conjugation of dar

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Conjugation of DAR

• www.creative-biolabs.com/adc

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As one major component of an antibody-drug
conjugate (ADC), the antibody is the key for
target specificity and serves as the cargo to
deliver the cytotoxic drug (payload). A payload
drug can be attached to different sites on an
antibody using diverse conjugation chemistry.
Multiple endogenous amino acids can serve as
potential conjugation sites. However, to achieve
more precisely controlled site-directed
conjugations and subsequently a narrower
distribution of drug-to-antibody ratio (DAR),
special moieties with unique conjugation
chemistries are engineered into antibody
sequences in our antibody design services.
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Some endogenous or engineered sites for the
conjugation of cytotoxic payload drugs to an
antibody (Antibodies,2015).
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To retain antibody bioactivity, mild,
near-physiological conditions are often used for
conjugation reactions. Under these conditions,
endogenous amino acids such as Lys and Cys are
chemically reactive and can be used as
conjugation sites. Scientists at Creative
Biolabs are experienced in performing Lysine
conjugation (amine reaction) as well as Cysteine
conjugation (thiol reactions) to create ADCs
using these endogenous sites. We are also
expertise in exploiting Tyrosine
conjugation approaches as another innovated
endogens site for ADC development.
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One downside in using the endogenous amino acids
for ADC development is a heavily dispersed
drug-to-antibody ratio (DAR) caused by the
non-uniform distribution of the conjugation
sites, especially in the case of Lysine-based
conjugations. Unnatural amino acids (UAAs), such
as p-Acetyl Phenylalanine, are integrated into
antibody sequences via amber stop codon-mediated
transcription and their chemically diverse side
chains are excellent sites to introduce the
payload drug for ADC preparation.
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About

• After years of pursuit for perfection, Creative
  Biolabs has established our leadership in
  targeted immunotherapy and antibody-drug
  conjugate (ADC) development. Creative Biolabs
  offers customers with comprehensive one-stop-shop
  of all aspects in ADC research and evaluation,
  ranging from antigen selection, antibody
  production/optimization, payload-linker
  synthesis, ADC conjugation, to various stages of
  ADC characterization and pre-clinical evaluation.
  Furthermore, inventory also contains an extensive
  list of linkers, payloads, payload-linker sets,
  and commonly used ADCs for quick deployment and
  concept validation.

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Contact

• 45-1 Ramsey Road, Shirley, NY 11967, USA
• Email marketing_at_creative-biolabs.com
• www.creative-biolabs.com/car-t

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