Correlation between Membrane Permeability and the Intracellular Degradation Activity of Proteolysis-Targeting Chimeras

• Published in: Chemical & pharmaceutical bulletin Vol. 72; no. 11; pp. 961 - 965
• Main Authors: Yokoo, Hidetomo, Osawa, Hinata, Saito, Kosuke, Demizu, Yosuke
• Format: Journal Article
• Language: English
• Published: Japan The Pharmaceutical Society of Japan 14.11.2024; Japan Science and Technology Agency
• Subjects: Cell Membrane Permeability - drug effects; Cell membranes; Chimeras; Chromatography, Liquid; Correlation; Degradation; degradation activity; Design optimization; Humans; LC-tandem mass spectrometry (LC-MS/MS); linker optimization; Mass spectrometry; Mass spectroscopy; Membrane permeability; Molecular Structure; Permeability; Proteolysis; Proteolysis - drug effects; proteolysis-targeting chimera; Tandem Mass Spectrometry; degradation activity; LC-tandem mass spectrometry (LC-MS/MS); linker optimization; membrane permeability; proteolysis-targeting chimera

Proteolysis-targeting chimeras (PROTACs) have attracted attention as an innovative drug modality that induces the selective degradation of target proteins. This technology shows higher activity than conventional inhibitors and holds great potential in the field of drug discovery. Optimization of the...