Highly Specific/Efficient Protein Linker

Simple Step N-terminal Ligation with Functional Compounds

Advantages

  • Functionalized natural proteins are easily available
  • Homologous molecules can be obtained with high efficiency and no sidechain reaction.
  • No restriction of N-terminal amino acid species

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 two linkers selectively react with N-terminal amine and enable to efficiently introduce new functional groups without modifying original function/structure of protein.

無題

Data

Linker 1 (TA4C method)

  • TA4C-ligands are synthesized easily by 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℃

Linker 2 (6AMPC method)

  • 6AMPC is synthesized by 5 steps.
  • ~80% of RNase was modified with 6AMPC at pH7.5 and 37℃ for 16 hrs, followed by conjugation with a ligand compound through CuAAC reaction at pH7.5 and room temperature for~2hrs.

Patent

Pending (Unpublished)

Researcher

Prof. Takashi HAYASHI    Department of Applied Chemistry, Graduate School of Engineering, Osaka University, Japan (http://www.applied-bioinorganic.jp/en/).

Expectations

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

Product No. : CD-02501

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