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Allosteric Sites
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Allosteric Sites

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.

Allosteric Modulation

Allosteric Modulation

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Allostery Benefits
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Addressing resistance

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


Improved specificity

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. 

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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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