Linchpins empower promiscuous electrophiles to enable site-selective modification of histidine and aspartic acid in proteins. Issue 19 (19th April 2021)

• Record Type: Journal Article
• Authors: Rawale, Dattatraya Gautam; Thakur, Kalyani; Sreekumar, Pranav; T. K., Sajeev; A., Ramesh; Adusumalli, Srinivasa Rao; Mishra, Ram Kumar; Rai, Vishal
• Is Part Of: Chemical science. Volume 12:Issue 19(2021)
• Page Start: 6732
• Page End: 6736
• Publication Date: 2021-04-19
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/d1sc00335f
• Languages: English
• ISSNs: 2041-6520

Abstract

Abstract : Linchpin-enabled promiscuous electrophile uncovers an unchartered reactivity landscape for the precision engineering of 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.