Friday, April 9, 2021

Linchpin empowers promiscuous electrophile to render site-selective modification of histidine and aspartic acid in proteins [@vishal_iiserb]

Dattatraya Gautam Rawale,   Kalyani Thakur,   Pranav Sreekumar,   Sajeev T. K.,   Ramesh A,   Srinivasa Rao Adusumalli,   Ram Kumar Mishra  and  Vishal Rai  

Chemical Science, 2021

https://doi.org/10.1039/D1SC00335F

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 render site-selectivity for histidine and aspartic acid modification overcoming the pre-requisite of chemoselectivity.

Preclinical characterization of EGT710, an oral non-peptidomimetic reversible covalent SARS-CoV-2 main protease inhibitor

Stephanie A. Moquin, Suresh B. Lakshminarayana, Kamal Kumar Balavenkatraman, Hilmar Schiller, Allison Claas, Barun Bhhatarai, Ioannis Loisio...