Lysosome-targeting chimaeras for degradation of extracellular proteins | Nature
Lysosome-targeting chimaeras—in which a small molecule or antibody is connected to a glycopeptide ligand to form a conjugate that can bind a cell-surface lysosome-shuttling receptor and a protein target—are used to achieve the targeted degradation of extracellular and membrane proteins.
Subjects Carbohydrate chemistry Chemical tools Lysosomes Transporters Abstract The majority of therapies that target individual proteins rely on specific activity-modulating interactions with the target protein—for example, enzyme inhibition or ligand blocking. However, several major classes of therapeutically relevant proteins have unknown or inaccessible activity profiles and so cannot be targeted by such strategies. Protein-degradation platforms such as proteolysis-targeting chimaeras (PROTACs) 1 , 2 and others (for example, dTAGs 3 , Trim-Away 4 , chaperone-mediated autophagy targeting 5 a
saved by
related reading
- Protein degradation reaches further outnature.com
- Lysosome-targeting chimeras evolve | Nature Chemical Biologynature.com
- Frontiers | Therapeutic Antibodies against Intracellular Tumor Antigensfrontiersin.org
- Development of a targeted BioPROTAC degrader selective for misfolded SOD1nature.com
- PDB101: Molecule of the Month: PROTACs and Molecular Glue Degraderspdb101.rcsb.org
- Engineering Plastic-Degrading Enzymes and PCSK9 Binders with Protein AI Toolsblog.latch.bio
- The dTAG system for immediate and target-specific protein degradationpmc.ncbi.nlm.nih.gov
- Targeting UGCG overcomes resistance to lysosomal autophagy inhibitionpmc.ncbi.nlm.nih.gov
- Protein purification workflow – The Bumbling Biochemistthebumblingbiochemist.com
- Technologies to measure and modulate protein subcellular localizationnature.com
- Programmed exosome fusion for energy generation in living cellsnature.com
- Spatial N-glycan rearrangement on α5β1 integrin nucleates galectin-3 oligomers to determine endocytic fatenature.com