Results 1 to 10 of about 38,081 (111)
Discovery of E3 Ligase Ligands for Target Protein Degradation
Molecules, 2022 Target protein degradation has emerged as a promising strategy for the discovery of novel therapeutics during the last decade. Proteolysis-targeting chimera (PROTAC) harnesses a cellular ubiquitin-dependent proteolysis system for the efficient degradation of a protein of interest.
Jaeseok Lee +2 more
exaly +6 more sources
E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones [PDF]
SLAS Discovery, 2021 Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are a new modality of chemical tools and potential therapeutics to understand and treat human disease. A required PROTAC component is a ligand binding to an E3 ubiquitin ligase, which is then joined to another ligand binding to a protein to be degraded via the ...
Alessio Ciulli
exaly +7 more sources
E3 ligase ligand optimization of Clinical PROTACs [PDF]
Frontiers in Chemistry, 2023 Proteolysis targeting chimeras (PROTACs) technology can realize the development of drugs for non-druggable targets that are difficult to achieve with traditional small molecules, and therefore has attracted extensive attention from both academia and industry.
Huan Xiong +2 more
exaly +6 more sources
E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points [PDF]
Frontiers in Chemistry, 2021 Proteolysis-targeting chimeras (PROTACs) have received tremendous attention as a new and exciting class of therapeutic agents that promise to significantly impact drug discovery. These bifunctional molecules consist of a target binding unit, a linker, and an E3 ligase binding moiety.
Aleša Bricelj +2 more
exaly +5 more sources
Design, Synthesis, and Biological Evaluation of HDAC Degraders with CRBN E3 Ligase Ligands [PDF]
Molecules, 2021 Histone deacetylases (HDACs) play important roles in cell growth, cell differentiation, cell apoptosis, and many other cellular processes. The inhibition of different classes of HDACs has been shown to be closely related to the therapy of cancers and other diseases.
Yingxin Lu +8 more
openaire +4 more sources
Informatics in Medicine Unlocked, 2023 Abstract 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 +4 more
openaire +3 more sources
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 attachment of ubiquitin to substrate proteins.
Iacovos N. Michaelides, Gavin W. Collie
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Mind Bomb-2 Is an E3 Ligase for Notch Ligand [PDF]
Journal of Biological Chemistry, 2005 The zebrafish gene, mind bomb (mib), encodes a protein that positively regulates of the Delta-mediated Notch signaling. It interacts with the intracellular domain of Delta to promote its ubiquitination and endocytosis. In our search for the mouse homologue of zebrafish mind bomb, we cloned two homologues in the mouse genome: a mouse orthologue (mouse ...
Bon-Kyoung, Koo +7 more
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BH3‐ligand regulates access of MCL‐1 to its E3 ligase [PDF]
FEBS Letters, 2005 A genome wide search for new BH3‐containing Bcl‐2 family members was conducted using position weight matrices (PWM) and identified a large (480 kDa), novel BH3‐only protein, originally called LASU1 (now also known as Ureb‐1, E3histone, ARF‐BP1, and Mule).
Warr, Matthew R. +7 more
openaire +2 more sources
A caged E3 ligase ligand for PROTAC-mediated protein degradation with light
Chemical Communications, 2020 Caging of a widely used Von Hippel Lindau E3 ligase ligand for targeted protein degradation with PROTACs allows light-activated proteolysis.
Cyrille S. Kounde +6 more
openaire +4 more sources