Linker Design and Synthesis

The design of linkers and release strategy of antibody-antibiotic conjugate (AAC) essentially follows the same principles as that of antibody-drug conjugate (ADC)- suitable structure must be chosen to achieve a well-balanced combination of drug efficacy, safety, circulation stability, target selectivity and cost. Despite the great progress in linker design over the past decade, several major challenges remain. Among the critical concerns is the fact that antibodies have half-lives of multiple days, therefore a linker is preferred to possess similar stability at physiologically relevant pH so as to prevent pre-mature drug release. In addition, attachment of linker and antibiotic agent to the antibody should have little adverse effect on the biological properties and stability of the antibody. With a deep understanding of important role in the AAC development and years of experience in compound synthesis, Creative Biolabs promise to deliver the most appropriate linker for your project.

Types of Linkers

As a result of the involvement of complex chemical and biological aspects in linker development, only a limited number of linker types are used in existing ADCs, including thioether, peptide, disulfide and hydrazine. In theory, these linkers exhibit different release mechanisms and thus allowing for a variety of conjugation strategies. According to the drug release mechanism, linkers are generally categorized either as cleavable linkers that are prone to chemical or enzymatic cleavage, or as non-cleavable linkers where drug is released upon the degradation of antibody.

AAC linkers

Our Strength

Inspired by the successful examples of chemical linker in previous ADC development, Creative Biolabs has built the “DrugLnk” service platform - a special technical service platform based on our comprehensive understandings of the drug and linker chemistry. “DrugLnk” is tailored into two interactive modules-the drug module and the linker module that both contribute to the drug-linker “warhead” assembly. To accommodate the diverse needs of our worldwide clients, we are proud to offer a large selection of known linkers for regular applications, as well as our featured custom linker services for your specific requirement.

The “DrugLnk” linker module is designated for linker design and we offer the preparation of different linker based on their drug release mechanisms:

  • pH-sensitive linkers provide simple but reliable chemical linkage that is readily hydrolysable under weakly acidic conditions.
  • Disulfide linkers are mimics of natural cysteine bridge, and are thus prone to cleavage in the presence of intracellular thiol nucleophiles (e.g., GSH).
  • Peptide linkers offer excellent releasing specificity that undergo enzymatic cleavage in the lysosome.
  • β-glucuronide linkers are a family of enzymatically cleavable linkers that mediate payload drug release via the linker hydrolysis by the lysosomal enzyme β-glucuronidase (GUSB).
  • Non-cleavable linkers deliver a combination of robustness and target specificity in that they are the least susceptible to cleavage and release payloads intracellularly upon degradation of the antibody.

Relying on the advanced synthetic chemistry platform and a large arsenal of in-house antibiotics, linkers, and drug-linker sets products at Creative Biolabs, in “DrugLnk” our experienced chemists will help clients to:

  • Design and synthesize chemical linkers
  • Select linkers with a suitable release mechanism
  • Structural modification of antibiotics for linker conjugation
  • Characterization of novel linker-payload conjugates
  • Construct antibody-antibiotic conjugates

Creative Biolabs is dedicated to providing quality services and products to promote the progress of AAC linker discovery and development. Our team of skilled scientists work closely with the clients to meet their project objectives and requirements. For more information about our AAC linker service, please contact us for more information and a detailed quote.


Other Antibody-antibiotic Conjugate (AAC):

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