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Millipore Technical Publications


Novel Assays to Harness the Drug Discovery Potential of Ubiquitination Pathways

Lit No:PS2486EN00
Year:2011



Ubiquitination is a key regulatory mechanism which attaches the small protein modifier ubiquitin to protein substrates, thereby modifying their structure, function, cellular location, or targeting them for destruction via proteolysis. Inappropriate regulation of ubiquitination pathways is linked with a number of human diseases and in recent years, components of these pathways have emerged as a new and relatively untapped class of targets for drug discovery. Despite a clear opportunity for the development of new therapeutic agents, exploration in this area has been significantly hindered by the complexity of the systems involved and the lack of suitable technology to allow identification of compounds with therapeutic potential. Here, we describe the development of robust assays for a number of ubiquitination pathway enzymes which can be used to screen compounds and assess their selectivity.

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