Covalent PROTAC design method based on a sulfonyl pyridone probe
Qinhong Luo, Yaqi Wang, Zhanfeng Hou, Huiting Liang, Licheng Tu, Yun Xing, Chuan Wan, Jianbo Liu, Rui Wang, Lizhi Zhu, Wei Han, Jianlong Wu, Fei Lü, Feng Yin, Zigang Li
Abstract
56.65%). This approach showcases the potential of nucleophilic amino acid labeling probes, particularly for proteins lacking easily accessible cysteine residues, opening new possibilities for covalent PROTAC design and targeted protein degradation therapies.
Topics & Concepts
MoietyCovalent bondCysteineChemistrySulfonylCombinatorial chemistryWarheadTyrosineProteolysisNucleophileAmino acidStereochemistryBiochemistryOrganic chemistryEnzymeAerospace engineeringEngineeringCatalysisAlkylProtein Degradation and InhibitorsPeptidase Inhibition and AnalysisCAR-T cell therapy research