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Drug Discovery

In Vitro Evaluation of PROTAC Molecules

PROTAC (proteolysis-targeting chimera) is a bifunctional specific small molecule. It can be understood as a dumbbell-shaped chimera, of which one end is used to target the target protein to be degraded, the other end is used to recruit protein degradation systems like E3 ubiquitin ligase and both ends are connected by a suitable linker. Therefore, the chimera is a ternary chimera featuring target protein - PROTAC - E3 ubiquitin ligase that promises close connection between target protein and E3 ligase, so that the target protein can be ubiquitinated and then further recognized and degraded by proteasome.

In theory, this new mechanism can target all drug target proteins, especially those that are previously thought to be undruggable, thus expanding the field of drug research and promising incalculable space and application prospects for new drugs R&D. PROTAC technology is novel and has many advantages compared with traditional micromolecule drugs, antibody drugs, RNAi, etc.. It is considered as one of the popularities in the field of drug R&D.

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As a new drug design strategy, drugs with alike triplet micromolecules can theoretically remove any overexpressed and mutated pathogenic proteins in the treatment of diseases. Medicilon has established a complete PROTAC in vitro analysis platform, with main services including:
  • Formation analysis of binary and ternary complexes
    Formation of binary and ternary complexes, based on TR-FRET assays (protein level)Formation of binary and ternary complexes based on Alphascreen assays (protein level)Formation of ternary complexes based on NanoBRET assays (cell level)
  • Target ubiquitination analysis
    Ubiquitination analysis based on Western blot Ubiquitination analysis based on TR-FRET assaysUbiquitination analysis based on Alphascreen assays
  • Target degradation analysis
    Target degradation analysis based on Western blot Target degradation analysis based on In-Cell Western Target degradation analysis based on MSD Target degradation analysis based on HTRF Target degradation analysis based on ELISA Target degradation analysis based on HiBiT
Relevant laboratories
  • Biacore8K
  • PCR
  • Bio-plex
  • centrifuge
  • covaris
  • Gyrolab-xPlore
  • electrochemiluminescence immunoassay
  • high-speed centrifuge
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