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Allosteric sites (YELLOW) are binding sites remote from the active site (RED) on an enzyme or other protein that when when occupied by a ligand or endogenous regulator can influence the binding behaviour of the active site.
In scenarios where the development of mutational resistance within target binding sites is likely (such as oncology and anti-infectives) allostery offers the ability to dually target 2 distinct sites on the same protein minimising or delaying the onset of resistance
Whilst the active sites of most enzymes and isoforms with a broadly similar function are highly conserved, allosteric sites across these are commonly diverse. Allosteric sites therefore enable better targeting in terms of specificity and selectivity.
New Targeting Paradigms
Allosteric binding sites offer an ideal opportunity for the design and development of 'warheads' for PROTACs (PROteolysis TArgeting Chimeras)
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