Building blocks and linkers for PROTAC synthesis
Proteolysis targeting chimeras (PROTACs) is the recently emerged field in drug discovery. This new approach works through the activation of the ubiquitin-proteasome system to remove disease-causing proteins. This new modality of therapeutic intervention requires new chemistry and new approaches to synthesize functional PROTAC molecules. Several recent papers of Oprea and Cravatt examined chemical space and ligandable proteome to evaluate a state of the targeted human genome. Herein we offer known and novel building blocks (E3 ligase ligands, ligands with linkers, linkers) for the synthesis of PROTACs.
Ligands for E3 ligases (Cereblon, VHL, MDM2 etc) from stock:
over 100 ligands:
PEG-linkers from stock:
over 50 linkers:
MedChem Highlights
- Aliphatic Trifluoroborates (-BF3) for C-C couplings
- Functionalized Vinyl Boronates for C-C couplings
- Unique 3D-shaped Spirocycles
- Water-soluble non-classical benzene mimics
- gem-Difluorinated Amines for Drug Design
- Fluorosulfates and Sulfamoyl Fluorides
- Alkyne-containing Linkers
- Structurally optimized tetrazines for rapid biological labeling
- Building blocks and linkers for PROTAC synthesis
- Heterocyclic Sulfonyl Fluorides
- Silicon-Containing Building Blocks
- Epoxides for Drug Design
- Analogues of CF3-Pyridine for Drug Design
- Piperazine Bioisosteres for Drug Design
- Sugar-like Building Blocks for Drug Design
- Cyclic Sulfonamides for Drug Design
- Morpholine Bioisosteres for Drug Design
- P(O)Me2-containing Building Blocks
- Saturated Bioisosteres of ortho-/meta-substituted Benzenes
- Saturated bioisosteres of para-substituted benzenes
- Sulfonyl fluorides (-SO2F)
- Diazirines
- Oxetane-containing Building Blocks
- SF5-Building Blocks
- Stannanes for coupling reactions
- Sulfoximines for Drug Design
- Heterocyclic scaffolds
- Azide-linkers for Drug Design
- Unnatural Amino Acids
- Cubane-containing building blocks
- Benzoxaboroles for Drug Design