Since less than 20% of the proteome has enzymatic activity and current drug development efforts rely heavily on the identification of enzymatic inhibitors, a significant fraction of the proteome, aka 'The Undruggable Proteome�, is currently being ignored.  Given the lack of active sites to inhibit, one possible solution to this problem is to induce the degradation of these proteins with a small molecule.  Using heterodimeric ligands to recruit target proteins to the intracellular protein degradation machinery, my lab has been able to selectively knock down intracellular levels of specific proteins, thus allowing one to target those proteins that are currently not 'pharmacologically vulnerable'.

Small molecule control of targeted protein degradation

244th National Meeting (2012)

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