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.

A Global Ligandability Map of Tryptoline Butynamide Stereoprobes Identifies Covalent Inhibitors of the Actin Maturation Protease ACTMAP

Yijun Xiong, Christopher J. Reinhardt, Tracey Nguyen, Melissa A. Hoffman, Gabriel M. Simon, Bruno Melillo, Benjamin F. Cravatt bioRxiv , 202...