Hydrophobic Tag Tethering Degradation, The Emerging Targeted Protein Degradation Strategy

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 atte...

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Bibliographic Details
Published inCurrent medicinal chemistry Vol. 30; no. 27; p. 3137
Main Authors Gao, Jieke, Zhang, Jiantao, Han, Xiaoli, Zhou, Jinming
Format Journal Article
LanguageEnglish
Published United Arab Emirates 01.01.2023
Subjects
Drug Discovery
Humans
Proteolysis
Skin Neoplasms
Structure-Activity Relationship
hydrophobic tag
hydrophobic tag tethering degrader
drug discovery
HyTTDs
structure-activity relationship
Targeted protein degradation
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Summary: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.
ISSN:1875-533X
DOI:10.2174/0929867329666220930120328