Protein-protein interactions (PPIs) regulate a host of critical cellular functions, from DNA replication and repair to intracellular communication and programmed cell death.  Aberrant or malfunctioning PPIs can cause a plethora of diseases and as such are a very attractive target for therapeutic intervention.Here, we describe the development of small-molecules designed to modulate interacting proteins, based on computational inspection of the protein interface.  A modular synthetic approach was employed, wherein individual building blocks were coupled together to form a scaffold, from which appropriate functionality can be appended in order to target 'hot-spot' residues on the protein surface.

Modulating protein-protein interactions with small molecules

243rd National Meeting (2012)

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