Results 271 to 280 of about 504,547 (295)
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Utilizing natural products as new E3 ligase ligands for targeted protein degradation.
Chinese Journal of Natural Medicines, 2023Yanan Gong +3 more
semanticscholar +3 more sources
Bioorganic & Medicinal Chemistry, 2023
Tumor hypoxia-activated proteolysis targeting chimeras (ha-PROTACs) 9 and 10 were designed and synthesized by incorporating the hypoxia-activated leaving group (1-methyl-2-nitro-1H-imidazol-5-yl)methyl or 4‑nitrobenzyl into the structure of the cereblon (
W. Cheng +8 more
semanticscholar +1 more source
Tumor hypoxia-activated proteolysis targeting chimeras (ha-PROTACs) 9 and 10 were designed and synthesized by incorporating the hypoxia-activated leaving group (1-methyl-2-nitro-1H-imidazol-5-yl)methyl or 4‑nitrobenzyl into the structure of the cereblon (
W. Cheng +8 more
semanticscholar +1 more source
Ligandability of E3 Ligases for Targeted Protein Degradation Applications
Biochemistry, 2021Targeted protein degradation (TPD) using proteolysis targeting chimeras (PROTACs) and molecular glue degraders has arisen as a powerful therapeutic modality for eliminating disease-causing proteins from cells. PROTACs and molecular glue degraders employ heterobifunctional or monovalent small molecules, respectively, to chemically induce the proximity ...
Bridget P. Belcher +2 more
openaire +2 more sources
Expanding the Ligand Spaces for E3 Ligases for the Design of Protein Degraders
Bioorganic and Medicinal ChemistryTargeted protein degradation (TPD) has recently emerged as an exciting new drug modality. However, the strategy of developing small molecule-based protein degraders has evolved over the past two decades and has now established molecular tags that are already in clinical use, as well as chimeric molecules, PROteolysis TArgeting Chimeras (PROTACs), based
Stefan Knapp +2 more
exaly +6 more sources
Dioxin Receptor Is a Ligand-Dependent E3 Ubiquitin Ligase
Nature, 2007Fat-soluble ligands, including sex steroid hormones and environmental toxins, activate ligand-dependent DNA-sequence-specific transcriptional factors that transduce signals through target-gene-selective transcriptional regulation. However, the mechanisms of cellular perception of fat-soluble ligand signals through other target-selective systems remain ...
Tomoki Chiba +2 more
exaly +3 more sources
European journal of medicinal chemistry, 2023
The scientific community has shown considerable interest in proteolysis-targeting chimeras (PROTACs) in the last decade, indicating their remarkable potential as a means of achieving targeted protein degradation (TPD).
Nisha Setia +2 more
semanticscholar +1 more source
The scientific community has shown considerable interest in proteolysis-targeting chimeras (PROTACs) in the last decade, indicating their remarkable potential as a means of achieving targeted protein degradation (TPD).
Nisha Setia +2 more
semanticscholar +1 more source
Bioorganic & Medicinal Chemistry, 2023
A proteolysis targeting chimera (PROTAC) is a bivalent molecule consisting of an E3 ligase ligand and a protein of interest ligand, which promotes the degradation of specific proteins by recruiting the ubiquitin-proteasome system.
Emma K. Seipp, Rong Huang
semanticscholar +1 more source
A proteolysis targeting chimera (PROTAC) is a bivalent molecule consisting of an E3 ligase ligand and a protein of interest ligand, which promotes the degradation of specific proteins by recruiting the ubiquitin-proteasome system.
Emma K. Seipp, Rong Huang
semanticscholar +1 more source
Chemical Specification of E3 Ubiquitin Ligase Engagement by Cysteine-Reactive Chemistry.
Journal of the American Chemical Society, 2023Targeted protein degradation relies on small molecules that induce new protein-protein interactions between targets and the cellular protein degradation machinery. Most of these small molecules feature specific ligands for ubiquitin ligases.
Roman C. Sarott +15 more
semanticscholar +1 more source
Chemical Proteomics Identifies RBBP7 as a New E3 Ligase Supporting Targeted Protein Degradation.
Angewandte ChemieTargeted protein degradation (TPD) has been recognized as a powerful therapeutic strategy for the treatment of a wide range of diseases. However, the application of existing degraders is constrained by their dependence on a limited number of E3 ubiquitin
Yue Liu +6 more
semanticscholar +1 more source
Evaluation and characterisation of novel E3 ligase ligands for degrader development
PROTACs (PROteolyis Targeting Chimeras) have assumed a pivotal role in drug discovery, introducing the event-driven pharmacology of targeted protein degradation (TPD) as a powerful novel drug modality. The ability of PROTACs to induce the proteolytic degradation of a POI by harnessing the endogenous ubiquitin proteasome system (UPS) in a catalytic ...openaire +1 more source