![Benzo[b]naphtho[2,1-d]thiophene structure](https://cnstatic.chemtradehub.com/structs/239/239-35-0-ff90.webp "Benzo[b]naphtho[2,1-d]thiophene structure")
Covalent PROTAC design method based on a sulfonyl pyridone probe
文献信息
发布日期
2023-11-29
DOI
10.1039/D3CC05127G
影响因子
6.222
作者
Yaqi Wang, Zhanfeng Hou, Licheng Tu, Chuan Wan, Jianbo Liu, Rui Wang, Wei Han, Jianlong Wu, Fei Lu
查看原文
摘要
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.
期刊推荐
Journal of Asian Natural Products Research
Bioorganic & Medicinal Chemistry
Bioorganic & Medicinal Chemistry Letters
Electroanalysis
Biocatalysis and Biotransformation
NDT & E International
Acta Metallurgica Sinica-English Letters
Medicinal Chemistry Research
Chinese Journal of Chemistry
Polycyclic Aromatic Compounds
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来源期刊
Chemical Communications
CiteScore:
8.6
自引率:
4.7%
年发文量:
2458
ChemComm publishes urgent research which is of outstanding significance and interest to experts in the field, while also appealing to the journal’s broad chemistry readership. Our communication format is ideally suited to short, urgent studies that are of such importance that they require accelerated publication. Our scope covers all topics in chemistry, and research at the interface of chemistry and other disciplines (such as materials science, nanoscience, physics, engineering and biology) where there is a significant novelty in the chemistry aspects. Major topic areas covered include: Analytical Chemistry Catalysis Chemical Biology and medicinal chemistry Computational Chemistry and Machine Learning Energy and sustainable chemistry Environmental Chemistry Green Chemistry Inorganic Chemistry Materials Chemistry Nanoscience Organic Chemistry Physical Chemistry Polymer Chemistry Supramolecular Chemistry
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