Design and Synthesis of Compound-specific Haptens for Sulfonamides

Creative Biolabs has extensive experience and impressive performance in the field of small molecule drugs and antibody development. With the deepening of the research on small molecule drugs, the demand for anti-drug antibodies is also increasing. Creative Biolabs, relying on its own expertise in these two fields, can provide customers with excellent hapten design and synthesis services to help customers develop better antibodies.

Necessity for Development of Antibodies Against Sulfonamides

Sulfonamides (SAs) are one of the most widely used antibacterial drugs in the global livestock industry. Most of the SAs drugs contain sulfonylamino groups, and the difference in the R group connected to the N1 position causes the structural differences of each monomer drug. SAs ingested by the human can accumulate in the body, which is not only harmful to the human body, but also causes resistance to many bacteria. Therefore, the EU, the United States, and China have all limited the total amount of SAs and the content of individual SAs in animal products to no more than 0.1 mg/kg. Existing instrument methods can meet the needs of sensitivity for the detection of SAs, but they are slow and inefficient, and not suitable for the detection of a large number of samples. Antibody-based immunoassay technology can replace instrumental methods for the screening and detection of large numbers of samples, and has become a hot spot in the field of residue detection. As a key reagent for immunoassay, the nature of the antibody determines the sensitivity and specificity of the detection method. Therefore, reasonable hapten design and preparation has become a bottleneck problem that restricts the development of antibody preparation technology and obtains ideal antibodies.

Toxic pig dissection. Fig.1 Toxic pig dissection.

Design and Synthesis of Compound-specific Haptens for Sulfonamides

In antibody preparation, the first step is the design and synthesis of the antigen, which is the key to the success of antibody preparation. If the synthetic antigens can fully expose the required epitopes, then the body can more easily recognize the epitopes, so that the specificity and affinity of the antibodies produced by the immunized animals fit the epitopes to the greatest extent. Therefore, designing and synthesizing antigens is particularly important in the process of preparing antibodies.

Before designing, the structure of the antigen to be synthesized should be carefully analyzed to find out the position of the antigen activity and the position of its epitope. The parent of SAs is p-aminobenzenesulfonamide. Most of the SAs have an N1 terminal connected to a substituent and its N4 terminal is an amino group, which means that various drugs have different activities due to the different N1 terminal substituents. Therefore, for antibodies against SAs, the antigen synthesis can choose to connect the protein at the N4 end and expose the pyrimidine ring at the N1 end, so that the body can produce antibodies against a specific SA after immunization. If carrier protein is connected at the N1 end, the hapten exposes the parent sulfamate core common to the SAs, so the prepared antibody will have greater cross-section, and it will be easier to identify other SAs (class-specific haptens for SAs).

Design of compound-specific haptens for sulfonamides. Fig.2 Design of compound-specific haptens for sulfonamides.

Based on the principle that the hapten should be coupled to the carrier to maintain and highlight the characteristic structure especially the three-dimensional structure of the analyte in the bound antigen, scientists at Creative Biolabs use computational chemistry to study the structure-activity relationship between small molecules and antibodies to better understand the antibody-antigen binding at the molecular level. And use non-characteristic structural parts of the analyte as spacers or construct spacers to couple the N4 end of SAs with various carrier proteins to prepare complete antigens to make antibodies specific to a particular SA. According to the basic strategy above and the specific needs of customers, we can provide you with professional hapten design, modification and synthesis services.

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