Linchpins empower promiscuous electrophiles to enable site-selective modification of histidine and aspartic acid in proteins

The conservation of chemoselectivity becomes invalid for multiple electrophilic warheads during protein bioconjugation. Consequently, it leads to unpredictable heterogeneous labeling of proteins. Here, we report that a linchpin can create a unique chemical space to enable site-selectivity for histid...

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Bibliographic Details
Published in:Chemical science (Cambridge) 2021-05, Vol.12 (19), p.6732-6736
Main Authors: Rawale, Dattatraya Gautam, Thakur, Kalyani, Sreekumar, Pranav, , Adusumalli, Srinivasa Rao, Mishra, Ram Kumar, Rai, Vishal
Format: Article
Language:English
Subjects:
Aspartic acid
Chemistry
Histidine
Proteins
Selectivity
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Summary:The conservation of chemoselectivity becomes invalid for multiple electrophilic warheads during protein bioconjugation. Consequently, it leads to unpredictable heterogeneous labeling of proteins. Here, we report that a linchpin can create a unique chemical space to enable site-selectivity for histidine and aspartic acid modifications overcoming the pre-requisite of chemoselectivity. Linchpin-enabled promiscuous electrophile uncovers an unchartered reactivity landscape for the precision engineering of proteins.
ISSN:2041-6520
2041-6539
DOI:10.1039/d1sc00335f