Highly Specific/Efficient Protein Linker

One Step N-terminal Ligation with Functional Compounds

Advantage and Core Benefit

  • Natural proteins easily functionalized.
  • Homologous molecule obtained with no sidechain reaction.
  • No limitation of N-terminal amino acid residue, except proline.

Potential Applications

  • Pharmaceuticals: Antigen-drug conjugates (ADCs), PEGylation, New modalities (e.g. DNA aptamer-antibody Fc conjugates), TR-FRET libraries for drug discovery, Radio-active labeling for pharmacokinetics
  • Diagnostics: ELISA/RIA, PET/SPECT

Background and Technology

There are several protein linking methods for functionalization. Some methods non-specifically modify functional groups of protein, which might affect original function of the protein, whereas others need protein modification at a gene design level.
Newly developed linker 1H-1,2,3-triazole-4-carbaldehyde (TA4C) derivatives selectively react with N-terminal amine of proteins, which enables to efficiently introduce new functional groups without modifying original function/structure of protein.​

Data

  • TA4C-ligands are easily synthesized with 1-3 steps using previously reported methods.
  • – 80% of RNase was conjugated with Bn using TA4C-Bn within 16 hrs. at pH7.5 and 37℃

Patent/Publication

Researchers

Prof. Akira Onoda (Hokkaido University)

Expectations

  • We are seeking companies to license and commercialize this technology.
  • Samples for your evaluation are available under material transfer agreement (MTA).

 

Project No: KJ-02501

 

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