Background

Targeted Protein Degradation

Targeted protein degradation relies on bringing a ubiquitin ligase into close proximity with a target protein.

As such, this modality does not depend on the target protein having a well-defined and accessible active site or functional binding pocket. Affinity screening methods based on ASMS or DEL approaches can identify ligands that bind to any accessible pocket on the target protein.

But not all proteins are the same and not all protein targets are easily degraded. What if you could rapidly assess the feasibility of a degrader project for your protein of interest?


Our CHARMED platform delivers fast, combinatorial degrader discovery. CHARMED delivers rapid synthesis, screening and characterization of potential bifunctional leads. Ready -to-couple plates of diverse linkers and commonly used ligase warheads accelerate the identification of degrader hits for novel targets.

Why CHARMED? Fast, combinatorial degrader discovery

With CHARMED, you can achieve rapid feasibility assessment through:

  • Rapid feasibility of degrading a target using two common ligases
  • Ready-to-couple 96 well plates of ligase warheads attached to linkers
  • Parallel synthesis of bifunctional PROTAC® degrader compounds
  • In stock collection of novel linkers and ligase ligands for lead optimization
  • HTRF®, AlphaLISA® or Jess-system degrader assays for endogenous
    targets
  • Engineered live-cell kinetic degradation assays
  • High throughput in vitro ADME assessment


Why Choose Sygnature Discovery for TPD
Support?

Sygnature Discovery has experience in designing, testing and evaluating targeted protein degraders, supported by expertise in the ubiquitin system and protein degradation biology. Our computational and medicinal chemistry, hit-finding capabilities including HTS and fragment -based screening, and disease area breadth make us a strong partner for targeted protein degradation.

TPD programs bring DMPK and pharmacokinetics complexity, understanding degrader effects in the human body as early as possible, can pay dividends, and our skills and solutions in these areas are built to support that need.



Sygnature Discovery successfully identifies potent SHP2 degrader compounds using its proprietary targeted protein degrader platform, CHARMED, in collaboration with Japanese speciality chemical company, UBE Corporation
Read our recent press release to find out how Japanese specialty chemical company, UBE Corporation, has been collaborating with the team at Sygnature Discovery.

Profile picture of Simon Hirst

Simon Hirst

Chief Executive Officer

Our team

Roland Hjerpe, PhD

Senior Principal Scientist – Induced Proximity Therapeutics (IPT)

Dr. Roland Hjerpe is a drug discovery expert in Targeted Protein Degradation (TPD), with extensive expertise in protein homeostasis and ubiquitin biology. He has over 20 years of experience spanning academia and industry, including research roles at the Universities of Glasgow and Dundee. Dr. Hjerpe has played a key role… Read More
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