Sentence examples for bind to the inactive from inspiring English sources
Laufer's group has developed a conformation-specific fluorescent polarization binding assay that was implemented to identify p38 inhibitors that preferably bind to the inactive conformation of the kinase.
A set of kinase-focused compound library was screened using this assay method, and compound 31 was successfully identified as a potent inhibitor which preferentially bind to the inactive conformation of BTK.
It is thought to bind to the inactive and active conformer of PERK (Axten et al., 2012).
Mutations in the a-loop shift the equilibrium towards the active kinase conformation, while imatinib and sunitinib bind to the inactive conformation [ 29].
66, 86 Imatinib is a competitive inhibitor of adenosine triphosphate (ATP) and can only bind to the inactive conformation of KIT.
Furthermore, recently published NMR data suggest that there is a dynamic equilibrium between functional substates of GPCRs and that agonists initially bind to the inactive state of the GPCR and then promote it toward the active state.
What the crystal structure reveals, the team reports in the 15 September issue of Science, is that STI-571 binds to the inactive conformation of Abl, effectively locking out the activating phosphate.
Dasatinib is an ATP-competitive inhibitor but it binds to Bcr-Abl in the active 'type I' conformation in contrast to nilotinib which binds to the inactive conformation.
Imatinib binds to the inactive conformation of the Abl kinase, which adopts a DFG flipped conformation (also termed DFG-out conformation) [13], [14].
