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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
Neutrophil Elastase-Responsive Linkers for Precision Antibody-Drug Conjugates
Anna C Renner1, Robert B Kargbo2
1North Dakota State University, Fargo, North Dakota 58108-6050, United States.
None:
Antibody-drug conjugates (ADCs) continue to transform oncology, yet premature payload release remains a major source of toxicity. This invention describes a novel class of neutrophil elastase-responsive linker systems that incorporate β-homoamino acids, α-methylamino acids, and polyethylene glycol motifs to improve plasma stability while enabling selective drug release at disease sites. These linker technologies offer a versatile platform for enhancing ADC efficacy, safety, and therapeutic precision.
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