Dynamics in the p38 alpha MAP Kinase-SB203580 Complex Observed by Liquid-State NMR Spectroscopy

摘要

Diaryl-heterocycle compounds were the first small-molecule inhibitors targeting mitogen-activated protein(MAP)kinases.The diaryl heterocycle SB203580 binds in an adenosine triphosphate(ATP)competitive manner to inactive and active p38 alpha MAP kinase with similar ICS0 values.A dissociation constant(K_D)of 11.5 nM was reported for the inactive form.Crystallographic studies showed that SB203580 binds in the ATP-binding site of p38 alpha.