Proteolysis Targeting Chimeric Molecules: Tuning Molecular Strategies for a Clinically Sound Listening

• Published in: International journal of molecular sciences Vol. 23; no. 12; p. 6630
• Main Authors: Pedrucci, Federica, Pappalardo, Claudia, Marzaro, Giovanni, Ferri, Nicola, Ferlin, Alberto, De Toni, Luca
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 14.06.2022; MDPI
• Subjects: Autoimmune diseases; Binding; Binding sites; Biological activity; Clinical trials; Dialectics; Drug development; Efficiency; Enzymes; Gene expression; Kinases; Ligands; Lipinski rule of five; Modular design; molecular glue; Pharmacodynamics; Pharmacokinetics; Pharmacology; Prostate cancer; Proteasome Endopeptidase Complex - metabolism; Proteasomes; Protein Binding; Proteins; Proteolysis; Review; thalidomide; Thrombocytopenia; Ubiquitin-protein ligase; Ubiquitin-Protein Ligases - metabolism; Ubiquitination; Von Hippel-Lindau; warhead; United States > US; Von Hippel-Lindau; molecular glue; warhead; thalidomide; Lipinski rule of five

From seminal evidence in the early 2000s, the opportunity to drive the specific knockdown of a protein of interest (POI) through pharmacological entities called Proteolysis Targeting Chimeric molecules, or PROTACs, has become a possible therapeutic option with the involvement of these compounds in c...