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Cysteine Conjugation

The most basic immunoglobulin G molecule consists of two light chains and two heavy chains connected by non-covalent binding forces and disulfide bonds. The two heavy chains are connected by a disulfide bond in the hinge region (hinge region). The disulfide bond connecting the two heavy chains in the hinge region can be specifically cleaved by reducing agents such as MEA, dithiothreitol (DTT) and tris (2-carboxyethyl) phosphine (TCEP) to generate two Half-antibody molecules, each containing an antigen-binding site.

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Lysine Conjugation

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.

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Chemical Payloads

Most of the compounds currently in clinical trials use maytansine derivatives (DM1/DM4) or auristatin (MMAE/MMAF), which are all microtubule inhibitors. These usually induce apoptosis in cells undergoing mitosis by arresting the cell cycle at G2/M. Recent studies have shown that microtubule inhibitors may also disrupt interphase non-dividing cells.

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Biological Payloads

An antibody-drug conjugate (ADC) connects a biologically active small molecule drug to a monoclonal antibody via a chemical link, and the monoclonal antibody acts as a carrier to target small molecule drugs to target cells. Effective payloads should be highly pharmacological and non-immunogenic, which is especially important in cancer treatment.

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Bioanalytics

ADC has both the specificity of large-molecule drugs and the cytotoxicity of small-molecule drugs, and ADC need to bioquantitate their antibody and small-molecule drug components during the development process. ELISA and LC-MS/MS methods have become common bioanalytical techniques for ADC analysis. In the process of ADC drug development, structural confirmation, characterization, and quality control are all important links, which must be as accurate, sensitive and selective as possible.

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Bioassays

In order to ensure the safety, effectiveness, and quality of the drug, the activity needs to be tested during the development of ADC. Viability measurement is one of the most important indicators to ensure the effectiveness of a drug. Methods for viability detection include: in vivo assays, in vitro animal organ assays, biochemical enzyme reaction assays, immunological activity assays, and in vitro cell culture assays.

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BOC Sciences has been committed to providing customers with high-quality products and services for antibody-drug conjugate research. Our unparalleled platform and outstanding drug discovery expertise allow us to provide you with comprehensive data and unique insights to provide you with the depth and breadth of science to advance your drug discovery program.

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About Us

BOC Sciences offers customers with comprehensive one-stop-shop of all aspects in antibody-drug conjugate (ADC) research and evaluation, ranging from antibody modification and conjugation technologies, ADC payloads development, payload-linker synthesis, ADC conjugation, to various stages of ADC characterization and manufacture. Furthermore, we also provide an extensive list of linkers, payloads and payload-linker sets.
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