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.

Sulfinyl Aziridines as Stereoselective Covalent Destabilizing Degraders of the Oncogenic Transcription Factor MYC

H. T. Rosen ,  K. Li ,  C. E. Stieger ,  E. L. Li ,  B. Currier ,  S. M. Brittain ,  F. J. Garcia ,  D. C. Beard ,  M. D. Jones ,  S. Haenni...