Lit Review

Novel drugs for cancer therapy development with PROTAC®

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A review of current homogeneous assay applications for PROTACs

Where traditional drugs can target only around 20% of the proteome, a new technology called PROteolysis TArgeting Chimeras (PROTACs) could reach the other 80%, currently undruggable. This hetero bifunctional molecule promotes protein of interest (POI) ubiquitination by forming a ternary complex with an E3 ligase. The use of PROTACs is a promising and highly appealing technology, but like any new approach a lot of effort is necessary to develop the ternary complex with the best affinity. It has been found that homogeneous assays like HTRF or AlphaLISA are well suited to reaching this goal.

Get your literature review to:

  • Find out recent data about PROTAC ternary complex assessment using homogeneous assays
  • Discover how a warhead or a linker can impact the affinity of the ternary complex
  • Learn how an AlphaLISA protein-protein interaction assay can be used as a screening platform for PROTACs

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