBH