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Updated: Aug 30, 2025
Genetic Encoding of a Non-Canonical Amino Acid for the Generation of Antibody-Drug Conjugates Through a Fast Bioorthogonal Reaction
Published on: September 14, 2018
A pH-responsive crosslinker platform for antibody-drug conjugate (ADC) targeting delivery
Francesca Migliorini1, Elena Cini1, Elena Dreassi1
1Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via A.Moro 2, 53100 Siena, Italy. maurizio.taddei@unisi.it.
Abstract:
We report a new 1-6 self-immolative, traceless crosslinker derived from the natural product gallic acid. The linker acts through a pH-dependent mechanism for drug release. This 5-(hydroxymethyl)pyrogallol orthoester derivative (HMPO) was stable for 24 hours at pH values of 7.4 and 6.6 and in plasma, releasing molecules bound to the hydroxymethyl moiety under acid-dependent stimuli at pH 5.5. The linker was non-toxic and was used for the conjugation of Doxorubicin (Doxo) or Combretastatin A4 with Cetuximab. The ADCs formed showed their pH responsivity reducing cell viability of A431 and A549 cancer cells better than Cetuximab alone.
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