Results 31 to 40 of about 419,478 (257)
Beyond canonical PROTAC: biological targeted protein degradation (bioTPD)
Biomaterials Research, 2023 Targeted protein degradation (TPD) is an emerging therapeutic strategy with the potential to modulate disease-associated proteins that have previously been considered undruggable, by employing the host destruction machinery. The exploration and discovery
Huifang Wang +12 more
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Targeted Strategies for Degradation of Key Transmembrane Proteins in Cancer
BioTech, 2023 Targeted protein degradation is an attractive technology for cancer treatment due to its ability to overcome the unpredictability of the small molecule inhibitors that cause resistance mutations.
Vehary Sakanyan +2 more
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Targeted Protein Degradation: Principles and Applications of the Proteasome
Cells, 2023 The proteasome is a multi-catalytic protease complex that is involved in protein quality control via three proteolytic activities (i.e., caspase-, trypsin-, and chymotrypsin-like activities).
Yosup Kim +4 more
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Interdisciplinary Medicine, 2023 Proteolysis‐targeting chimeras (PROTACs) is a targeted protein degradation (TPD) technique effected by hijacking the ubiquitin‐proteasome system (UPS) of the cells.
Xuyang Zhao +3 more
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Targeted protein degradation in cancers: Orthodox PROTACs and beyond
The Innovation, 2023 Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology can be used to target proteins by hijacking the ubiquitin-proteasome ...
Jin Li +3 more
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Design of a Cereblon construct for crystallographic and biophysical studies of protein degraders
Nature CommunicationsThe ubiquitin E3 ligase cereblon (CRBN) is the target of therapeutic drugs thalidomide and lenalidomide and is recruited by most targeted protein degraders (PROTACs and molecular glues) in clinical development. Biophysical and structural investigation of
Alena Kroupova +17 more
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Proteomic approaches advancing targeted protein degradation
Trends in Pharmacological Sciences, 2023 Targeted protein degradation (TPD) is an emerging modality for research and therapeutics. Most TPD approaches harness cellular ubiquitin-dependent proteolytic pathways. Proteolysis-targeting chimeras (PROTACs) and molecular glue (MG) degraders (MGDs) represent the most advanced TPD approaches, with some already used in clinical settings.
Gajanan Sathe, Gopal P. Sapkota
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Reciprocal control of viral infection and phosphoinositide dynamics
FEBS Letters, EarlyView.Phosphoinositides, although scarce, regulate key cellular processes, including membrane dynamics and signaling. Viruses exploit these lipids to support their entry, replication, assembly, and egress. The central role of phosphoinositides in infection highlights phosphoinositide metabolism as a promising antiviral target.
Marie Déborah Bancilhon, Bruno Mesmin
wiley +1 more source
DNA framework-engineered chimeras platform enables selectively targeted protein degradation
Nature Communications, 2023 A challenge in developing proteolysis targeting chimeras (PROTACs) is the establishment of a universal platform applicable in multiple scenarios for precise degradation of proteins of interest (POIs).
Li Zhou +7 more
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Targeted Protein Degradation for Kinase Selectivity [PDF]
Cell Chemical Biology, 2019 Targeted protein degradation offers considerable promise for the discovery of new therapeutics. In Cell Chemical Biology, Brand et al. (2019) identify selective degraders of CDK6 derived from clinically approved CDK4/6 inhibitors. This approach offers the possibility of a differentiated therapeutic profile with potential to treat acute myeloid leukemia.
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