Metabolically Labile Fumarate Esters Impart Kinetic Selectivity to Irreversible Inhibitors
Balyn W. Zaro, Landon R. Whitby, Kenneth M. Lum, and Benjamin F. Cravatt*
The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, 10550 North Torrey Pines Road, La Jolla, California 92037, United States
J. Am. Chem. Soc., 2016, 138 (49), pp 15841–15844
DOI: 10.1021/jacs.6b10589
The use of a fumarate ester warhead is found to confer greater selectivity than a simple acrylamide warhead for inhibition of Bruton's Tyrosine Kinase (BTK).
