Linchpins empower promiscuous electrophiles to enable site-selective modification of histidine and aspartic acid in proteins.
Dattatraya Gautam RawaleKalyani ThakurPranav SreekumarSajeev T KRamesh ASrinivasa Rao AdusumalliRam Kumar MishraVishal RaiPublished in: Chemical science (2021)
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.
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