Monday, January 15, 2018

Progress with covalent small-molecule kinase inhibitors

Zheng Zhao, Philip E. Bourne
Drug Discovery Today, 2018
With reduced risk of toxicity and high selectivity, covalent small-molecule kinase inhibitors (CSKIs) have emerged rapidly. Through the lens of structural system pharmacology, here we review this rapid progress by considering design strategies and the challenges and opportunities offered by current CSKIs.

Covalent Ligand Electrophiles Are Differentially Activated by Proximity Effects Which Govern Latent Protein Reactivit

  Tomas V. Frankovich, Harrison M. McCann, Kyle S. Hoffman, and Anthony F. Rullo ACS Central Science   Article ASAP DOI: 10.1021/acscentsci....