Hydrophobic Tag Tethering Degradation, The Emerging TargetedProtein Degradation Strategy
Jieke Gao, Jiantao Zhang, Xiaoli Han, Jinming Zhou
Abstract
Targeted protein degradation (TPD) strategies have become a new trend in drug discovery due to the capability of triggering the degradation of protein of interest (POI) selectively and effectively in recent decades. Particularly, the hydrophobic tag tethering degrader (HyTTD) has drawn a lot of attention and may offer a promising strategy for new drug research and development in the future. Herein, we will give an overview of the development of HyTTD, the structure-activity relationship (SAR) between HyTTD and linkers, HyTs, and ligand motifs, as well as the various HyTTDs targeting different targets, thus offering a rational strategy for the design of HyTTDs in further TPD drug discovery.
Topics & Concepts
Drug discoveryTetheringDegradation (telecommunications)Computational biologyChemistryDrugProtein degradationNanotechnologyComputer scienceCell biologyBiologyBiochemistryPharmacologyMaterials scienceTelecommunicationsProtein Degradation and InhibitorsRadiation Effects in ElectronicsUbiquitin and proteasome pathways