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Bioorthogonally Activated Target Identification Platform

A novel affinity labelling platform, with greater labelling efficiency than photoaffinity labelling (PAL) and no dependence on linker length

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Project Overview

  • Target identification (Target ID) is a critical step in the drug discovery process for identifying the pharmacological target of a drug and potential off-target effects, but it is often difficult and time-consuming.
  • Target ID is particularly challenging when the protein–small molecule interaction is weak. In these circumstances, photoaffinity labelling (PAL) is the current gold standard. Unfortunately, PAL methods are plagued by low labelling efficiency and dependence on linker length, as well as prone to false-positive and false-negative identifications.
  • There is a need for new affinity labelling methods for enhancing small molecule–protein interactions without these limitations.
  • Dana-Farber scientists have developed a platform addressing these limitations and are looking for collaborations or sponsored research partnerships to advance this technology.

Technology

Dana-Farber has created a novel affinity labelling platform that is bioorthogonally activated and quickly and accurately labels proteins in a small molecule dependent manner. In Target ID experiments with a known protein-small molecule pair, this method labelled the protein of interest with 14x greater efficiency compared to gold standard PAL. Further experiments with several known protein-small molecule pairs demonstrated that the use of this method resulted in strikingly lower incidences of false-positive and false-negative rates compared to PAL methods. 

Benefits:

  • New alternative method to PAL for Target ID enhancement 
  • No dependence on linker length 
  • Greater labelling efficiency 
  • Lower false-positive and false-negative rates 

Further details:

Siriwongsup, Surached et al. Bioorthogonally activated reactive species for target identification Chem, Volume 10, Issue 4, 1306 – 1315

Team Members: Justin Kim, PhD, Surached (James) Siriwongsup, PhD

Opportunities

Dana-Farber is looking for commercial collaboration or sponsored research opportunities. 

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Team Members