Issue 19, 2021

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

Abstract

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.

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

Supplementary files

Article information

Article type
Edge Article
Submitted
19 jan 2021
Accepted
03 apr 2021
First published
09 apr 2021
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY-NC license

Chem. Sci., 2021,12, 6732-6736

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

D. G. Rawale, K. Thakur, P. Sreekumar, S. T. K., R. A., S. R. Adusumalli, R. K. Mishra and V. Rai, Chem. Sci., 2021, 12, 6732 DOI: 10.1039/D1SC00335F

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