Journal
CHEMICAL COMMUNICATIONS
Volume 57, Issue 96, Pages 12968-12971Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d1cc04191f
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Funding
- National Natural Science Foundation of China [21778068, 21977111, 22007096]
- Shenzhen Sciences & Technology Innovation Council [JCYJ20170818153538196]
- Natural Science Foundation of Guangdong Province [2019A1515012073, 2018B030308001]
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The dearomatization-rearomatization strategy modifies peptides/proteins through a specific chemical reaction, enriching the toolbox for conjugation and showing great potential for applications in medicinal chemistry and chemical biology.
We have developed a dearomatization-rearomatization strategy for the modification of peptides/proteins through a thiol-Michael addition to the electrophilic cyclohexadienone intermediate that is generated in situ via the oxidation of tyrosine. This strategy enriches the conjugation toolbox and has great potential for applications in medicinal chemistry and chemical biology.
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