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In Vitro Evaluation of PROTAC Molecules

In Vitro Evaluation of PROTAC Molecules

PROTAC (proteolysis-targeting chimera) are bifunctional specific small molecules that can target otherwise undruggable target proteins for degradation, thereby reducing their biological activity in a cell. 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, a ternary chimera is formed featuring target protein - PROTAC - E3 ubiquitin ligase that ensures 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 previously thought to be undruggable, thus expanding the field of drug research and promising prospects for new drugs R&D. PROTAC technology is novel and has many advantages compared with traditional micromolecule drugs, antibody drugs, RNAi.. It is considered one of the most popular new modalities in drug discovery and Medicilon is highly experienced in PROTAC development.

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As a new drug design strategy, drugs with alike triplet micromolecules can theoretically remove any protein 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
Service Cases

Signing Ceremony for Strategic Cooperation Between Gluetacs and Medicilon IND R&D Service.webp

Signing Ceremony for Strategic Cooperation Between Gluetacs and Medicilon IND R&D Service

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Medicilon Assists | Cullgen's class 1 new drug TRK degrader CG001419 was approved for clinical use.webp

Medicilon Assists | Cullgen's class 1 new drug TRK degrader CG001419 was approved for clinical use

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 CGeneTech and Medicilon Held the Conference Titled PROTAC Project Contract Signing & Kick-off Meeting.webp

CGeneTech and Medicilon Held the Conference Titled "PROTAC Project Contract Signing & Kick-off Meeting"

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