Lysine Conjugation

Lysine Conjugation

BOC Sciences can perform lysine conjugation in antibody-drug conjugate (ADC) development. Scientists from BOC Sciences are able to provide ADC suitable for commercial, low-cost and large-scale production, based on a thorough understanding of your individual needs.

Lysine-linked ADC

A humanized antibody contains 80 to 90 lysins, so modification of partial lysine has no effect on the natural disulfide bond, nor does it significantly change the stability, biophysical properties, or affinity of the antibody. However, through lysine conjugation, each antibody will be coupled with 0~8 small molecule drugs, and the location of the coupling may occur on nearly 40 different lysine residues on the light and heavy chains of the antibody, and more than 1 million ADCs will be generated. When a small molecule of a drug is anchored to a monoclonal antibody's lysine by a covalent bond, the ADC is able to control the number of small molecule drugs in the chain.

An example of a disulfide-containing ADC is the attachment of DM1 or DM4 to an immunoglobulin. It is transported to the lysosome by vesicle transport by endocytosis of the antigen, and the monoclonal antibody is degraded to provide a lysine derivative linked to a small molecule drug. Further changes in the cell, such as the disulfide linkage, are broken by the exchange of disulfide bonds, and finally the thiol may be methylated by methyltransferase to form a potent derivative of DM1 or DM4. These methylated drugs can penetrate the cell membrane to exert a broader effect. The drug not only kills cells from the inside, but also kills nearby cells that do not express antigen.

Advantages of Lysine Conjugation

  • The most common method of non-specific coupling
  • Large number of lysine residue sites for modification in IgG scaffolds

We offer the following services

  • The lysine conjugation method is generally divided into a one-step coupling method and a two-step coupling method.
  • In a one-step binding, the lysine ε-amino group of the antibody reacts with the amine reactive group of the drug to form an amide bond.
  • Although the two-step conjugate first introduces a chemical function to modify the lysine residue of the antibody. BOC Sciences can couple small molecule drugs to peptide through isomeric peptide bond at high specific site in vitro, and the binding site only occurs at the ε - amino site of lysine in specific amino acid sequence.

Our advantages

  • Skilled chemistry team
  • Fully equipped analytical support
  • High quality, low cost products
  • Advanced technology and methods
  • Personalized service
  • Strict quality control
* Only for research. Not suitable for any diagnostic or therapeutic use.

Get in Touch

Verification code
Inquiry Basket