Abstract
Protein kinases are now recognised as an important class of drug targets.
Whilst many protein kinase inhibitors directly interact with the
ATP-binding site, Gleevec is a notable example from a new class of
allosteric inhibitors that alter protein kinase conformation to block
productive ATP binding. Recently, kinase inhibitors with different
mechanisms of action have also been described. Some of these are
allosteric inhibitors that alter kinase conformation and prevent
protein substrate binding. Other inhibitors directly compete with
protein substrate binding. These inhibitors promise exciting therapeutic
opportunities by exploiting new mechanisms of action and may thus
allow greater specificity in protein kinase inhibition with fewer
off-target side effects.
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