Covalent PROTAC design method based on a sulfonyl pyridone probe
Literature Information
Publication Date
2023-11-29
DOI
10.1039/D3CC05127G
Impact Factor
6.222
Authors
Yaqi Wang, Zhanfeng Hou, Licheng Tu, Chuan Wan, Jianbo Liu, Rui Wang, Wei Han, Jianlong Wu, Fei Lu
View Original
Abstract
Covalent proteolysis-targeting chimeras (PROTACs) offer enhanced selectivity, prolonged action, and increased efficacy against challenging target proteins. The conventional approach relies on covalent ligands, but our study presents an innovative method employing an N-sulfonyl pyridone warhead to selectively target tyrosine (Tyr) residues. The von Hippel–Lindau (VHL) moiety is transferred from the warhead to the exposed Tyr, allowing us to design a STING degrader (DC50 0.53 μM, Dmax 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.
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Source Journal
Chemical Communications
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Recommended Compounds
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N-{[(2-Methyl-2-propanyl)oxy]carbonyl}-L-methionylglycine
CAS Number:
23446-03-9
Molecular Formula:
C12H22N2O5S
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1-{3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl}-2,3-dihydroxy-1-propanone
CAS Number:
1226872-27-0
Molecular Formula:
C25H26N6O4
Benzyl 6-oxo-3,6-dihydro-1(2H)-pyridinecarboxylate
CAS Number:
725746-35-0
Molecular Formula:
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