Therapeutic targeting of the Ubiquitin Pathway

There are over 670 post translational modification (PTM) types currently described (1) and it has been estimated that up to 21% of disease associated single nucleotide missense mutations are located in protein PTM sites (2). Besides theflagship PTM target of the phosphorylation pathway (currently 65 FDA approved kinase inhibitor drugs [3]), drugs targeting the acetylation, PARylation and ubiquitination PTM pathways have received FDA approval (4-5, Table 1). This newsletter briefly reviews some of the therapeutic advances in targeting the ubiquitination PTM pathway and highlights the clinical importance and potential of PTMs in drug discovery.

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