Instead, omecamtiv mecarbil binds to
an allosteric site that stabilizes states of the motor domain primed to interact with actin at the beginning of force production, thus increasing the number of motors that can participate in force production once the cardiac contraction cycle starts during systole.
The new paper by Tonks and collaborators importantly reveals an alternative binding site, called
an allosteric site, that does not present the biochemical difficulties that the main, or «catalytic,» binding site does.
Based on this work, the researchers identified a previously unknown regulatory mechanism in 2 - epimerase that involves direct interaction between one substrate molecule in the enzyme's active site and another in the enzyme's
allosteric site.
Fischetti and his colleagues chose to target
the allosteric site of 2 - epimerase to develop inhibitory compounds, because it is found in other bacterial 2 - epimerases but not in the human equivalent of the enzyme.
Not exact matches
S - citalopram molecules bound to the
allosteric (yellow) and central (magenta)
sites are shown as spheres.
One approach is based on the combination of ATP - binding
site inhibitors with so - called
allosteric inhibitors, which bind to a different location.