Cephalosporin

Creative Biolabs provides customized antibody-antibiotic conjugates (AACs) development services using cephalosporins as payloads for targeted immunotherapy with optimized linkers and conjugation strategies.

Cephalosporins

The cephalosporin was found firstly from the aerobic mold in the sea near a sewage outfall in Su Siccu, Cagliari harbor in Sardinia, by the Italian pharmacologist Giuseppe Brotzu in July 1945. Cephalosporins are used for the prophylaxis and treatment of infections caused by bacteria which is susceptible to this kind of antibiotic. The first-generation cephalosporin predominantly against Gram-positive bacteria, the second to the fourth generation have enhanced activity against Gram-negative bacteria that lead to the more spectral antibacterial capability of cephalosporins. The latest generation cephalosporin has a greater resistance to β-lactamases than the third-generation.

Mode of Action of Cephalosporins

Cephalosporins have the ability of sterilization and they have the same reaction model with other β-lactam antibiotics such as penicillin. Bacteria are generally in the low permeability osmotic pressure environment to spontaneously absorb moisture from the outside. To prevent the crack expansion, bacteria must synthesize cell wall. Peptidoglycan is an essential material in the cell wall of bacteria, which is responsible for cell wall structural integrity. Cephalosporins can disturb the transformation of peptidoglycan-synthesis process of bacteria to inhibit peptidoglycan synthesis, resulting in bacteria loses the ability of resistance to osmotic pressure and burst. In addition, Cephalosporins disrupt the synthesis of the peptidoglycan layer of bacterial cell walls, which is important for cell wall structural integrity, especially for gram-positive bacteria cell.

Fig.1 Mechanism of cephalosporin kills bacteria. Cephalosporin inhibits the synthesis of the peptidoglycan layer of bacterial cell walls which is responsible for cell wall structural integrity. Peptidoglycan synthesis is facilitated by transpeptidases known as penicillin-binding proteins (PBPs). PBPs bind to the D-Ala-D-Ala at the end of peptidoglycan precursors to crosslink the peptidoglycan. Cephalosporin antibiotics mimic the D-Ala-D-Ala site, thereby competitively inhibiting PBP crosslinking of peptidoglycan.

Cephalosporin-based AACs

AACs use cephalosporins as payloads can be a potential therapy for bacterial infection. Namely, the specific targeting capability of a monoclonal antibody enables the delivery of cephalosporins exclusively to the infection site without collateral damage to the normal tissues. β-GlcNAc-WTA mAb is a distinctive monoclonal antibody, which targets bacterial antigen residues β-GlcNAc specifically, and it can be conjugated with a cytotoxic cephalosporin to generate a customized AAC. Upon β-GlcNAc binding, AAC is internalized via receptor-mediated endocytosis and the cephalosporin payload is released to accomplish its cytotoxic effects.

Features

With advanced synthesis platform and the experienced scientists, Creative Biolabs is dedicated to helping customers develop cephalosporins-linker complexes using readily available or customized linkers for antibody conjugation in a cost-effective manner.

• Offer antibody-drug conjugates (ADCs) design with various specialized strategies.
• Perform antibody-antibiotic conjugates (AACs) service with advanced platforms.
• Experienced scientists are committed to providing high-quality services for every customer.
• A good choice for cost-effective service.

Please contact us for more information and a detailed quote.