Discovery of E3 Ligase Ligands for Target Protein Degradation [PDF]
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 ...
Jaeseok Lee +5 more
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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.
Aleša Bricelj +4 more
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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 ...
Hanrui Jiang +6 more
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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.
Alessio Ciulli
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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 ...
Yingxin Lu +8 more
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Proteomic analysis reveals novel ligands and substrates for LNX1 E3 ubiquitin ligase. [PDF]
PLoS ONE, 2017 Ligand of Numb protein X1 (LNX1) is an E3 ubiquitin ligase that contains a catalytic RING (Really Interesting New Gene) domain and four PDZ (PSD-95, DlgA, ZO-1) domains. LNX1 can ubiquitinate Numb, as well as a number of other ligands.
Joan A Lenihan +2 more
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Discovery of Small Molecule Ligands for the Von Hippel-Lindau (VHL) E3 Ligase and Their Use as Inhibitors and PROTAC Degraders [PDF]
Chemical Society Reviews, 2022 The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-proteasome system that recruits substrates such as the hypoxia inducible factor for ubiquitination and subsequent proteasomal degradation.
Claudia J Diehl, Alessio Ciulli
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A Patent Review of Von Hippel-Lindau (VHL)-Recruiting Chemical Matter: E3 Ligase Ligands for PROTACs and Targeted Protein Degradation (2019–Present) [PDF]
Expert Opinion on Therapeutic PatentsIntroduction The von Hippel-Lindau (VHL) E3 ubiquitin ligase has seen extensive research due to its involvement in the ubiquitin proteasome system and role as a tumor suppressor within the hypoxia signaling pathway.
Aina Urbina +2 more
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PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective
Acta Materia Medica, 2022 Mouse double minute 2 (MDM2) is an oncogenic E3 ligase that effectively degrades the tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt MDM2-p53 binding have been discovered and developed.
Xin Han, Wenyi Wei, Yi Sun
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Cell Chemical Biology, 2020 SUMMARY Proteolysis targeting chimeras (PROTACs) is a paradigm shift for small molecule drug discovery. However, limited E3 ubiquitin ligase ligands with cellular activity are available.
Bo Wang, Ka Yang, Weiping Tang
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