Results 11 to 20 of about 504,547 (295)

Workflow for E3 Ligase Ligand Validation for PROTAC Development [PDF]

ACS Chemical Biology
Proteolysis targeting chimeras (PROTACs) have gained considerable attention as a new modality in drug discovery. The development of PROTACs has been mainly focused on using CRBN (Cereblon) and VHL (Von Hippel-Lindau ligase) E3 ligase ligands.
Stefan Knapp, Václav Nemec, Martin P Schwalm   +2 more
exaly   +7 more sources

Pharmacophore-based ML model to filter candidate E3 ligands and predict E3 Ligase binding probabilities

Informatics in Medicine Unlocked, 2023
Among the plethora of E3 Ligases, only a few have been utilized for the novel PROTAC technology. However, extensive knowledge of the preparation of E3 ligands and their utilization for PROTACs is already present in several databases.
Reagon Karki, Yojana Gadiya, Simran Shetty, Philip Gribbon, Andrea Zaliani   +4 more
doaj   +5 more sources

Discovery of Ligands for TRIM58, a Novel Tissue-Selective E3 Ligase.

ACS Medicinal Chemistry Letters, 2023
Redirecting E3 ligases to neo-substrates, leading to their proteasomal disassembly, known as targeted protein degradation (TPD), has emerged as a promising alternative to traditional, occupancy-driven pharmacology.
Klemens Hoegenauer, Shaojian An, Jake Axford, Christina Benander, Christian Bergsdorf, J. Botsch, Suzanne Chau, César Fernández, Scott Gleim, U. Hassiepen, J. Hunziker, Emilie Joly, Aramis Keller, Sandra López Romero, Robert Maher, A. Mangold, Craig Mickanin, M. Mihalic, P. Neuner, Andrew W. Patterson, Francesca Perruccio, S. Roggo, Julien Scesa, Martina Schröder, Dojna Shkoza, B. Thái, A. Vulpetti, M. Renatus, J. Reece-Hoyes   +28 more
semanticscholar   +4 more sources

The Expanding E3 Ligase-Ligand Landscape for PROTAC Technology

Targets
Proteolysis-targeting chimeras (PROTACs) are a transformative therapeutic modality that co-opts the ubiquitin-proteasome system for selective protein degradation. To date, the development of PROTACs has been overwhelmingly dominated by the recruitment of
Yunxiu Zhang
exaly   +3 more sources

Identification of suitable target/E3 ligase pairs for PROTAC development using a rapamycin-induced proximity assay (RiPA)

eLife
The development of proteolysis targeting chimeras (PROTACs), which induce the degradation of target proteins by bringing them into proximity with cellular E3 ubiquitin ligases, has revolutionized drug development. While the human genome encodes more than
Bikash Adhikari, Katharina Schneider, Mathias Diebold, Christoph Sotriffer, Elmar Wolf   +4 more
doaj   +2 more sources

Peptide-Based Molecular Glues for Targeted Protein Degradation [PDF]

Pharmaceutics
Targeted protein degradation has transformed drug discovery by replacing occupancy-driven inhibition with event-driven removal of disease-causing proteins, opening previously “undruggable” targets, including transcription factors, scaffolding proteins ...
Walaa S. Aburayan, Ibrahim A. Alradwan, Beshair A. Alsaffar, Othman A. Alhazzaa, Fahad A. Almughem, Abdullah A. Alshehri, Ibtihal S. Alduhaymi, Mohannad M. Fallatah, Meshael Alturki, Hassa A. Alshaya, Essam A. Tawfik   +10 more
doaj   +2 more sources

E3 Ligases Meet Their Match: Fragment-Based Approaches to Discover New E3 Ligands and to Unravel E3 Biology

Journal of Medicinal Chemistry, 2023
Ubiquitination is a key post-translational modification of proteins, affecting the regulation of multiple cellular processes. Cells are equipped with over 600 ubiquitin orchestrators, called E3 ubiquitin ligases, responsible for directing the covalent ...
Iacovos N. Michaelides, G. Collie
semanticscholar   +3 more sources

Exploiting ELIOT for Scaffold-Repurposing Opportunities: TRIM33 a Possible Novel E3 Ligase to Expand the Toolbox for PROTAC Design [PDF]

International Journal of Molecular Sciences, 2022
The field of targeted protein degradation, through the control of the ubiquitin–proteasome system (UPS), is progressing considerably; to exploit this new therapeutic modality, the proteolysis targeting chimera (PROTAC) technology was born.
Tommaso Palomba, G. Tassone, C. Vacca, Matteo Bartalucci, Aurora Valeri, C. Pozzi, S. Cross, L. Siragusa, J. Desantis   +8 more
semanticscholar   +2 more sources

A Facile Synthesis of Ligands for the von Hippel–Lindau E3 Ligase

Synthesis, 2020
The proteolysis-targeting chimeras (PROTACs) have become an integral part of different stages of drug discovery. This growing field, therefore, benefits from advancements in all segments of the design of these compounds.
M. Gütschow, C. Steinebach, Sabine Anna Voell, Lan Phuong Vu, Aleša Bricelj, I. Sosič, G. Schnakenburg   +6 more
semanticscholar   +2 more sources

A Caged E3 Ligase Ligand for PROTAC-Mediated Protein Degradation with Light [PDF]

, 2019
A caging group has been appended to a widely used Von Hippel Lindau (VHL) E3 ligase ligand for targeted protein degradation with PROTACs. Proteolysis is triggered only after a short irradiation time allowing spatiotemporal control of the protein’s ...
Maria M., Shchepinova, Edward, Tate, Cyrille, Kounde   +2 more
core   +3 more sources